PF-06424439|CAS 1469284-79-4|DC Chemicals

Cas No.:	1469284-78-3
Chemical Name:	(R)-(1-(2-(1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl)-3H-imidazo[4,5-b]pyridin-5-yl)piperidin-3-yl)(pyrrolidin-1-yl)methanone
Synonyms:	(R)-(1-(2-(1-(4-chloro-1H-pyrazol-1-yl)cyclopropyl)-3H-imidazo[4,5-b]pyridin-5-yl)piperidin-3-yl)(pyrrolidin-1-yl)methanone;BDBM215552;US9296745, 109-A;US9296745, 109-B;US9296745, 190;[(3R)-1-[2-[1-(4-chloropyrazol-1-yl)cyclopropyl]-1H-imidazo[4,5-b]pyridin-5-yl]piperidin-3-yl]-pyrrolidin-1-ylmethanone
SMILES:	ClC1C([H])=NN(C=1[H])C1(C2=NC3=C(C([H])=C([H])C(=N3)N3C([H])([H])C([H])([H])C([H])([H])[C@@]([H])(C(N4C([H])([H])C([H])([H])C([H])([H])C4([H])[H])=O)C3([H])[H])N2[H])C([H])([H])C1([H])[H]
Formula:	C₂₂H₂₆ClN₇O
M.Wt:	439.9411
Purity:	>98%
Sotrage:	Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Description:	PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM[1]. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate[2].
Target:	IC50: 14 nM (DGAT2)[1]
In Vivo:	PF-06424439 (p.o.; 60 mg/kg/day; for 3 days) reduces plasma triglyceride (TG) and cholesterol levels and decreases nonsignificant in circulating lipids in mice (Ldlr-/-)[1]. PF-06424439 (i.v.; 1 mg/kg) shows moderate clearance in rats following intravenous administration and moderate steady-state volume of distribution (Vdss) results in a short half-life[1]. Animal Model: Male low-density lipoprotein receptor (Ldlr) knockout mice (Ldlr-/-)[1] Dosage: 60 mg/kg Administration: P.o.; daily; for 3 days Result: Reduced plasma TG and cholesterol levels and decreased nonsignificant in circulating lipids. Animal Model: Male Wistar-Han rats[1] Dosage: 1 mg/kg Administration: I.v. Result: Showed moderate clearance and a short half-life with t1/2=1.39 h.
References:	[1]. Futatsugi K, et al. Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). J Med Chem. 2015 Sep 24;58(18):7173-85. [2]. Pabst B, et al. Mechanistic Characterization of Long Residence Time Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). Biochemistry. 2018 Dec 26;57(51):6997-7010.

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