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首页-小分子抑制剂&激动剂-GPCR-Protease-activated Receptor (PAR)-GB-88
GB-88

Chemical Structure : GB-88

CAS No.: 1416435-96-5

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GB-88 (GB 88;GB88)

货号: PC-60318Not For Human Use, Lab Use Only.

GB-88 is a selective, orally available PAR2 antagonist that inhibits PAR2 activated Ca(2+) release with IC50 of 2 uM.

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5 mg ￥3880 In stock
10 mg ￥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GB-88 is a selective, orally available PAR2 antagonist that inhibits PAR2 activated Ca(2+) release with IC50 of 2 uM.
GB-88 (10 mg/kg) inhibits acute colonic inflammation induced in rats by the PAR2 agonist SLIGRL-NH2 with markedly reduced edema, mucin depletion, PAR2 receptor internalization, and mastocytosis.

物理化学性质&存储条件

分子量 546.712
分子式 C32H42N4O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-((S)-3-cyclohexyl-1-(((2S,3S)-3-methyl-1-oxo-1-(spiro[indene-1,4'-piperidin]-1'-yl)pentan-2-yl)amino)-1-oxopropan-2-yl)isoxazole-5-carboxamide

参考文献

1. Suen JY, et al. Br J Pharmacol. 2012 Mar;165(5):1413-23.

2. Lohman RJ, et al. J Pharmacol Exp Ther. 2012 Feb;340(2):256-65.

3. Cheng RKY, et al. Nature. 2017 May 4;545(7652):112-115.

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