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BMS-687453 98%

BMS-687453

源葉(MedMol)
S81598
1000998-59-3
C22H21ClN2O6
444.8649
品牌 貨號 產品規格 價格(RMB) 庫存(上海) 北京 武漢 南京 購買數量
源葉(MedMol) S81598-5mg 98% ¥200.00元 8 - - -
源葉(MedMol) S81598-10mg 98% ¥320.00元 預計交期:2-3天 - - -
源葉(MedMol) S81598-25mg 98% ¥440.00元 10 - - -
源葉(MedMol) S81598-50mg 98% ¥780.00元 預計交期:2-3天 - - -
源葉(MedMol) S81598-100mg 98% ¥1300.00元 7 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.
產品描述: BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.
靶點: PPARα:260 nM (IC50, Human PPARα);PPAR
體外研究:
BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and ~410-fold and more than 57-fold selectivity vs human PPARγ of 4100 nM and >15000 nM in PPAR-GAL4 transactivation assays. BMS-687453 exhibits high PPARα potency (EC50 = 47 nM) with ~50-fold selectivity vs PPARγ (EC50 = 2400 nM) in HepG2 cells. However, BMS-687453 shows less potent activities in rodent PPARα functional assays, with a moderate EC50 of 426 nM for mouse and 488 nM for hamster but remains a full PPARα agonist in both species
體內研究:
BMS-687453 (10, 50, 100, p.o.) dose-dependently increases serum ApoA1 protein levels and low-density lipoprotein-cholesterol (LDLc) levels in mice. BMS-687453 (1, 3, 10 mg/kg, p.o.) decreases HDLc levels in high fat-fed hamsters. BMS-687453 induces PDK4 mRNA in the liver, with ED50 value of 0.24 mg/kg. BMS-687453 (300 mg/kg, p.o.) causes skeletal myofiber degeneration and necrosis characterized by observed discoid changes, myofibril lysis, hyalinization, and cellular infiltration in male rats. BMS-687453 (300 mg/kg, p.o.) induces a mild toxicity in both fast and slow-twitch muscles in male rats
參考文獻:
1. Li J, et al. Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453). J Med Chem. 2010 Apr 8;53 2. Mukherjee R, et al. Novel peroxisome proliferator-activated receptor alpha agonists lower low-density lipoprotein and triglycerides, raise high-density lipoprotein, and synergistically increase cholesterol excretion with a liver X receptor agonist. J Pharmacol Exp Ther. 2008 Dec;327(3):716-26. 3. Vassallo JD, et al. Biomarkers of drug-induced skeletal muscle injury in the rat: troponin I and myoglobin. Toxicol Sci. 2009 Oct;111(2):402-12.
溶解性: soluble  in  DMSO
保存條件: -20℃
配置溶液濃度參考:
1mg 5mg 10mg
1 mM 2.248 ml 11.239 ml 22.479 ml
5 mM 0.45 ml 2.248 ml 4.496 ml
10 mM 0.225 ml 1.124 ml 2.248 ml
50 mM 0.045 ml 0.225 ml 0.45 ml
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參考文獻

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