AM095|AM-095|LPA1 receptor antagonist

Cas No.:	1345614-59-6
Chemical Name:	sodium (R)-2-(4'-(3-methyl-4-(((1-phenylethoxy)carbonyl)amino)isoxazol-5-yl)-[1,1'-biphenyl]-4-yl)acetate
Synonyms:	AM095 AM-095; AM 095; AM095 sodium.
SMILES:	[Na+].O=C(CC1=CC=C(C2=CC=C(C3ON=C(C)C=3NC(O[C@@H](C3=CC=CC=C3)C)=O)C=C2)C=C1)[O-]
Formula:	C₂₇H₂₃N₂NaO₅
M.Wt:	478.47
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.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47220	Zectivimod	Zectivimod is a sphingosine-1-phosphate receptor agonist. Zectivimod can be used for the research of autoimmune diseases, chronic inflammatory diseases and immunoregulation disorders.
DC44942	H2L 5765834	H2L 5765834 is an antagonist of lysophosphatidic acid receptors LPA1, LPA3, and LPA5, with IC50s of 94, 752, and 463 nM respectively.
DC42560	1-Oleoyl lysophosphatidic acid	1-Oleoyl lysophosphatidic acid (1-Oleoyl-sn-glycero-3-phosphate) is an abundant LPA species with high biological activity due to its strong affinity for the LPA receptors. 1-Oleoyl lysophosphatidic acid is commonly used in most laboratories as a reagent for LPA receptor activation. 1-Oleoyl lysophosphatidic acid increases SRE-drivenβ-galactosidase activity.
DC28324	LPA2 antagonist 2	LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM, which is ＞480-fold more selective than LPA3 (IC50 of 13.85 μM).
DC28232	CYM50260	CYM50260 is a potent and exquisitely selective sphingosine-1-phosphate 4 receptor (S1P4-R) agonist with an EC50 of 45 nM. CYM50260 displays no activity against S1P1-R, S1P2-R, S1P3-R and S1P5-R.
DC10392	S1p receptor agonist 1	S1p receptor agonist 1 is an S1P receptor agonist extracted from patent WO 2015039587 A1, compound example 2.
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.
DC11561	SPM-242 racemate	A potent, selective S1P3 antagonist with Ki of 0.25 nM.
DC11560	SPM-242	A potent, selective S1P3 antagonist with Ki of 0.25 nM.
DC11605	ONO-0300302	A novel potent, slow tight binding LPA1 receptor antagonist with IC50 of 86 nM, Kd of 0.34 nM.