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[(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate

Basic information Safety Supplier Related

[(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate Basic information

Product Name:
[(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate
Synonyms:
  • PF-06424439
  • [(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate
  • PF-06424439 methanesulfonate
  • PF-06424439 >=98% (HPLC)
  • acyl-CoA:cholesterol acyltransferase,Inhibitor,Acyltransferase,mono- acylglycerol acyltransferase,PF-06424439,PF 06424439 methanesulfonate,inhibit,Diacylglycerol acyltransferase,PF06424439,Diglyceride acyltransferase,PF06424439 methanesulfonate,PF 06424439
  • (R)-(1-(2-(1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl)-1H-imidazo[4,5-b]pyridin-5-yl)piperidin-3-yl)(pyrrolidin-1-yl)methanone methanesulfonate
CAS:
1469284-79-4
MF:
C23H30ClN7O4S
MW:
536.0468
Mol File:
1469284-79-4.mol
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[(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate Chemical Properties

storage temp. 
room temp
solubility 
H2O: soluble10mg/mL, clear
form 
powder
color 
white to light brown
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Safety Information

WGK Germany 
3
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[(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate Usage And Synthesis

Description

PF-06424439 is an orally bioavailable inhibitor of diacylglycerol acyltransferase 2 (DGAT-2; IC50 = 14 nM). It is selective for DGAT-2 over the related acyltransferases DGAT-1, MGAT-2, and MGAT-3 (IC50s = >50 μM). PF-06424439 (0.1-10 mg/kg) reduces plasma triglyceride levels in sucrose-fed rats in a dose-dependent manner. It also reduces plasma levels of cholesterol and triglycerides as well as hepatic triglycerides in LDL receptor knockout mice fed a high-fat, high-cholesterol diet when administered at a dose of 60 mg/kg per day.

Uses

PF-06424439 has been used as a diacylglycerol acyltransferase 2 (DGAT2)?inhibitor:

  • to study its effects on cell mortality and lipid synthesis in epithelial colon cells and colorectal cancer stem cells
  • to study its effects on HeLa cells
  • to study its inhibitory effects on neutral lipid synthesis in HT-1080 cells

Biochem/physiol Actions

PF-06424439 is a potent and selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).

storage

Desiccate at RT

[(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonateSupplier

Shanghai Aladdin Bio-Chem Technology Co.,LTD
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18521735133 18521732826;
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Guangzhou Isun Pharmaceutical Co., Ltd
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020-39119399 18927568969
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isunpharm@qq.com
ShangHai Caerulum Pharma Discovery Co., Ltd.
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18149758185
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sales-cpd@caerulumpharma.com
Sigma-Aldrich
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021-61415566 800-8193336
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orderCN@merckgroup.com
Shanghai EFE Biological Technology Co., Ltd.
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021-65675885 18964387627
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info@efebio.com
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[(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate(1469284-79-4)Related Product Information