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4-Methylumbelliferone (4-MU)

Name: 4-Methylumbelliferone (4-MU)
Brand: Selleck Chemicals
SKU: S2256
Rating: 5 (5 reviews)

N. Cat.S2256

4-Methylumbelliferone è un inibitore della sintesi dell'acido ialuronico (HA) con un IC50 di 0,4 mM.

4-Methylumbelliferone (4-MU) Chemical Structure

Struttura chimica

Peso molecolare: 176.17

Vai a

Controllo Qualità

Lotto: Purezza: 99.89%

99.89

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Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dellattività
COS1 cells	Function assay			Agonistic activity was determined in COS1 cells transfected with GAL 4-PPAR gamma receptor, EC50=0.021 μM
CV-1 cells	Function assay			Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay, EC50=0.043 μM
COS-1 cells	Function assay			In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cells, EC50=0.02 μM
CV-1 cells	Function assay			Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells, EC50=0.08913 μM
CV-1 cells	Function assay			In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells, EC50=0.06 μM
COS-1 cells	Function assay			In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells, EC50=0.02 μM
CV-1 cells	Function assay			In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined, EC50=0.325 μM
HepG2 cells	Function assay			Effective concentration against human PPARgamma expressed in HepG2 cells, EC50=0.039 μM
Huh7 cells	Function assay			Functional activity at human PPAR gamma in Huh7 cells by transactivation assay, EC50=0.22 μM
Huh7 cells	Function assay			Effect on PPAR gamma transactivation activity in Huh7 cells, EC50=0.22 μM
U2OS cells	Function assay			Effect on PPARgamma transactivation activity in U2OS cells, EC50=0.03 μM
CV1 cells	Function assay			Transactivation of PPARgamma in CV1 cells, EC50=0.076 μM
human keratinocytes	Proliferation assay			Antiproliferative activity against human keratinocytes, EC50=8 μM
HT29 cell	Proliferation assay			Antiproliferative activity against human HT29 cell line, EC50=45 μM
NIH3T3 cells	Function assay			Activity at human PPAR gamma transfected in NIH3T3 cells by luciferase activity assay, EC50=0.32 μM
CV1 cells	Function assay			Transactivation of human PPARgamma in CV1 cells by luciferase reporter gene assay, EC50=0.308 μM
Huh7 cells	Function assay			Activity at human PPAR gamma in Huh7 cells by transactivation assay, EC50=0.22 μM
HepG2 cells	Function assay			Agonist activity at human PPAR gamma in a HepG2 cells by PPAR-GAL4 transactivation assay, EC50=0.158 μM
HepG2 cells	Function assay			Agonist activity at human PPAR gamma in HepG2 cells by PPAR-GAL4 transactivation assay, EC50=0.158μM
CV1 cells	Function assay			Activity at human PPARgamma in CV1 cells, EC50=0.308 μM
HEK293 cells	Function assay			Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay, EC50=0.31 μM
rat L6 cells	Function assay			Effect on fatty acid oxidation in rat L6 cells, EC50=5 μM
HepG2 cells	Function assay			Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assay, EC50=0.082 μM
CV1 cells	Function assay			Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs, EC50=3.46 μM
CV1 cells	Function assay			Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs, EC50=0.03 μM
CV1 cells	Function assay			Agonist activity at human PPARgamma expressed in CV1 cells by receptor transactivation assay, EC50=0.308 μM
CV1 cells	Function assay			Agonist activity at PPARgamma in CV1 cells by transactivation assay, EC50=0.308 μM
HEK293 cells	Function assay			Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay, EC50=0.035 μM
NIH3T3 cells	Function assay			Agonist activity at human PPARgamma expressed in NIH3T3 cells by GAL4 transactivation assay, EC50=0.32 μM
HEK293 cells	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells by GAL4 transactivation assay, EC50=0.19 μM
HEK293 cells	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells assessed as aP2 gene induction, EC50=0.12 μM
HEK293 cells	Function assay			Agonist activity at PPARgamma in HEK293 cells by GAL4 transactivation assay, EC50=0.045 μM
HepG2 cells	Function assay			Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay, EC50=0.039 μM
RAW264.7 cells	Function assay			Suppression of LPS/IFN-gamma-stimulated NO production in mouse RAW264.7 cells, EC50=17.5 μM
BL21 cells	Function assay			Displacement of radio labeled 2(S)-(2-benzoyl-phenylamino)-3-{4-[1,1-ditritio-2-(5-methyl-2-phenyl-oxazol-4-yl)-ethoxy]-phenyl}-propionic acid from GST-fused human PPARgamma expressed in Escherichia coli BL21 cells by scintillation proximity assay, EC50=0.45 μM
BHK21 cells	Function assay			Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay, EC50=0.45 μM
HepG2/C3A cells	Function assay			Activation of human PPARgamma ligand binding domain-mediated transcriptional activity in human HepG2/C3A cells co-transfected with fused Gal4-LBD by cotransfection assay, EC50=0.0038 μM
HepG2 cells	Function assay			Agonist activity at PPARgamma expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control, EC50=0.05 μM
COS1 cells	Function assay			Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay, EC50=0.02 μM
HepG2 cells	Function assay			Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay, EC50=0.223 μM
CV1 cells	Function assay			Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50=0.033 μM
CV1 cells	Function assay			Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50=3.46 μM
U2OS cells	Function assay			Agonist activity at human PPARgamma in U2OS cells by transactivation assay, EC50=0.02 μM
Hep G2 cells	Function assay			Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay, EC50=0.04 μM
HeLa cells	Function assay			Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay, EC50=0.015 μM
COS1 cells	Function assay			Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay, EC50=0.02 μM
U2OS cells	Function assay			Agonist activity at human PPARgamma expressed in U2OS cells by luciferase transactivation assay, EC50=0.05 μM
HepG2 cells	Function assay			Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay, EC50=0.039 μM
HepG2 cells	Function assay			Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay, EC50=0.223 μM
COS7 cells	Function assay			Agonist activity at human recombinant PPARgamma2 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay, EC50=0.1 μM
COS7 cells	Function assay			Agonist activity at human recombinant PPARgamma1 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay, EC50=0.03 μM
HEK cells	Function assay			Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay, EC50=10.58 μM
HEK cells	Function assay			Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay, EC50=0.035 μM
3T3L1 cells	Function assay		7 days	Induction of adipogenesis in mouse 3T3L1 cells assessed as increase in lipid accumulation after 7 days by Oil red O staining
CHO-K1 cells	Function assay			Partial agonist activity at human PPARgamma-LBD expressed in CHO-K1 cells co-transfected with GAL4 assessed as luciferase activity by transactivation assay, EC50=0.1 μM
HEK293T cells	Function assay	1 μM	24 hrs	Partial agonist activity at human PPARgamma-LBD expressed in HEK293T cells assessed as induction of receptor transactivation at 1 uM after 24 hrs by luciferase reporter gene assay
CV1 cells	Function assay			Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay, EC50=0.1 μM
HEK293 cells	Function assay		16 to 20 hrs	Transactivation of Gal4-fused human PPARgamma expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assay, EC50=0.043 μM
HepG2 cells	Function assay	10 umol/L	24 hrs	Increase in glucose consumption in human HepG2 cells at 10 umol/L after 24 hrs relative to control
3T3L1 cell	Function assay	1 uM		Induction of mouse 3T3L1 cell differentiation assessed as increase in accumulation of intracellular lipid droplet at 1 uM by Oil red O staining
CV1 cells	Function assay		40 h	Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay, EC50=0.1 μM
HepG2 cells	Function assay			Agonist activity at PPARgamma receptor expressed in human HepG2 cells by PPRE-luciferase reporter gene assay, EC50=0.01 μM
HepG2 cells	Function assay			Transactivation of human PPARgamma expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay, EC50=0.05 μM
COS7 cells	Function assay			Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay, EC50=0.043 μM
COS-1 cells	Function assay		24 hrs	Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis, EC50=0.048 μM
COS1 cells	Function assay		24 hrs	Transactivation of human full length PPARgamma expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay, EC50=0.12 μM
MG-63 cells	Function assay			Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay, EC50=0.011 μM
COS1 cells	Function assay			Binding affinity to human wild type PPARgamma LBD expressed in COS1 cells co-expressing GAL4 by scintillation proximity assay
MG-63 cells	Function assay		24 hrs	Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay, EC50=0.011 μM
Ac2F cells	Function assay	0.1 to 10 μM	6 hrs	Agonist activity at PPARgamma in rat Ac2F cells assessed as luciferase activity at 0.1 to 10 uM after 6 hrs by reporter gene assay
293H DA cells	Function assay		16 h	Agonist activity at PPARgamma LBD in human 293H DA cells after 16 hrs by TR-FRET activation reporter assay, EC50=0.0024 μM
3T3L1 cells	Function assay	10 uM		Increase in adiponectin mRNA levels in TNFalpha-induced mouse 3T3L1 cells pretreated at 10 uM before TNF-alpha challenge relative to control
HepG2 cells	Function assay	10 uM	24 h	Reduction of glucose consumption in insulin-resistant human HepG2 cells at 10 uM after 24 hrs by glucose oxidase method in presence of 22.2 mM of glucose
HepG2 cells	Function assay	10 uM	24 h	Reduction of glucose consumption in insulin-resistant human HepG2 cells at 10 uM after 24 hrs by glucose oxidase method in presence of 0.1 uM of insulin
THP1 cells	Function assay	100 uM	3 hrs	Transactivation of PPARgamma in human THP1 cells assessed as decrease in LPS-induced MCP1 mRNA expression at 100 uM preincubated for 3 hrs prior to LPS challenge measured after 18 hrs by RT-PCR analysis relative to untreated control
THP1 cells	Function assay	100 uM	3 hrs	Transactivation of PPARgamma in human THP1 cells assessed as decrease in LPS-induced IL6 mRNA expression at 100 uM preincubated for 3 hrs prior to LPS challenge measured after 18 hrs by RT-PCR analysis relative to untreated control
HepG2 cells	Function assay			Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells by luciferase reporter gene assay, EC50=0.1 μM
HepG2 cells	Function assay		20 h	Agonist activity at human GAL4-fused PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay, EC50=0.02 μM
BL21 DE3 cells	Function assay			Displacement of [3H]rosiglitazone from N-terminal His-tagged human PPARgamma ligand binding domain expressed in Escherichia coli BL21 DE3 cells by scintillation proximity assay, Ki=0.074 μM
human L02 cells	Function assay			Agonist activity at PPARgamma-LBD expressed in human L02 cells co-expressing pGL3-SV40-GAL4 after 24 hrs by luciferase reporter gene based transactivation assay, EC50=0.9 μM
HepG2 cells	Function assay		20 h	Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay, EC50=0.039 μM
HEK293 cells	Function assay	10 μM		Transactivation of PPARgamma (unknown origin) expressed in HEK293 cells co-transfected with AP2-PPRE at 10 uM by luciferase reporter gene assay
HEK293 cells	Function assay			Agonist at human PPARgamma LBD expressed in human HEK293 cells cotransfected with GAL4-Luc assessed as transcriptional activation by luciferase reporter gene assay, EC50=0.004 μM
HEK293 cells	Function assay		24 h	Transactivation of GAL4 DBD-fused human PPARgamma-LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay, EC50=0.1 μM
HEK293 cells	Function assay		48 hrs	Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay, EC50=43.71 μM
HepG2 cells	Function assay			Agonist activity at GAL4-fused PPARgamma (unknown origin) expressed in human HepG2 cells by transactivation assay, EC50=0.01 μM
HepG2 cells	Function assay			Agonist activity at GAL4-fused PPARgamma M463A mutant (unknown origin) expressed in human HepG2 cells by transactivation assay, EC50=0.002 μM
L6 cells	Function assay		24 hrs	Induction of glucose uptake in rat L6 cells pulsed with C14-deoxy glucose after 24 hrs in presence of insulin, EC50=4.49 μM
L6 cells	Function assay		16 hrs	Increase in 2-[3H]-deoxyglucose uptake in rat L6 cells after 16 hrs by scintillation counting analysis, EC50=4.8 μM
DU145 cells	Cytotoxicity assay		48 hrs	Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay, EC50=16 μM
PC3 cells	Cytotoxicity assay		48 hrs	Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay, EC50=20.3 μM
MDA-MB-231 cells	Growth inhibition assay		24 hrs	Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay, EC50=5.23 μM
HEK293 cells	Function assay			Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase reporter gene assay, EC50=0.01 μM
HepG2 cells	Function assay		20 hrs	Transactivation of PPAR transfected in human HepG2 cells after 20 hrs by PPAR-luciferase assay, EC50=1.6 μM
HEK293 cells	Function assay		24 hrs	Transactivation of PPARgamma (unknown origin) expressed in HEK293 cells incubated for 24 hrs by luciferase reporter gene assay
HepG2 cells	Function assay			Agonist activity at human GAL4-PPARgamma ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay, EC50=0.039 μM
HEK293 cells	Function assay		24 hrs	Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay, EC50=0.03 μM
HepG2 cells	Function assay		20 hrs	Agonist activity at GAL4-DNA binding domain fused human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay, EC50=0.04 μM
HepaR cells	Function assay		1 day	Agonist activity at PPARgamma in human HepaR cells assessed as increase in HMGCS2 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control
HepaR cells	Function assay	1 uM	1 day	Agonist activity at PPARgamma in human HepaR cells assessed as increase in ANGPTL4 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control
HepaR cells	Function assay	1 uM	1 day	Agonist activity at PPARgamma in human HepaR cells assessed as increase in FABP1 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control
HEK293 cells	Function assay	10 μM	24 hrs	Transactivation of PPAR-gamma (unknown origin) expressed in HEK293 cells at 10 uM after 24 hrs by luciferase reporter gene assay
C2C12 cells	Function assay	30 μM	2 h	Induction of 2-deoxy-[3H]-glucose uptake in mouse C2C12 cells at 30 uM after 2 hrs by liquid scintillation counting analysis
MCF7 cells	Function assay		16 h	Agonist activity at human PPARgamma transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay, EC50=0.087 μM
HEK293 cells	Function assay	10 μM	24 h	Agonist activity at PPARgamma (unknown origin) expressed in HEK293 cells assessed as receptor transactivation at 10 uM incubated for 24 hrs by luciferase reporter gene assay
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Informazioni chimiche, conservazione e stabilità

Peso molecolare	176.17	Formula	C₁₀H₈O₃	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	90-33-5	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	N/A			Smiles	CC1=CC(=O)OC2=C1C=CC(=C2)O

Solubilità

In vitro
Lotto:

DMSO : 35 mg/mL (198.67 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 35 mg/mL

Water : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	10.000mg/ml (56.76mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	3.000mg/ml (17.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Informazioni sullo studio clinico

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT05295680	Recruiting	Primary Sclerosing Cholangitis	Aparna Goel\|Stanford University	May 10 2023	Phase 2

Supporto tecnico

Istruzioni per la manipolazione

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