An LPA1 receptor antagonist (IC50s = 25 and 23 nM in CHO cells expressing human or mouse receptors

AM095 – 10 mg

Brand:
Cayman
CAS:
1228690-36-5
Storage:
-20
UN-No:
Non-Hazardous - /

AM095 is an orally bioavailable antagonist of lysophosphatidic acid receptor 1 (LPA1) with IC50 values of 25 and 23 nM in CHO cells expressing human or mouse receptors, respectively.{41865} It is selective for LPA1 over LPA2, LPA3, LPA4, and LPA5 (IC50s = >10,000 nM for human LPA2-5). It inhibits chemotaxis of CHO cells overexpressing LPA1 and of A2058 human melanoma cells (IC50s = 778 and 233 nM, respectively) and prevents LPA-induced increases in plasma histamine levels in mice (ED50 = 8.3 mg/kg).{41866} It also decreases collagen and protein levels in bronchoalveolar lavage fluid (BALF) in a mouse model of bleomycin-induced lung injury (ED50s = ~10 mg/kg for both) and decreases kidney fibrosis in a mouse model of unilateral ureteral obstruction when administered at a dose of 30 mg/kg for eight days.  

 

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Description

An LPA1 receptor antagonist (IC50s = 25 and 23 nM in CHO cells expressing human or mouse receptors, respectively); selective for LPA1 over LPA2, LPA3, LPA4, and LPA5 (IC50s = >10,000 nM for human LPA2-5); inhibits chemotaxis of CHO cells overexpressing LPA1 and of A2058 human melanoma cells (IC50s = 778 and 233 nM, respectively); prevents LPA-induced increases in plasma histamine levels in mice (ED50 = 8.3 mg/kg); decreases kidney fibrosis in a mouse model of unilateral ureteral obstruction at 30 mg/kg for eight days

Formal name: 4′-[3-methyl-4-[[[(1R)-1-phenylethoxy]carbonyl]amino]-5-isoxazolyl]-[1,1′-biphenyl]-4-acetic acid

Synonyms: 

Molecular weight: 456.5

CAS: 1228690-36-5

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation

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