Ki16425

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ki16425 是 LPA1、LPA2 和 LPA3 的竞争性、有效和可逆拮抗剂，Ki 分别为 0.34 μM、6.5 μM 和 0.93 μM。

Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, respectively, shows no activity at LPA4, LPA5, LPA6.

Ki16425 (10 μM; 1.5 hours; HEK293A cells) treatment blocks LPA-induced dephosphorylation of YAP/TAZ in HEK293A cells. Ki16425 partially inhibits the ability of serum to repress YAP/TAZ phosphorylation, particularly at low serum concentrations (0.2%). Western Blot Analysis Cell Line:HEK293A cells Concentration:10 μM Incubation Time:1.5 hours Result:Blocked LPA-induced dephosphorylation of YAP/TAZ. Partially inhibited the ability of serum to repress YAP/TAZ phosphorylation.

Ki16425 (Debio 0719) (1-30 mg/kg; i.p.; at 30 min prior to LPA injection) inhibits LPA-induced neuropathic pain-like behaviors. Animal Model:20-24 g male standard ddY-strain mice Dosage:1-30 mg/kg Administration:Intraperitoneal injection; at 30 minutes prior to LPA injection Result:LPA-induced neuropathic pain behaviors were attenuated in a dose-dependent manner.

Ki16425 | Ki-16425 | Ki 16425

GPCR/G Protein

LPA Receptor

LPA1| LPA2| LPA3

Cancer

——

355025-24-0

474.96

C23H23ClN2O5S

>98% (HPLC)

DMSO:95 mg/mL (200.01 mM); Ethanol:95 mg/mL (200.01 mM); Water:<1 mg/mL (<1 mM)

O=C(O)CCSCC1=CC=C(C2=C(NC(OC(C3=CC=CC=C3Cl)C)=O)C(C)=NO2)C=C1

3-((4-(4-(((1-(2-chlorophenyl)ethoxy)carbonyl)amino)-3-methylisoxazol-5-yl)benzyl)thio)propanoic acid

(-20℃)

With Ice Pack

≥ 2 years