Chemical Structure : Ki16425
CAS No.: 355025-24-0
Catalog No.: PC-43463Not For Human Use, Lab Use Only.
Ki16425 (Debio 0719) is a potent, subtype-selective, competitive antagonist of lysophosphatidic acid receptor LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, shows no activity at LPA4, LPA5, LPA6.
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Ki16425 (Debio 0719) is a potent, subtype-selective, competitive antagonist of lysophosphatidic acid receptor LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, shows no activity at LPA4, LPA5, LPA6.
Ki16425 inhibits the LPA-induced response in the decreasing order of LPA1>LPA3>LPA2, inhibits LPA-induced guanosine 5'-O-(3-thio)triphosphate binding as well as LPA receptor binding to membrane fractions in intact cells.
Ki16425 also inhibits LPA-induced long-term responses, including DNA synthesis and cell migration in A431 cells, selectively inhibits LPA receptor-mediated actions, especially through LPA1 and LPA3.
Ki16425 reduces both ethanol-induced sedation and ethanol reward in mice, prevents the effects of ethanol on basal c-Fos expression in the medial prefrontal cortex and on adult neurogenesis in the hippocampus.
M.Wt | 474.96 | |
Formula | C23H23ClN2O5S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
Propanoic acid, 3-[[[4-[4-[[[1-(2-chlorophenyl)ethoxy]carbonyl]amino]-3-methyl-5-isoxazolyl]phenyl]methyl]thio]- |
1. Ohta H, et al. Mol Pharmacol. 2003 Oct;64(4):994-1005.
2. Yamada T, et al. J Biol Chem. 2004 Feb 20;279(8):6595-605.
3. Zhao J, et al. Transl Res. 2015 Jul;166(1):80-8.
4. Sánchez-Marín L, et al. Neuropharmacology. 2018 May 1;133:189-201.
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