GSK-1482160
Based on 1 Customer Validation
GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.67%
- No. CAS: 1001389-72-5
- Fòrmula: C14H14ClF3N2O2
- Peso molecular:334.72
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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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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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Actividad biológica
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P2X7 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
119.3 nM
Compound: 1b; GSK1482160
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Inhibition of human P2X7 expressed in human HEK293 cells assessed as reduction in BzATP-stimulated TO-PRO-3 incorporation preincubated with compound and TO-PRO-3 for 15 mins prior to BzATP addition and measured after 1 hr by Fluo-3AM dye based flow cytome
Inhibition of human P2X7 expressed in human HEK293 cells assessed as reduction in BzATP-stimulated TO-PRO-3 incorporation preincubated with compound and TO-PRO-3 for 15 mins prior to BzATP addition and measured after 1 hr by Fluo-3AM dye based flow cytome
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[PMID: 31525963] |
| HEK293 | IC50 |
332.4 nM
Compound: 1b; GSK1482160
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Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell membrane incubated for 1 hr by microplate scintillation counting method
Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell membrane incubated for 1 hr by microplate scintillation counting method
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[PMID: 31525963] |
| HEK293 | IC50 |
8.9 nM
Compound: GSK1482160
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Displacement of [11C]GSK1482160 from human recombinant P2X7 receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method based radioligand competitive binding assay
Displacement of [11C]GSK1482160 from human recombinant P2X7 receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method based radioligand competitive binding assay
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[PMID: 31005444] |
GSK-1482160 (Compound 31) has extremely low clearance rates in both rat and human liver microsomes, and shows no significant inhibition on the major CYP450 subtypes (1A2, 2C9, 2C19, 2D6, 3A4)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GSK-1482160 (20 mg/kg, p.o., twice daily for 8 days) significantly reverses mechanical allodynia 1 h post dose on day 1 and this effect was maintained for the duration of the dosing period in the rat chronic constriction injury (CCI) model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Chronic knee joint inflammatory pain induced by complete Freund's adjuvant (CFA) established in rats[2]
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Dosage:5, 20 and 50 mg/kg
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Administration:Oral administration (p.o.), twice daily for 5 days
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Result:Exhibited the analgesic effect comparable to that of the Celecoxib (HY-14398) at a dose of 50 mg/kg.
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Animal Model:Neurogenic pain induced by sciatic nerve ligation in rats[2]
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Dosage:20 mg/kg
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Administration:Oral administration (p.o.), twice daily for 8 days
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Result:Effectively alleviated neuropathic pain, and its effect was comparable to that of Gabapentin (HY-A0057).
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1001389-72-5
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Appearance Solid
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Peso molecular 334.72
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Fòrmula C14H14ClF3N2O2
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Color White to off-white
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SMILES
O=C([C@H](CC1)N(C)C1=O)NCC2=CC=CC(C(F)(F)F)=C2Cl
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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
Solvente y solubilidad
DMSO : 100 mg/mL (298.76 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
[2]. Abdi MH, et al. Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5080-4. [Content Brief]
[3]. Liu X, et al. Unlocking the therapeutic potential of P2X7 receptor: a comprehensive review of its role in neurodegenerative disorders. Front Pharmacol. 2024 Jul 30;15:1450704. [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 | 2.9876 mL | 14.9379 mL | 29.8757 mL | 74.6893 mL |
| 5 mM | 0.5975 mL | 2.9876 mL | 5.9751 mL | 14.9379 mL | |
| 10 mM | 0.2988 mL | 1.4938 mL | 2.9876 mL | 7.4689 mL | |
| 15 mM | 0.1992 mL | 0.9959 mL | 1.9917 mL | 4.9793 mL | |
| 20 mM | 0.1494 mL | 0.7469 mL | 1.4938 mL | 3.7345 mL | |
| 25 mM | 0.1195 mL | 0.5975 mL | 1.1950 mL | 2.9876 mL | |
| 30 mM | 0.0996 mL | 0.4979 mL | 0.9959 mL | 2.4896 mL | |
| 40 mM | 0.0747 mL | 0.3734 mL | 0.7469 mL | 1.8672 mL | |
| 50 mM | 0.0598 mL | 0.2988 mL | 0.5975 mL | 1.4938 mL | |
| 60 mM | 0.0498 mL | 0.2490 mL | 0.4979 mL | 1.2448 mL | |
| 80 mM | 0.0373 mL | 0.1867 mL | 0.3734 mL | 0.9336 mL | |
| 100 mM | 0.0299 mL | 0.1494 mL | 0.2988 mL | 0.7469 mL |
GSK-1482160 Related Classifications
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