H2L5186303
Based on 3 publication(s) in Google Scholar
H2L5186303 is a potent and selective LPA2 receptor antagonist with an IC50 of 9 nM. H2L5186303 promotes Apoptosis. H2L5186303 inhibits cell proliferation and motility. H2L5186303 has anti-inflammatory effects.
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- Pureza: 98.50%
- No. CAS: 139262-76-3
- Fòrmula: C26H20N2O8
- Peso molecular:488.45
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) H2L5186303
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Actividad biológica
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LPA2 Receptor 9 nM (IC50) |
H2L5186303 (0.3-10 μM, 30 min) inhibits mast cell degranulation[2].
H2L5186303 (10 μM, 2 days) inhibits LPA2 and promotes apoptosis in intestinal epithelial cells (IEC)[3].
H2L5186303 (10 μM) suppresses the cell motile activity of MG63-A12 cells in the presence of Lysophosphatidic acid[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:IECs
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Concentration:10 μM
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Incubation Time:0 and 2 days
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Result:Blocked intestinal-like growth, reduced cell proliferation.
H2L5186303 (10 mg/kg, given by intraperitoneal injection, three times every other day, 6 days) inhibits cell proliferation in Lpar5f/f Villin-Cre mice intestinal crypts and promotes apoptosis[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Ovalbumin-Induced allergic asthma in BALB/c mice[2]
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Dosage:1 mg/kg, single dose; 0, 6.25, 12.5, 25, 50 mg/mL, single dose
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Administration:Intraperitoneal injection (i.p.)
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Result:Showed strong inhibitory effects, reducing airway hyper-responsiveness, levels of inflammatory cytokines, mucus production, and the number of eosinophils before sensitization and toxin exposure in OVA.
Lowered AHR and inflammation scores.
Suppressed mRNA levels of IL-4, IL-13, and IFN-γ, but did not inhibit IgE levels.
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Animal Model:Lpar5f/f Villin-Cre mice[3]
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Dosage:10 mg/kg, every other day for three times, 6 days
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Administration:Intraperitoneal injection (i.p.)
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Result:Reduced the number of proliferating cells in the intestinal crypts of mice and increased cell apoptosis.
Chemical Information
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No. CAS 139262-76-3
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Appearance Solid
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Peso molecular 488.45
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Fòrmula C26H20N2O8
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Color Light yellow to yellow
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SMILES
OC(/C=C\C(NC(C=C1)=CC=C1OC2=CC=CC(OC3=CC=C(C=C3)NC(/C=C\C(O)=O)=O)=C2)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Diabetologia
Phosphodiesterase ENPP2, which is co-upregulated in obese and pregnant mice, is essential for islet beta cell compensation during obesity. [Abstract]2025 Dec 26. PMID: 41454014 -
Sci China Life Sci
2025 Feb;68(2):441-453. PMID: 39400871 -
Eur J Pharmacol
Inhibition of lysophosphatidic acid receptor 2 attenuates neonatal chronic lung disease in mice by preserving vascular and alveolar development. [Abstract]2024 Dec 15:985:177120. PMID: 39522686
Solvente y solubilidad
DMSO : 250 mg/mL (511.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Fells JI, et al. Structure-based drug design identifies novel LPA3 antagonists. Bioorg Med Chem. 2009 Nov 1;17(21):7457-64. [Content Brief]
[2]. Ye-Ji Lee, et al. Efficacy Comparison of LPA2 Antagonist H2L5186303 and Agonist GRI977143 on Ovalbumin-Induced Allergic Asthma in BALB/c Mice. Int J Mol Sci. 2022 Aug 28;23(17):9745. [Content Brief]
[3]. Zhongxing Liang, et al. Compensatory Upregulation of LPA2 and Activation of the PI3K-Akt Pathway Prevent LPA5-Dependent Loss of Intestinal Epithelial Cells in Intestinal Organoids. Cells. 2022 Jul 20;11(14):2243. [Content Brief]
[4]. Ishimoto K, et al. Rapid establishment of highly migratory cells from cancer cells for investigating cellular functions. J Recept Signal Transduct Res. 2019 Jun;39(3):194-198. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0473 mL | 10.2365 mL | 20.4729 mL | 51.1823 mL |
| 5 mM | 0.4095 mL | 2.0473 mL | 4.0946 mL | 10.2365 mL | |
| 10 mM | 0.2047 mL | 1.0236 mL | 2.0473 mL | 5.1182 mL | |
| 15 mM | 0.1365 mL | 0.6824 mL | 1.3649 mL | 3.4122 mL | |
| 20 mM | 0.1024 mL | 0.5118 mL | 1.0236 mL | 2.5591 mL | |
| 25 mM | 0.0819 mL | 0.4095 mL | 0.8189 mL | 2.0473 mL | |
| 30 mM | 0.0682 mL | 0.3412 mL | 0.6824 mL | 1.7061 mL | |
| 40 mM | 0.0512 mL | 0.2559 mL | 0.5118 mL | 1.2796 mL | |
| 50 mM | 0.0409 mL | 0.2047 mL | 0.4095 mL | 1.0236 mL | |
| 60 mM | 0.0341 mL | 0.1706 mL | 0.3412 mL | 0.8530 mL | |
| 80 mM | 0.0256 mL | 0.1280 mL | 0.2559 mL | 0.6398 mL | |
| 100 mM | 0.0205 mL | 0.1024 mL | 0.2047 mL | 0.5118 mL |
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