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Ki16425

Chemical Structure : Ki16425

CAS No.: 355025-24-0

Ki16425 (Debio 0719;Ki 16425)

Catalog No.: PC-43463Not For Human Use, Lab Use Only.

Ki16425 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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Biological Activity

Ki16425 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.

Physicochemical Properties

M.Wt 474.96
Formula C23H23ClN2O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Propanoic acid, 3-[[[4-[4-[[[1-(2-chlorophenyl)ethoxy]carbonyl]amino]-3-methyl-5-isoxazolyl]phenyl]methyl]thio]-

References

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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