Ki16425

SKU: orb1301066

Description

Ki16425 (Debio 0719) is a potent, reversible, and competitive antagonist of lysophosphatidic acid receptors LPA1, LPA2, and LPA3. It is widely used in both in vitro and in vivo research to investigate LPA signaling pathways in fields such as fibrosis, cancer, and neuropathic pain.

Research Area

Pharmacology & Drug Discovery, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 355025-24-0
• MW: 474.96
• Purity: 96.15% (May vary between batches)
• Formula: C₂₃H₂₃ClN₂O₅S
• SMILES: CC(OC(=O)Nc1c(C)noc1-c1ccc(CSCCC(O)=O)cc1)c1ccccc1Cl
• Target: YAP,LPL Receptor,LPA Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.95 mM);DMSO:94 mg/mL (197.91 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:84 mg/mL (176.86 mM)

Bioactivity

• Target IC50:
  LPA3:0.93 μM(Ki)|LPA2:6.5 μM(Ki)|LPA1:0.34 μM(Ki)
• In Vivo:
  Ki-16425 (30 mg/kg, i.p.) completely blocks LPA-induced neuropathic pain-like behaviors, when administered 30 min but not 90 min before lysophosphatidic acid injection, suggesting that Ki-16425 is a short-lived inhibitor. Ki-16425 also inhibits nerve injury-induced up-regulation of Caα2δ-1 in the dorsal root ganglion and reduction of SP immunoreactivity in the spinal dorsal horn.
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• In Vitro:
  Kil6425 preferentially inhibits LPA1- and LPA3-mediated responses but has only a moderate effect on LPA2. Ki16425 inhibits the LPA-induced Ca(2+) response in THP-1 cells, 3T3 fibroblasts, and A431 cells, but had only a marginal effect in PC-12 cells and HL-60 cells, which means that Ki16425 seems to be a useful tool for evaluating the involvement of specific LPA receptors in the short-term response to LPA. Ki16425 inhibits long-term DNA synthesis and cell migration as induced by LPA in Swiss 3T3 fibroblasts. Ki16425 reduces the LPA-induced activation of p42/p44 mitogen activated protein kinase (MAPK), while acting as a weak stimulator of p42/p44 MAPK on its own, properties typical of a protean agonist. Ki16425 also significantly reduces the NGF-induced stimulation of p42/p44 MAPK and inhibited NGF-stimulated neurite outgrowth in PC-12 cells. Ki16425 markedly inhibits the expressions of COX-2 protein induced by synovial fluids. The enhancement of the IL-1 action by LPA on COX-2 expression is also inhibited by Ki16425.
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Storage & Handling

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

Alternative Names

LPA Receptor, LPA2, LPA1, LPAReceptor, LPA3, LPL, LPL Receptor, LPLReceptor, Lysophospholipid Receptor, inhibit, Ki16425, Ki-16425, Ki 16425, Inhibitor, Debio0719, Debio-0719, Debio 0719

Compound Identifiers

PubChem CID

10367662