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300657-03-8

300657-03-8 structure
300657-03-8 structure
  • Name: BMS-309403
  • Chemical Name: 2-[3-[2-(5-ethyl-3,4-diphenylpyrazol-1-yl)phenyl]phenoxy]acetic acid
  • CAS Number: 300657-03-8
  • Molecular Formula: C31H26N2O3
  • Molecular Weight: 474.550
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease FABP
  • Create Date: 2018-10-15 08:45:56
  • Modify Date: 2024-01-02 15:26:08
  • BMS-309403 is a potent, selective and cell-permeable inhibitor of fatty acid binding protein 4 (FABP4) with a Ki of less than 2 nM.
Name 2-[3-[2-(5-ethyl-3,4-diphenylpyrazol-1-yl)phenyl]phenoxy]acetic acid
Synonyms Acetic acid, 2-[[2'-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)[1,1'-biphenyl]-3-yl]oxy]-
{[2'-(5-Ethyl-3,4-diphenyl-1H-pyrazol-1-yl)-3-biphenylyl]oxy}acetic acid
2-[[2'-(5-Ethyl-3,4-diphenyl-1H-pyrazol-1-yl)[1,1'-biphenyl]-3-yl]oxy]acetic acid
UNII-M5X9XSU6J5
T4B
((2'-(5-Ethyl-3,4-Diphenyl-1h-Pyrazol-1-Yl)-3-Biphenylyl)oxy)acetic Acid
cc-561
[2'-(5-Ethyl-3,4-diphenyl-pyrazol-1-yl)-biphenyl-3-yloxy]acetic acid
BMS-309403
Description BMS-309403 is a potent, selective and cell-permeable inhibitor of fatty acid binding protein 4 (FABP4) with a Ki of less than 2 nM.
Related Catalog
Target

Ki: less than 2 nM (FABP4), 250 nM (FABP3), 350 nM (FABP5)[1]

In Vitro BMS-309403 binds to FABP4 with high affinity and shows over 100-fold selectivity against FABP5 as well as the heart isoform FABP3[1]. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. Treatment with BMS-309403 significantly decreased MCP-1 production from THP-1 macrophages in a dose- and time-dependent manner[2]. BMS-309403 stimulates glucose uptake in C2C12 myotubes in a temporal and dose dependent manner via activation of AMP-activated protein kinase (AMPK) signaling pathway but independent of FABPs[3].
In Vivo A 6 week treatment with BMS-309403 improves endothelial function, phosphorylated and total eNOS and reduced plasma triglyceride levels but does not affect endothelium-independent relaxations. In cultured human microvascular endothelial cells, lipid-induced A-FABP expression is associated with reduced phosphorylated eNOS and NO production and is reversed by BMS-309403[4]. The extent of atherosclerotic lesion area in the proximal aorta is significantly reduced in the BMS-309403-treated group compared with vehicle-treated controls in both the early and late intervention studies[2].
Animal Admin Mice: To determine the effects of pharmacological inhibition of the actions of A-FABP, either the A-FABP inhibitor BMS-309403 (15 mg/kg) or vehicle (4% Tween 80) are administered chronically by daily oral gavage for 6 weeks in ApoE−/− mice (starting at weeks 12 of age). Mice are anaesthetized with a bolus injection of pentobarbitone sodium (230 mg/kg) and their aorta removed and dissected for further analysis[4].
References

[1]. Sulsky R, et al. Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP). Bioorg Med Chem Lett. 2007 Jun 15;17(12):3511-5.

[2]. Furuhashi M, et al. Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2. Nature. 2007 Jun 21;447(7147):959-65.

[3]. Lin W, et al. BMS309403 stimulates glucose uptake in myotubes through activation of AMP-activated protein kinase. PLoS One. 2012;7(8):e44570.

[4]. Lee MY, et al. Chronic administration of BMS309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells. Br J Pharmacol. 2011 Apr;162(7):1564-76.

Density 1.2±0.1 g/cm3
Boiling Point 657.5±55.0 °C at 760 mmHg
Molecular Formula C31H26N2O3
Molecular Weight 474.550
Flash Point 351.4±31.5 °C
Exact Mass 474.194336
PSA 64.35000
LogP 7.69
Vapour Pressure 0.0±2.1 mmHg at 25°C
Index of Refraction 1.623
Hazard Codes Xi

Chemsrc provides CAS#:300657-03-8 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 300657-03-8 | Chemsrc address: https://m.chemsrc.com/en/baike/894842.html

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