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> Ki16425 [355025-24-0]

Ki16425 [355025-24-0]

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Référence HY-13285-5mg

Conditionnement : 5mg

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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 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells.

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Ki16425 Chemical Structure

Ki16425 Chemical Structure

CAS No. : 355025-24-0

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Based on 8 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 can also inhibit 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ki16425 Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Masse moléculaire

474.96

Formule

C23H23ClN2O5S
CAS No.

355025-24-0
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvant et solubilité
In Vitro: 

DMSO : ≥ 100 mg/mL (210.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation

Purity: 98.11%

COA (255 KB)

Instruction de manipulation (2659 KB)
Références

  • [1]. Ohta H, et al. Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors.Mol Pharmacol, 2003, 64(4), 994-1005.  [Content Brief]

    [2]. Moughal NA, et al. Protean agonism of the lysophosphatidic acid receptor-1 with Ki16425 reduces nerve growth factor-induced neurite outgrowth in pheochromocytoma 12 cells. J Neurochem, 2006, 98(6), 1920-1929.  [Content Brief]

    [3]. Yu FX, et al. Regulation of the Hippo-YAP pathway by G-protein-coupled receptor signaling. Cell. 2012 Aug 17;150(4):780-91.  [Content Brief]

    [4]. Ma L, et al. Evidence for lysophosphatidic acid 1 receptor signaling in the early phase of neuropathic pain mechanisms in experiments using Ki-16425, a lysophosphatidic acid 1 receptor antagonist. J Neurochem, 2009, 109(2), 603-610.  [Content Brief]

  • [1]. Ohta H, et al. Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors.Mol Pharmacol, 2003, 64(4), 994-1005.

    [2]. Moughal NA, et al. Protean agonism of the lysophosphatidic acid receptor-1 with Ki16425 reduces nerve growth factor-induced neurite outgrowth in pheochromocytoma 12 cells. J Neurochem, 2006, 98(6), 1920-1929.

    [3]. Yu FX, et al. Regulation of the Hippo-YAP pathway by G-protein-coupled receptor signaling. Cell. 2012 Aug 17;150(4):780-91.

    [4]. Ma L, et al. Evidence for lysophosphatidic acid 1 receptor signaling in the early phase of neuropathic pain mechanisms in experiments using Ki-16425, a lysophosphatidic acid 1 receptor antagonist. J Neurochem, 2009, 109(2), 603-610.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1054 mL 10.5272 mL 21.0544 mL 52.6360 mL
5 mM 0.4211 mL 2.1054 mL 4.2109 mL 10.5272 mL
10 mM 0.2105 mL 1.0527 mL 2.1054 mL 5.2636 mL
15 mM 0.1404 mL 0.7018 mL 1.4036 mL 3.5091 mL
20 mM 0.1053 mL 0.5264 mL 1.0527 mL 2.6318 mL
25 mM 0.0842 mL 0.4211 mL 0.8422 mL 2.1054 mL
30 mM 0.0702 mL 0.3509 mL 0.7018 mL 1.7545 mL
40 mM 0.0526 mL 0.2632 mL 0.5264 mL 1.3159 mL
50 mM 0.0421 mL 0.2105 mL 0.4211 mL 1.0527 mL
60 mM 0.0351 mL 0.1755 mL 0.3509 mL 0.8773 mL
80 mM 0.0263 mL 0.1316 mL 0.2632 mL 0.6580 mL
100 mM 0.0211 mL 0.1053 mL 0.2105 mL 0.5264 mL
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Ki16425 Related Classifications

  • GPCR/G Protein
  • LPL Receptor
Help & FAQs

Keywords:

Ki16425355025-24-0Debio 0719Ki 16425Ki-16425Debio0719Debio-0719LPL ReceptorLysophospholipid ReceptorInhibitorinhibitorinhibit

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