AS2717638
Based on 2 publication(s) in Google Scholar
AS2717638 is a highly selective, brain-penetrant and orally active lysophosphatidic acid receptor 5 (LPA5) antagonist with an IC50 value of 38 nM. AS2717638 is highly selective and shows no significant antagonistic activity against other LPA receptors (LPA1, LPA2, and LPA3). AS2717638 can be used in the research of pain and neuroinflammation-related diseases.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.85%
- No. CAS: 2148339-28-8
- Fòrmula: C25H25N3O5
- Peso molecular:447.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) AS2717638
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Actividad biológica
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LPA5 Receptor 38 nM (IC50, Human) |
LPA5 Receptor 9.1 nM (Ki, Human) |
LPA5 Receptor 16 nM (Ki, Rat) |
LPA5 Receptor 7.3 nM (Ki, Mouse) |
AS2717638 (0.038 μM; 20 min) inhibits LPA-induced cAMP accumulation in the cAMP accumulation assay using CHO cells expressing human LPA5[2].
AS2717638 (0.1 μM, 1 μM; 24 h) has no effect on MTT reduction in BV-2 cells, and the cell viability is not significantly affected; at 10 μM (24 h), the cell viability is reduced by 50%[2].
AS2717638 (0.1-1 μM; 2-24 h) inhibits the phosphorylation of STAT1, p65, and c-Jun in LPS-stimulated BV-2 cells. AS2717638 reduces the expression of TLR4 and COX2, and decreases NO production in LPS-stimulated BV-2 cells[2].
AS2717638 (0.1-1 μM; 2-24 h) reduces the secretion of cytokines and chemokines such as TNFα, IL-6, CXCL10, CXCL2, and CCL5 in the supernatants of LPS-stimulated BV-2 cell cultures[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BV-2 microglia
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Concentration:0.1 μM, 1 μM, 10 μM
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Incubation Time:24 h
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Result:At 0.1 μM and 1 μM, had no significant effect on cell viability as indicated by MTT reduction. At 10 μM, it compromised cell viability by 50%.
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Cell Line:BV-2 microglia
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Concentration:0.1 μM, 1 μM
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Incubation Time:2 h, 8 h, 24 h
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Result:Inhibited the phosphorylation of STAT1, p65, and c-Jun, reduced the expression of TLR4 and COX2, decreased NO production, and reduced the secretion of TNFα, IL-6, CXCL10, CXCL2, and CCL5 in LPS-stimulated BV-2 cells.
AS2717638 (10-30 mg/kg; oral administration; 1 h before the experiment; single dose) alleviates allodynia in mouse models of allodynia induced by PGE2, PGF2α, or AMPA[1].
AS2717638 (10 mg/kg; oral administration; 2 h before the experiment; single dose) ameliorates static mechanical allodynia and thermal hyperalgesia in a rat model of neuropathic pain induced by chronic constriction injury (CCI)[1].
AS2717638 (10 mg/kg; oral administration; 2 h before the experiment; single dose) improves hind paw weight - bearing ability in a rat model of inflammatory pain induced by adjuvant[1].
AS2717638 (10 mg/kg; oral administration; before the experiment; single dose) reduces LPS (HY-D1056)-induced iNOS, TNFα, IL-6, and CXCL2 mRNA expression, improves the expression of neuroinflammation - related proteins, and reduces peripheral cytokine concentrations in a mouse endotoxemia model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ICR mice, LPA- and GGPP-induced allodynia model[1]
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Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg (dissolved in 30% propylene glycol solvent in distilled water)
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Administration:Orally, administered once, 1 h before i.t. injection of LPA or GGPP
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Result:Significantly inhibited LPA- and GGPP-induced allodynia.
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Animal Model:Male ICR mice, PGE2-, PGF2α- or AMPA-induced allodynia model[1]
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Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg (dissolved in 30% propylene glycol solvent in distilled water)
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Administration:Orally, administered once, 1 h before i.t. injection of PGE2, PGF2α, or AMPA
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Result:Significantly alleviated allodynia in all three pain sensitizer-induced pain models.
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Animal Model:Male Sprague-Dawley rats, chronic constriction injury (CCI)-induced neuropathic pain model[1]
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Dosage:10 mg/kg (dissolved in 30% propylene glycol solvent in distilled water)
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Administration:Orally, administered once, 2 h before the von Frey and plantar tests
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Result:Significantly ameliorated both static mechanical allodynia and thermal hyperalgesia in CCI rats.
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Animal Model:Female Lewis rats, adjuvant-induced inflammatory pain model[1]
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Dosage:10 mg/kg (dissolved in 30% propylene glycol solvent in distilled water)
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Administration:10 mg/kg (dissolved in 30% propylene glycol solvent in distilled water)
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Result:Significantly improved weight bearing difference in a rat model of adjuvant-induced inflammatory pain.
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Animal Model:C57BL/6J mice (8-10 weeks, 20-30 g), mouse endotoxemia model[2]
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Dosage:10 mg/kg
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Administration:Orally, administered once, 24 h before sacrifice
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Result:Significantly reduced the mRNA expression of iNOS, TNFα, IL6, and CXCL2.
Also amended the expression of neuroinflammatory parameters such as TLR4, Iba1, GFAP, COX-2, and the Bax/Bcl2 ratio.
Chemical Information
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No. CAS 2148339-28-8
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Appearance Solid
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Peso molecular 447.48
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Fòrmula C25H25N3O5
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Color White to off-white
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SMILES
O=C1N(C=C(C2=C1C=C(C(OC)=C2)OC)C(N3CCCCC3)=O)C4=NOC5=C4C=C(C=C5)C
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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 (2)
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Journal Impact Factor
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Most Recent
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J Clin Invest
Autotaxin suppresses cytotoxic T cells via LPAR5 to promote anti-PD-1 resistance in non-small cell lung cancer. [Abstract]2023 Sep 1;133(17):e163128. PMID: 37655662 -
Placenta
Upregulation of PLAAT3 in syncytiotrophoblast induces activation of neutrophils via LPA-LPAR5 axis in preeclampsia. [Abstract]2025 Aug:168:219-231. PMID: 40623340
Solvente y solubilidad
DMSO : 60 mg/mL (134.08 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 6 mg/mL (13.41 mM); Clear solution
This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (289 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Murai N, et al. Analgesic effects of novel lysophosphatidic acid receptor 5 antagonist AS2717638 in rodents. Neuropharmacology. 2017 Nov;126:97-107. [Content Brief]
[2]. Joshi L, et al. Inhibition of Autotaxin and Lysophosphatidic Acid Receptor 5 Attenuates Neuroinflammation in LPS-Activated BV-2 Microglia and a Mouse Endotoxemia Model. Int J Mol Sci. 2021 Aug 7;22(16):8519. [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 | 2.2347 mL | 11.1737 mL | 22.3474 mL | 55.8684 mL |
| 5 mM | 0.4469 mL | 2.2347 mL | 4.4695 mL | 11.1737 mL | |
| 10 mM | 0.2235 mL | 1.1174 mL | 2.2347 mL | 5.5868 mL | |
| 15 mM | 0.1490 mL | 0.7449 mL | 1.4898 mL | 3.7246 mL | |
| 20 mM | 0.1117 mL | 0.5587 mL | 1.1174 mL | 2.7934 mL | |
| 25 mM | 0.0894 mL | 0.4469 mL | 0.8939 mL | 2.2347 mL | |
| 30 mM | 0.0745 mL | 0.3725 mL | 0.7449 mL | 1.8623 mL | |
| 40 mM | 0.0559 mL | 0.2793 mL | 0.5587 mL | 1.3967 mL | |
| 50 mM | 0.0447 mL | 0.2235 mL | 0.4469 mL | 1.1174 mL | |
| 60 mM | 0.0372 mL | 0.1862 mL | 0.3725 mL | 0.9311 mL | |
| 80 mM | 0.0279 mL | 0.1397 mL | 0.2793 mL | 0.6984 mL | |
| 100 mM | 0.0223 mL | 0.1117 mL | 0.2235 mL | 0.5587 mL |
AS2717638 Related Classifications
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