Name: Ezetimibe (SCH-58235)
Brand: Selleck Chemicals
SKU: S1655
Rating: 5 (21 reviews)

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Controllo Qualità (Quality Control)

Lotto: Purezza: 99.91%

99.91

Target correlati	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Altro LDL Inibitori	Phillygenin Cashew Extract

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	409.4	Formula	C₂₄H₂₁F₂NO₃	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	163222-33-1	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	SCH-58235			Smiles	C1=CC(=CC=C1C2C(C(=O)N2C3=CC=C(C=C3)F)CCC(C4=CC=C(C=C4)F)O)O

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 82 mg/mL (200.29 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 82 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.
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.
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.
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.
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 l'esperimento)

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 c'è 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, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Targets/IC₅₀/Ki	NPC1L1
In vitro	Ezetimibe (SCH-58235) produces a significant reduction in total cholesterol, LDL cholesterol, and triglycerides as well as a small but significant increase in HDL cholesterol. This compound reduces cholesterol transport by 31% in Caco-2 cells, but not retinol transport. It results in a significant decrease in mRNA expression for the surface receptors SR-BI, Niemann-Pick type C1 Like 1 protein (NPC1L1), and ATP-binding cassette transporter, subfamily A (ABCA1) and for the nuclear receptors retinoid acid receptor (RAR)gamma, sterol-regulatory element binding proteins (SREBP)-1 and -2, and liver X receptor (LXR)beta as assessed by real-time PCR analysis in Caco-2 cells.
In vivo	Ezetimibe (SCH-58235) reduces plasma cholesterol levels from 964 to 374 mg/dL, from 726 to 231 mg/dL, and from 516 to 178 mg/dL in the western, low-fat, and cholesterol-free diet mice, respectively. It reduces aortic atherosclerotic lesion surface area from 20.2% to 4.1% in the western diet group and from 24.1% to 7.0% in the low-fat cholesterol diet mice. This compound reduces carotid artery atherosclerotic lesion cross-sectional area by 97% in the western and low-fat cholesterol groups and by 91% in the cholesterol-free mice. It inhibits cholesterol absorption, reduces plasma cholesterol, increases high density lipoprotein levels, and inhibits the progression of atherosclerosis under western, low-fat, and cholesterol-free dietary conditions in apoE-/- mice. Ezetimibe potently inhibits the transport of cholesterol across the intestinal wall, thereby reducing plasma cholesterol in preclinical animal models of hypercholesterolemia. It eliminates exocrine pancreatic function from the intestine while maintaining bile flow, as established in the rat. The compound reduces plasma cholesterol and hepatic cholesterol accumulation in cholesterol-fed hamsters with an ED(50) of 0.04 mg /kg.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/14695813/ [2] https://pubmed.ncbi.nlm.nih.gov/16177187/ [3] https://pubmed.ncbi.nlm.nih.gov/11742881/ [4] https://pubmed.ncbi.nlm.nih.gov/16801428/ [5] https://pubmed.ncbi.nlm.nih.gov/11564660/ [6] https://pubmed.ncbi.nlm.nih.gov/17587760/

Applicazioni (Applications)

Metodi	Biomarcatori	Immagini	PMID
Western blot	p-AMPK / AMPK LC3B-I / LC3B-II / Nuclear TFEB PCSK9 / LDLR / SREBP2 / HNF1-a		28933629

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2025-08-07)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT06722521	RECRUITING	Primary Prevention; Vascular Calcification	Asan Medical Center	2025-07-09	PHASE4
NCT07524101	RECRUITING	Renal Insufficiency; Atherosclerosis; Dyslipidemia; Hypercholesterolemia; Cardiovascular Diseases	Yonsei University	2026-05-28
NCT05579626	ENROLLING_BY_INVITATION	Pre Diabetes; ASCVD	Seung-Whan Lee, M.D., Ph.D.	2023-03-14	PHASE4
NCT06649240	RECRUITING	Ischemic Stroke; Small Vessel Cerebrovascular Disease; Cholesterol, LDL; Secondary Prevention; Cardiovascular Diseases	Seoul National University Hospital	2024-10-04
NCT07359105	RECRUITING	Dyslipidemia Associated With Type II Diabetes Mellitus	Sin Gon Kim	2026-03-09
NCT07799779	NOT_YET_RECRUITING	Acute Coronary Syndromes (ACS)	Seoul National University Bundang Hospital	2026-09	PHASE4

Domande Frequenti (Frequently Asked Questions)

Domanda 1:
I am planning to deliver it per orally and wonder proper vehicle for this compound and effective dose level for lowering intestinal cholesterol absorption.

Risposta:
It can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 10 mg/ml clearly. If you are going to use this vehicle, please dissolve the compound in DMSO clearly first. Then add PEG 300 and Tween 80, after mixed homogeneously, then dilute with water.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Ezetimibe (SCH-58235) LDL Modulatore

Peso molecolare: 409.4