BMS-986020 selectively inhibits the LPA receptor, which is involved in binding of the signaling molecule lysophosphatidic acid, which in turn is involved in a host of diverse biological functions like cell proliferation, platelet aggregation, smooth muscle contraction, chemotaxis, and tumor cell invasion, among others.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 50 mg/mL|
Lysophospholipid receptors in drug discovery.
Kihara Y, et al. Exp Cell Res. 2015 May 1;333(2):171-7. PMID: 25499971.
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|AM095 free acid
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AM966 is a potent, selective and orally active LPA(1) receptor antagonist which inhibits lung fibrosis in the mouse bleomycin model.
AM095 is a potent and selective, orally bioavailable antagonist of lysophosphatidic acid receptor1 (LPA1).
AKP-11 has potent immune modulatory activity for treatment of EAE/MS, but with relatively low adverse effects suggesting AKP-11 as a potential therapeutic drug for MS patients.
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