1. GPCR/G Protein
  2. LPL Receptor
  3. Ki16425

Ki16425 (Synonyms: Debio 0719)

Cat. No.: HY-13285 Purity: 98.67%
Handling Instructions

Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK. Ki16425 also can inhibits LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells.

For research use only. We do not sell to patients.

Ki16425 Chemical Structure

Ki16425 Chemical Structure

CAS No. : 355025-24-0

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
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50 mg USD 432 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK[1][2]. Ki16425 also can inhibits LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells[3].

IC50 & Target

Ki: 0.34 μM (LPA1), 0.93 μM (LPA3), 6.5 μM (LPA2)[1]

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%)[3].

Western Blot Analysis[3]

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.
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[4].

Animal Model: 20-24 g male standard ddY-strain mice[4]
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.
Molecular Weight

474.96

Formula

C₂₃H₂₃ClN₂O₅S

CAS No.

355025-24-0

SMILES

ClC1=C(C=CC=C1)C(C)OC(NC2=C(ON=C2C)C3=CC=C(C=C3)CSCCC(O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (210.54 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Ki16425Debio 0719Ki 16425Ki-16425Debio0719Debio-0719LPL ReceptorLysophospholipid ReceptorInhibitorinhibitorinhibit

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Product name:
Ki16425
Cat. No.:
HY-13285
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