AZ 11645373
Based on 1 Customer Validation
AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors，AZ11645373 inhibits ATP-evoked IL-1β release from lipopolysaccharide-activated THP-1 cells , with an IC50 value of 90 nM.
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- Purity : 99.54%
- CAS No.: 227088-94-0
- 화학식: C24H21N3O5S
- 분자량:463.51
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보관:
Store at room temperature 3 years.
In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
In Vitro
AZ11645373 produces a concentration-dependent inhibition of BzATP-mediated calcium transients, with complete inhibition observed at concentrations between 100 and 300 nM according to concentration-inhibition curves[1].
AZ11645373 inhibits ATP- or BzATP-evoked YO-PRO1 fluorescence in HEK cells stably expressing hP2X7R, but not in cells expressing rP2X7R, with an KB value not significantly different from those obtained in experiments measuring membrane currents or calcium mobilization[1].
AZ11645373 (0.01, 0.1, 1 μM; 30 min) has no significant effect on basal levels of IL-1β in culture medium of LPS-treated cells, but produces a concentration-dependent inhibition of ATP-mediated IL-1β release with a calculated KB value of 92 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 227088-94-0
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Appearance Solid
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분자량 463.51
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화학식 C24H21N3O5S
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Color Off-white to light yellow
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SMILES
O=C(N1C(COC2=CC=C(C3=CC=CC([N+]([O-])=O)=C3)C=C2)CCC4=CC=NC=C4)SCC1=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Store at room temperature 3 years
In solvent -80°C 2 years -20°C 1 year
용액&용해도
In Vitro:
DMSO : 17.5 mg/mL (37.76 mM; ultrasonic and warming and heat to 60°C; 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, 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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
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Pyroptosis Solutions
Pyroptosis is a lytic inflammatory cell-death pathway executed by gasdermin pores, most classically through inflammasome-mediated activation of caspase-1, cleavage of gasdermin D, membrane pore formation, LDH release, and secretion of IL-1β and IL-18. The canonical pathway is commonly modeled by priming cells with an inflammatory signal such as LPS to induce pro-IL-1β and inflammasome components, followed by an activation signal such as ATP or nigericin to activate NLRP3, ASC speck formation, caspase-1 cleavage, GSDMD cleavage, cytokine release, and pyroptotic membrane rupture. The non-canonical pathway is triggered when cytosolic LPS activates mouse caspase-11 or human caspase-4/5, leading to GSDMD cleavage and pyroptosis, and this can secondarily activate NLRP3-dependent IL-1β release. Pyroptosis is linked to inflammatory injury, infection, cancer, liver disease, ocular disease, placental inflammation, and other disease phenotypes, but unresolved questions include which gasdermin fam
순도&문서
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Data Sheet (271 KB)
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SDS (614 KB)
- English - EN (614 KB)
- Français - FR (614 KB)
- Deutsch - DE (614 KB)
- Norwegian - NO (614 KB)
- Español - ES (614 KB)
- Swedish - SV (614 KB)
- Italian - IT (614 KB)
- Korean - KR (614 KB)
- Portuguese - PT (614 KB)
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Handling Instructions (2659 KB)
References
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 | 2.1575 mL | 10.7873 mL | 21.5745 mL | 53.9363 mL |
| 5 mM | 0.4315 mL | 2.1575 mL | 4.3149 mL | 10.7873 mL | |
| 10 mM | 0.2157 mL | 1.0787 mL | 2.1575 mL | 5.3936 mL | |
| 15 mM | 0.1438 mL | 0.7192 mL | 1.4383 mL | 3.5958 mL | |
| 20 mM | 0.1079 mL | 0.5394 mL | 1.0787 mL | 2.6968 mL | |
| 25 mM | 0.0863 mL | 0.4315 mL | 0.8630 mL | 2.1575 mL | |
| 30 mM | 0.0719 mL | 0.3596 mL | 0.7192 mL | 1.7979 mL |
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