Ki16425

SKU: orb1225218

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.

Key Properties

• CAS Number: 355025-24-0
• MW: 474.96
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₃ClN₂O₅S
• SMILES: O=C(O)CCSCC1=CC=C(C2=C(NC(OC(C3=CC=CC=C3Cl)C)=O)C(C)=NO2)C=C1
• Target: LPA Receptor
• Solubility: DMSO:95 mg/mL (200.01 mM); Ethanol:95 mg/mL (200.01 mM); Water:<1 mg/mL (<1 mM)

Bioactivity

• 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.
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• 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ki16425 | Ki-16425 | Ki 16425

Quick Database Links

Gene Symbol

LPA Receptor