Ki16425( Ki16425 | Ki-16425 | Ki 16425 )

Catalog No. M14214 CAS No. 355025-24-0

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

Ki16425
Note

Research use only, not for human use.
Brief Description

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.
Description

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.
In Vitro

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.
In Vivo

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.
Synonyms

Ki16425 | Ki-16425 | Ki 16425
Pathway

GPCR/G Protein
Target

LPA Receptor
Recptor

LPA1| LPA2| LPA3
Research Area

Cancer
Indication

——

CAS Number

355025-24-0
Formula Weight

474.96
Molecular Formula

C23H23ClN2O5S
Purity

>98% (HPLC)
Solubility

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

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

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

1.Ohta H, et al, Mol Pharmacol, 2003, 64(4), 994-1005.

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