Name: Ki16425
Brand: Selleck Chemicals
SKU: S1315
Availability: InStock
Rating: 5 (26 reviews)

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Quality Control

Batch: Purity: 99.03%

99.03

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other LPA Receptor Inhibitors	ONO-7300243 AM 095 Ki16198 BMS-986278 AM966 BMS-986020 ACT-1016-0707 Oleoyl-L-alpha-lysophosphatidic acid sodium salt

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 94 mg/mL (197.91 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 94 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	474.96	Formula	C₂₃H₂₃ClN₂O₅S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	355025-24-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Debio 0719			Smiles	CC1=NOC(=C1NC(=O)OC(C)C2=CC=CC=C2Cl)C3=CC=C(C=C3)CSCCC(=O)O

Mechanism of Action

Targets/IC₅₀/Ki	LPA1 (RH7777 cells) 0.34 μM(Ki) LPA3 (RH7777 cells) 0.93 μM(Ki) LPA2 (RH7777 cells) 6.5 μM(Ki)
In vitro	Kil6425 preferentially inhibits LPA1- and LPA3-mediated responses but has only a moderate effect on LPA2. This compound 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 it seems to be a useful tool for evaluating the involvement of specific LPA receptors in the short-term response to LPA. It inhibits long-term DNA synthesis and cell migration as induced by LPA in Swiss 3T3 fibroblasts. This chemical 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. It also significantly reduces the NGF-induced stimulation of p42/p44 MAPK and inhibited NGF-stimulated neurite outgrowth in PC-12 cells. It 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 this compound.
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 this compound is a short-lived inhibitor. This chemical 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/14500756/ [2] https://pubmed.ncbi.nlm.nih.gov/16945108/ [3] https://pubmed.ncbi.nlm.nih.gov/18802115/ [4] https://pubmed.ncbi.nlm.nih.gov/19222705/

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Ki16425 LPA Receptor antagonist

Chemical Structure

Molecular Weight: 474.96