LY2955303

产品名称：

1433497-19-8
LY2955303
4-[5-[3,5-bis(1,1-Dimethylethyl)phenyl]-1-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-1H-pyrazol-3-yl]-benzoic acid
LY 2955303

产品介绍：

产品说明

生化/生理作用

LY2955303 is a potent and selective RARγ antagonist (Ki = 1.09 nM/RARγ, >1.70 μM/RARα, >2.98 μM/RARβ) that effectively inhibits RARγ-, but not RARα- or RARβ-, dependent reporter activity upon 15 nM all-trans retinoic acid stimulation in respective HEK293 transfectants (KB = 7.11 nM/RARγ, 1.51 μM/RARβ, 4.44 μM/RARα; 10 nM ATRA for RARβ transfectant). LY2955303 exhibits therapeutic efficacy in a rat model of osteoarthritis-like joint pain (ED50 = 0.72 mg/kg; single p.o. dosage 9 days post OA pain induction by MIA intra-articular injection) with good pharmacokinetic properties, aqueous solubility (>1.0 mg/mL in simulated intestinal fluid), oral availability (F = 26%; 10 mg/kg p.o. over 2 mg/kg i.v.), and no RARα antagonism-associated adverse effects (no testicular degeneration up to 10 mg/kg) seen with BMS-189453 treatment or in RARα-knockout mice.

基本信息

经验(实验)分子式	C₃₆H₄₂N₄O₃
分子量	578.74
MDL编号	MFCD31561443
NACRES	NA.77

产品性质

测定	≥98% (HPLC)
形式	powder
颜色	white to beige
溶解性	DMSO: 2 mg/mL, clear
储存温度	2-8℃
SMILES string	CC(C)(C)C1=CC(C2=CC(C3=CC=C(C(O)=O)C=C3)=NN2C4=CC=C(C=C4)C(N5CCN(CC5)C)=O)=CC(C(C)(C)C)=C1

安全信息

储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable