Home GPCR & G Protein LPA Receptor antagonist Ki16425 For research use only.

Ki16425

Synonyms: Debio 0719

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 in RH7777 cell lines, respectively, shows no activity at LPA4, LPA5, LPA6.

Ki16425 Chemical Structure

Ki16425 Chemical Structure

CAS No. 355025-24-0

Purity & Quality Control

Ki16425 Related Products

Signaling Pathway

LPA Receptor Signaling Pathways

LPA Receptor Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
chem1 cells Function assay Antagonist activity at LPA1 expressed in human chem1 cells assessed as effect on intracellular calcium mobilization by FLIPR assay, IC50=0.046μM 20056548
RH7777 Function assay Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells, Ki=0.148μM 16033271
stellate cells Function assay Antagonist activity at LPA1 receptor in rat hepatic stellate cells assessed as inhibition of lysophosphatidic acid-induced intracellular calcium influx, IC50=0.16μM 17467986
RH7777 Function assay Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptor, IC50=0.301μM 16033271
RH7777 Function assay Binding affinity for Lysophosphatidic acid receptor 1 expressed in RH7777 rat hepatoma cells, Ki=0.425μM 16033271
CHOK1 Function assay Antagonist activity at human recombinant LPA1 receptor expressed in CHOK1 cells assessed as inhibition of lysophosphatidic acid-induced intracellular calcium influx, IC50=0.51μM 17467986
RH7777 Function assay Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA1 receptor, IC50=0.762μM 16033271
PC-3 Function assay Binding affinity for Lysophosphatidic acid receptor in PC-3 cells, Ki=1.74μM 16033271
PC-3 Function assay Inhibition of LPA-induced calcium transients in PC-3 cells, IC50=3.384μM 16033271
HEK293 Function assay 60 mins Antagonist activity at human LPA2 receptor expressed in HEK293 cells assessed as inhibition of LPA-induced AP-TGF-alpha release treated 5 mins before LPA addition measured after 60 mins 22658556
HEK293 Function assay 60 mins Antagonist activity at human LPA1 receptor expressed in HEK293 cells assessed as inhibition of LPA-induced AP-TGF-alpha release treated 5 mins before LPA addition measured after 60 mins 22658556
PC3 Function assay Antagonist activity at LPA receptor in human PC3 cells assessed as inhibition of LPA-induced cell migration 22658556
CHO Function assay Competitive antagonist activity at human LPA1 receptor overexpressed in CHO cells assessed as inhibition of LPA-induced [35S]GTPgammaS binding by liquid scintillation counting 22180836
CHO Function assay Competitive antagonist activity at N-terminal 3XHA-tagged human LPA3 receptor overexpressed in CHO cells assessed as inhibition of LPA-induced [35S]GTPgammaS binding by liquid scintillation counting 22180836
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Biological Activity

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 in RH7777 cell lines, respectively, shows no activity at LPA4, LPA5, LPA6.
Targets
LPA1 [1]
(RH7777 cells)		 LPA3 [1]
(RH7777 cells)		 LPA2 [1]
(RH7777 cells)
0.34 μM(Ki) 0.93 μM(Ki) 6.5 μM(Ki)
In vitro
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. [1] 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. [2] 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. [3]
In Vivo
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. [4]
Animal Research Animal Models Male standard ddY-strain mice are used.
Dosages 30 mg/kg.
Administration Administered via i.p.

Chemical Information & Solubility

Molecular Weight 474.96 Formula

C23H23ClN2O5S
CAS No. 355025-24-0 SDF Download Ki16425 SDF
Smiles CC1=NOC(=C1NC(=O)OC(C)C2=CC=CC=C2Cl)C3=CC=C(C=C3)CSCCC(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 94 mg/mL ( (197.91 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 94 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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