AZD4144
Based on 1 Customer Validation
AZD4144 is an orally active NLRP3 inhibitor (EC50: 0.082 μM). AZD4144 effectively inhibits the release of IL-1β when NLRP3 is overactivated, exerting an anti-inflammatory effect. AZD4144 has low inhibitory effect on hERG and low cardiotoxicity. AZD4144 has the potential to study diseases and conditions associated with NLRP3 inflammasome activation.
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- Purity: 99.67%
- CAS No.: 2890191-41-8
- 화학식: C18H16F3N3O3
- 분자량:379.33
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
AZD4144 (Example 1) inhibits Nigericin (HY-127019)- and Lipopolysaccharides (HY-D1056) (LPS)-induced human NLRP3 puncta formation in THP-ASC-GFP cells (EC50: 0.082 μM)[1].
AZD4144 effectively inhibits Nigericin-induced IL-1β release from THP-1 human monocytes (IC50: 0.027 μM)[1].
AZD4144 effectively inhibits BzATP (HY-136254)-induced IL-1β release from THP-1 human monocytes (IC50: 0.01 μM)[1].
AZD4144 has a low inhibitory effect on hERG in Chinese hamster ovary K1 cells expressing hERG (IC50: > 40 μM), has no cardiotoxicity, and is highly safe[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/cAJcl mice (male, aged 7 weeks) injected with LPS (0.5 mL of 4 pg/mL) and ATP (0.5 mL of 30 pmol/L)[1]
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Dosage:3 mg/kg
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Administration:p.o. one dose
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Result:Showed an inhibition rate of 82% on IL-1β.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2890191-41-8
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Appearance Solid
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분자량 379.33
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화학식 C18H16F3N3O3
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Color Off-white to light yellow
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SMILES
OC1=C(C2=C(C=CC=C3)C3=C(NC[C@H](O)CO)N=N2)C=CC(C(F)(F)F)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 125 mg/mL (329.53 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)
순도&문서
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Data Sheet (273 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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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, 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 | 2.6362 mL | 13.1811 mL | 26.3623 mL | 65.9057 mL |
| 5 mM | 0.5272 mL | 2.6362 mL | 5.2725 mL | 13.1811 mL | |
| 10 mM | 0.2636 mL | 1.3181 mL | 2.6362 mL | 6.5906 mL | |
| 15 mM | 0.1757 mL | 0.8787 mL | 1.7575 mL | 4.3937 mL | |
| 20 mM | 0.1318 mL | 0.6591 mL | 1.3181 mL | 3.2953 mL | |
| 25 mM | 0.1054 mL | 0.5272 mL | 1.0545 mL | 2.6362 mL | |
| 30 mM | 0.0879 mL | 0.4394 mL | 0.8787 mL | 2.1969 mL | |
| 40 mM | 0.0659 mL | 0.3295 mL | 0.6591 mL | 1.6476 mL | |
| 50 mM | 0.0527 mL | 0.2636 mL | 0.5272 mL | 1.3181 mL | |
| 60 mM | 0.0439 mL | 0.2197 mL | 0.4394 mL | 1.0984 mL | |
| 80 mM | 0.0330 mL | 0.1648 mL | 0.3295 mL | 0.8238 mL | |
| 100 mM | 0.0264 mL | 0.1318 mL | 0.2636 mL | 0.6591 mL |