Ki16425 (Debio 0719)

Alias: Ki16425; Debio0719; Ki-16425; Debio 0719; Ki 16425; Debio-0719
Cat No.:V1496 Purity: ≥98%
Ki16425 (also called Ki 16425; Debio-0719; Ki-16425; Debio 0719) is a competitive, selective and reversible antagonist of LPA which inhibits LPA1, LPA2 and LPA3 with Ki values of 0.34 μM, 6.5 μM and 0.93 μM in RH7777 cell lines, respectively.
Ki16425 (Debio 0719) Chemical Structure CAS No.: 355025-24-0
Product category: LPA Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Ki16425 (also called Ki 16425; Debio-0719; Ki-16425; Debio 0719) is a competitive, selective and reversible antagonist of LPA which inhibits LPA1, LPA2 and LPA3 with Ki values of 0.34 μM, 6.5 μM and 0.93 μM in RH7777 cell lines, respectively. Ki16425 inhibits neurite outgrowth induced by nerve growth factor in pheochromocytoma 12 cells. ki16425 reduces inflammation in the abdomen and throughout the body in a mouse model of peritoneal sepsis.

Biological Activity I Assay Protocols (From Reference)
Targets
LPA1 ( Ki = 0.34 μM ); LPA3 ( Ki = 0.93 μM ); LPA2 ( Ki = 6.5 μM )
ln Vitro

In vitro activity: Kil6425 has a modest impact on LPA2, but preferentially inhibits LPA1- and LPA3-mediated responses. Ki16425 has a negligible effect on PC-12 and HL-60 cells, but it significantly inhibits the LPA-induced Ca(2+) response in THP-1, 3T3 fibroblasts, and A431 cells. These findings suggest that Ki16425 may be a valuable tool for assessing the role of particular LPA receptors in the short-term response to LPA. In Swiss 3T3 fibroblasts, Ki16425 prevents long-term DNA synthesis and cell migration that are brought on by LPA.[1] As a protean agonist, ki16425 acts as a weak stimulator of p42/p44 MAPK on its own, while also reducing the LPA-induced activation of p42/p44 mitogen activated protein kinase (MAPK). Additionally, Ki16425 dramatically inhibits PC-12 cell NGF-stimulated neurite outgrowth and significantly lowers NGF-induced stimulation of p42/p44 MAPK.[2] Ki16425 significantly reduces the expression of COX-2 protein that synovial fluids induce. Additionally, Ki16425 suppresses the enhancement of IL-1 action by LPA on COX-2 expression.[3]

ln Vivo
Ki-16425 (30 mg/kg, i.p.) entirely prevents LPA-induced neuropathic pain-like behaviors when given 30 minutes in advance of a lysophosphatidic acid injection, but not 90 minutes beforehand, indicating that Ki-16425 is a transient inhibitor. Additionally, Ki-16425 prevents the dorsal root ganglion's up-regulation of Caα2δ-1 caused by nerve damage as well as the spinal dorsal horn's decrease in SP immunoreactivity.[4]
Enzyme Assay
The inositol phosphates (sum of inositol bisphosphate and inositol trisphosphate) were measured after 1 minute of incubation of RH7777 cells with or without Ki16425. The radioactivity of the trichloroacetic acid(5%)-insoluble fraction was taken into consideration as the total radioactivity, and the results were normalized to 105 dpm of the total radioactivity incorporated into the cellular inositol lipids.
Cell Assay
Ki16425 suppressed the expression of heparin-binding EGF-like growth factor (HB-EGF) in human breast and prostate cancer cells.
Animal Protocol
Dissolved in sesame oil; 30 mg/kg; i.p. administration.
Male standard ddY-strain mice
References

[1]. Mol Pharmacol . 2003 Oct;64(4):994-1005.

[2]. J Neurochem . 2006 Sep;98(6):1920-9.

[3]. J Immunol . 2008 Oct 1;181(7):5111-9.

[4]. J Neurochem . 2009 Apr;109(2):603-10.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H23CLN2O5S
Molecular Weight
474.96
Exact Mass
474.1
Elemental Analysis
C, 58.16; H, 4.88; Cl, 7.46; N, 5.90; O, 16.84; S, 6.75
CAS #
355025-24-0
Appearance
Solid powder
SMILES
CC1=NOC(=C1NC(=O)OC(C)C2=CC=CC=C2Cl)C3=CC=C(C=C3)CSCCC(=O)O
InChi Key
LLIFMNUXGDHTRO-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H23ClN2O5S/c1-14-21(25-23(29)30-15(2)18-5-3-4-6-19(18)24)22(31-26-14)17-9-7-16(8-10-17)13-32-12-11-20(27)28/h3-10,15H,11-13H2,1-2H3,(H,25,29)(H,27,28)
Chemical Name
3-[[4-[4-[1-(2-chlorophenyl)ethoxycarbonylamino]-3-methyl-1,2-oxazol-5-yl]phenyl]methylsulfanyl]propanoic acid
Synonyms
Ki16425; Debio0719; Ki-16425; Debio 0719; Ki 16425; Debio-0719
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~94 mg/mL (~197.9 mM)
Water: <1 mg/mL
Ethanol: ~94 mg/mL (~197.9 mM)
Solubility (In Vivo)
5%DMSO+95%Corn oil: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1054 mL 10.5272 mL 21.0544 mL
5 mM 0.4211 mL 2.1054 mL 4.2109 mL
10 mM 0.2105 mL 1.0527 mL 2.1054 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • Inhibitory effect of antagonist (Ki16425) for LPA receptor on the LPA- and synovial fluid-induced COX-2 expression in RA synovial cells. J Immunol . 2008 Oct 1;181(7):5111-9.
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