Products for Research Use Only

AM095 free acid

CAT: 0013-GTR19157501-01Size: 500 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19157501-01Size:500 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
AM095 (free acid) is a potent LPA1 receptor antagonist (IC50s: 0.98 and 0.73 μM for recombinant human or mouse LPA1) .In vitro, AM095 was a potent LPA receptor antagonist because it inhibited GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA with IC values of 0.98 and 0.73 μM, respectively, and exhibited no LPA agonism. In functional assays, AM095 inhibited LPA-driven chemotaxis of CHO cells overexpressing mouse LPA (IC = 778 nM) and human A2058 melanoma cells (IC = 233 nM) .In vivo, AM095: 1) had high oral bioavailability and a moderate half-life and was well tolerated at the doses tested in rats and dogs after oral and intravenous dosing, 2) dose-dependently reduced LPA-stimulated histamine release, 3) attenuated bleomycin-induced increases in collagen, protein, and inflammatory cell infiltration in bronchalveolar lavage fluid, and 4) decreased kidney fibrosis in a mouse unilateral ureteral obstruction model.
CAS Number
1228690-36-5
Purity
>98% (HPLC)
Solubility
DMSO:67.3 mg/mL (147.43 mM; Need ultrasonic and warming)
Smiles
O=C (CC1=CC=C (C=C1) C2=CC=C (C=C2) C3=C (C (C) =NO3) NC (O[C@H] (C) C4=CC=CC=C4) =O) O
Molecular Formula
C27H24N2O5
Molecular Weight
456.49
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.