AM095|AM-095|LPA1 receptor antagonist

Cas No.:	1345614-59-6
Chemical Name:	Am095
Synonyms:	Am095;sodium,2-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]acetate;AM-095;1,1′-Biphenyl]-4-acetic acid, 4′-[3-methyl-4-[[[(1R)-1-phenylethoxy]carbonyl]amino]-5-isoxazolyl]-, sodium salt (1:1);AMI-000533;Sodium {4′-[3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-biphenyl-4-yl}-acetate;GLXC-10016;CS-1118;AM095 sodium;DTXSID70693387;AS-55886;SODIUM 2-{4'-[3-METHYL-4-({[(1R)-1-PHENYLETHOXY]CARBONYL}AMINO)-1,2-OXAZOL-5-YL]-[1,1'-BIPHENYL]-4-YL}ACETATE;BCP16047;HY-16039;AM095, >=98% (HPLC);Sodium {4'-[3-methyl-4-({[(1R)-1-phenylethoxy]carbonyl}amino)-1,2-oxazol-5-yl][1,1'-biphenyl]-4-yl}acetate;AKOS030526424;sodium;2-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]acetate;AC-35293;AM095;1345614-59-6;EX-A1954;Sodium {4'-[3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-biphenyl-4-yl}-acetate;AM-095 Sodium;Sodium (R)-2-(4'-(3-methyl-4-(((1-phenylethoxy)carbonyl)amino)isoxazol-5-yl)-[1,1'-biphenyl]-4-yl)acetate;AM 095
SMILES:	O=C([O-])CC1=CC=C(C2=CC=C(C3=C(NC(O[C@@H](C4=CC=CC=C4)C)=O)C(C)=NO3)C=C2)C=C1.[Na+]
Formula:	C₂₇H₂₃N₂NaO₅
M.Wt:	478.471698045731
Purity:	98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively. AM095 is an LPA1 receptor antagonist with good oral exposure and antifibrotic activity in rodent models. In vitro, AM095 inhibited GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA1 with IC50 values of 0.98 and 0.73 μM, respectively, and exhibited no LPA1 agonism. In functional assays, AM095 inhibited LPA-driven chemotaxis of CHO cells overexpressing mouse LPA? (IC50= 778 nM) and human A2058 melanoma cells (IC50 = 233 nM). Another study showed that LPA/LPA1 pathway inhibition has the potential to be an effective new therapeutic strategy for systemic sclerosis (SSc), and that LPA1 is an attractive pharmacologic target in dermal fibrosis.

Cat. No.	Product name	Field of application
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DC10561	GSK-2018682	GSK-2018682 is a sphingosine 1 phosphate receptor (S1PR)-1 agonist potentially for the treatment of multiple sclerosis.
DC10923	TAK-615	TAK-615 (TAK615) is a potent, selective, negative allosteric modulator (NAM) of the LPA1 receptor, partially inhibits the LPA response with IC50 of 91 nM (60% at 10 uM) in calcium mobilisation assays..
DC10925	SAR-100842	SAR-100842 (SAR100842) is a potent, selective, orally available antagonist of the Lysophosphatidic Acid 1 Receptor (LPA1 receptor) with IC50 of 31 nM in β-arrestin assays.
DC10924	BMS986202	BMS-986202 is a clinical Tyk2 inhibitor that binds to Tyk2 JH2 with IC50 of 0.19 nM and shows remarkably selectivity over other kinases including Jak family members.
DC8622	AM095 free acid	AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.
DC8621	AM095	AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.