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首页-小分子抑制剂&激动剂-GPCR-Lysophospholipid Receptor-AM095
AM095

Chemical Structure : AM095

CAS No.: 1345614-59-6

AM095 (AM-095)

货号: PC-49650Not For Human Use, Lab Use Only.

AM095 (AM-095) is a potent, selective and orally active lysophosphatidic acid type 1 receptor (LPA1) antagonist with IC50 of 0.98 and 0.73 uM for hLPA1 and mLPA1 in GTP S binding assays, respectively, with no LPA1 agonism.

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5 mg ¥1280 In stock
10 mg ¥1980 In stock
25 mg ¥3280 In stock
50 mg ¥5280 In stock
100 mg Get quote

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AM095 (AM-095) is a potent, selective and orally active lysophosphatidic acid type 1 receptor (LPA1) antagonist with IC50 of 0.98 and 0.73 uM for hLPA1 and mLPA1 in GTP S binding assays, respectively, with no LPA1 agonism.
AM095 inhibited LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 (IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM) in function assays.
AM095 inhibited LPA1-driven chemotaxis of both human A2058 melanoma cells (IC50 =0.23 uM) and mouse LPA1/CHO cells (IC50=0.78 uM)。
AM095 dose-dependently reduced LPA-stimulated histamine release, attenuated bleomycin-induced increases in collagen, protein, and inflammatory cell infiltration in bronchalveolar lavage fluid in vivo.
AM095 decreased kidney fibrosis in a mouse unilateral ureteral obstruction model.

物理化学性质&存储条件

分子量 478.48
分子式 C27H23N2NaO5
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

sodium, {4'-[3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-biphenyl-4-yl}-acetate

参考文献

1. Swaney JS, et al. J Pharmacol Exp Ther. 2011 Mar;336(3):693-700.

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