Ki16425 (Synonyms: Debio 0719) |
| Catalog No.GC11374 |
Ki16425 is an antagonist of the lysophosphatidic acid receptors LPA1 and LPA3 and Ki values are 0.25 and 0.36μM respectly. Ki16425 reduces the LPA-induced activation of p42/p44 MAPK.Blocks LPA-induced dephosphorylation of Yes-associated protein (YAP) and WW domain-containing transcription regulator protein 1 (TAZ), inhibiting the Hippo signaling pathway.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 355025-24-0
Sample solution is provided at 25 µL, 10mM.
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Ki16425 is an antagonist of the lysophosphatidic acid receptors LPA1 and LPA3 and Ki values are 0.25 and 0.36μM respectly. Ki16425 reduces the LPA-induced activation of p42/p44 MAPK.Blocks LPA-induced dephosphorylation of Yes-associated protein (YAP) and WW domain-containing transcription regulator protein 1 (TAZ), inhibiting the Hippo signaling pathway [1].
Ki1642 (10μM; 24h) decreases lysophosphatidic acid (LPA)-induced HaCaT cell proliferation[2].LPA increased IL-17 mRNA expression in a dose-dependent manner, while the LPA inhibitor Ki16425 (10μM; 24h) suppressed this response[2]. Ki16425 (10μM; 120min) treatment suppressed LPA-induced ROCK2 and p38 MAPK expression[3].
Ki16425 (15mg/kg; ip; 7days) decreases the Epidermal Expression of ROCK2 and p-AKT in Imiquimod-Induced Psoriasis-like Mice)[2].Ki16425 (15mg/kg; ip; 4weeks ) treatment reduced serum IL-17 levels and IL-17 expression in exocrine glands in an adoptive transfer model[3].Ki16425 blocked the damage to the intestinal barrier of mice caused by Escherichia coli after LPA 1 signaling in the host[4].
References:
[1].Ohta H, Sato K, Murata N, Damirin A, Malchinkhuu E, Kon J, Kimura T, Tobo M, Yamazaki Y, Watanabe T, Yagi M, Sato M, Suzuki R, Murooka H, Sakai T, Nishitoba T, Im DS, Nochi H, Tamoto K, Tomura H, Okajima F. Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors. Mol Pharmacol. 2003 Oct;64(4):994-1005.
[2].Kim D, Kim HJ, Baek JO, Roh JY, Jun HS. Lysophosphatidic Acid Mediates Imiquimod-Induced Psoriasis-like Symptoms by Promoting Keratinocyte Proliferation through LPAR1/ROCK2/PI3K/AKT Signaling Pathway. Int J Mol Sci. 2021 Oct 5;22(19):10777.
[3].Park E, Kim D, Lee SM, Jun HS. Inhibition of lysophosphatidic acid receptor ameliorates Sjögren's syndrome in NOD mice. Oncotarget. 2017 Apr 18;8(16):27240-27251.
[4]. Zou D, Pei J, Lan J, Sang H, Chen H, Yuan H, Wu D, Zhang Y, Wang Y, Wang D, Zou Y, Chen D, Ren J, Gao X, Lin Z. A SNP of bacterial blc disturbs gut lysophospholipid homeostasis and induces inflammation through epithelial barrier disruption.
| Cell experiment [1]: | |
Cell lines | HaCaT cells |
Preparation Method | HaCaT cells were treated with or without 10μM LPA and ki16425 (10μM ) concentration for 24 h, and cell viability was examined by CCK8 assay. |
Reaction Conditions | Ki16425:10μM; 24h |
Applications | Ki16425 (10μM; 24h) decreases lysophosphatidic acid (LPA)-induced HaCaT cell proliferation. |
| Animal experiment [2]: | |
Animal models | Colon epithelial barrier disruption model |
Preparation Method | Ki16425 was injected into mice before E. coli BW25113 or blcE84 infection. Control groups received the same volume of DMSO. |
Dosage form | Ki16425:20mg/kg; ip; 24h |
Applications | Ki16425 blocked the damage to the intestinal barrier of mice caused by Escherichia coli after LPA 1 signaling in the host. |
References: | |
| Cas No. | 355025-24-0 | SDF | |
| Synonyms | Debio 0719 | ||
| Chemical Name | 3-[[4-[4-[1-(2-chlorophenyl)ethoxycarbonylamino]-3-methyl-1,2-oxazol-5-yl]phenyl]methylsulfanyl]propanoic acid | ||
| Canonical SMILES | CC1=NOC(=C1NC(=O)OC(C)C2=CC=CC=C2Cl)C3=CC=C(C=C3)CSCCC(=O)O | ||
| Formula | C23H23ClN2O5S | M.Wt | 474.96 |
| Solubility | ≥ 23.75mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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