Merck

PZ0362

Sigma-Aldrich

CP-640186 hydrochloride

≥95% (HPLC)

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別名:
(3R)-Anthracen-9-yl-[3-(morpholine-4-carbonyl)-[1,4′]bipiperidinyl-1′-yl]-methanone hydrochloride, CP 640186 hydrochloride, CP640186 hydrochloride, [(3R)-1′-(9-Anthracenylcarbonyl)[1,4′-bipiperidin]-3-yl]-4-morpholinyl-methanone hydrochloride
Empirical Formula (Hill Notation):
C30H35N3O3 · HCl
CAS番号:
分子量:
522.08
MDL番号:
NACRES:
NA.77

品質水準

アッセイ

≥95% (HPLC)

形状

powder

manufacturer/tradename

Pfizer®

保管条件

desiccated

white to beige

溶解性

H2O: 2 mg/mL, clear (warmed)

オーガナイザー

Pfizer

保管温度

room temp

SMILES string

O=C(C1=C2C=CC=CC2=CC3=CC=CC=C31)N(CC4)CCC4N5C[C@H](C(N6CCOCC6)=O)CCC5.[H]Cl

InChI

1S/C30H35N3O3.ClH/c34-29(32-16-18-36-19-17-32)24-8-5-13-33(21-24)25-11-14-31(15-12-25)30(35)28-26-9-3-1-6-22(26)20-23-7-2-4-10-27(23)28;/h1-4,6-7,9-10,20,24-25H,5,8,11-19,21H2;1H/t24-;/m1./s1

InChI key

DUBNXJIOBFRASV-GJFSDDNBSA-N

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当該品目
PZ0354PZ0374PZ0386
CP-640186 hydrochloride ≥95% (HPLC)

Sigma-Aldrich

PZ0362

CP-640186 hydrochloride

PF-04363467 hydrochloride ≥98% (HPLC)

Sigma-Aldrich

PZ0354

PF-04363467 hydrochloride

PF-06446846 hydrochloride ≥98% (HPLC)

Sigma-Aldrich

PZ0374

PF-06446846 hydrochloride

form

powder

form

powder

form

powder

form

powder

manufacturer/tradename

Pfizer®

manufacturer/tradename

Pfizer®

manufacturer/tradename

Pfizer®

manufacturer/tradename

Pfizer®

storage condition

desiccated

storage condition

-

storage condition

desiccated

storage condition

desiccated

color

white to beige

color

white to beige

color

white to beige

color

white to beige

solubility

H2O: 2 mg/mL, clear (warmed)

solubility

H2O: 3 mg/mL, clear (warmed)

solubility

H2O: 2 mg/mL, clear

solubility

H2O: 2 mg/mL, clear

アプリケーション

CP-640186 hydrochloride has been used as an allosteric acetyl-CoA carboxylase (ACC) inhibitor (ACCi) for pharmacological inhibition of lipogenesis to determine if fatty acid synthesis is essential for brown adipose tissue (BAT) whitening. It has also been used as an inhibitor of mammalian acetyl-CoA carboxylase (mACC1/2) to study its effect on meropenem potency against the persisters from multiple pathogens, including B. thailandensis, P. aeruginosa, S.Typhimurium, and attenuated Y. pestis.

生物化学的/生理学的作用

CP-640186 is a potent and orally active acetyl-CoA carboxylase 1/2 (ACC-alpha/beta, ACC1/2) inhibitor (IC50 ~50 nM) that targets the carboxyltransferase (CT) domain at the ACC dimer interface (via tight interactions with the putative biotin-binding site) in a reversible manner, uncompetitive with respect to ATP, and non-competitive with respect to bicarbonate, acetyl-CoA, and citrate. CP-610431 inhibits fatty acid (FA) synthesis, triglyceride (TG) synthesis, TG and apoB secretion (IC50 = 1.6, 1.8, 3.0, and 5.7 μM, respectively), but not cholesterol synthesis or apoC3 secretion in HepG2 cells (ACC1), as well as stimulates FA oxidation in C2C12 cells (ACC2) and in rat epitrochlearis muscle strips (EC50 = 57 nM and 1.3 μM, respectively). Oral administration is shown to inhibit FA synthesis in rats, CD1 mice, and ob/ob mice (ED50 = 13, 11, and 4 mg/kg, respectively) and stimulate rat whole body FA oxidation (ED50 ∼30 mg/kg) in vivo.

法的情報

Sold for research purposes under agreement from Pfizer Inc.
Pfizer is a registered trademark of Pfizer, Inc.

保管分類コード

11 - Combustible Solids

WGK

WGK 3


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Yasunori Nio et al.
Antiviral research, 132, 262-267 (2016-07-10)
Recently, direct antiviral agents against hepatitis C virus (HCV) infection have been developed as highly effective anti-HCV drugs. However, the appearance of resistant viruses against direct anti-viral agents is an unsolved problem. One of the strategies considered to suppress the
Daniel Hess et al.
PloS one, 5(6), e11394-e11394 (2010-07-09)
Lung cancer is the most frequent form of cancer. The survival rate for patients with metastatic lung cancer is approximately 5%, hence alternative therapeutic strategies to treat this disease are critically needed. Recent studies suggest that lipid biosynthetic pathways, particularly
Hailong Zhang et al.
Structure (London, England : 1993), 12(9), 1683-1691 (2004-09-03)
Acetyl-coenzyme A carboxylases (ACCs) are important targets for the development of therapeutic agents against obesity, diabetes, and other diseases. CP-640186 is a potent inhibitor of mammalian ACCs and can reduce body weight and improve insulin sensitivity in test animals. It
Deepa S Valsangkar et al.
Molecular reproduction and development, 82(9), 679-693 (2015-06-05)
In mouse oocytes, meiotic induction by pharmacological activation of PRKA (adenosine monophosphate-activated protein kinase; formerly known as AMPK) or by hormones depends on stimulation of fatty acid oxidation (FAO). PRKA stimulates FAO by phosphorylating and inactivating acetyl CoA carboxylase (ACAC;
P B Patil et al.
Archives of physiology and biochemistry, 113(1), 13-24 (2007-05-25)
There seems to be an association between increased concentrations of malonyl coenzyme A (malonyl CoA) in skeletal muscle and diabetes and/or insulin resistance. The purpose of the current study was to test the hypothesis that treatments designed to manipulate malonyl

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