Usnoflast
Based on 1 Customer Validation
Usnoflast is the selective, orally active inhibitor for NLRP3 that blocks the release of IL-1β, and exhibits anti-inflammatory activity.
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- Purity : 98.59%
- CAS No.: 2455519-86-3
- 화학식: C21H29N3O3S
- 분자량:403.54
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
제품 설명
IC50 & Target
NLRP3[1]
In Vitro
Usnoflast inhibits Nigericin (HY-127019)-induced IL-1β release in THP-1 cells, ATP (HY-B2176)-mediated IL-1β release in human PBMCs, and Nigericin (HY-127019)-mediated IL-1β release in primary mouse microglia, IC50s are 11 nM, 4.5 nM and 43 nM, respectively[2].
Usnoflast inhibits the oligomerization of caspase recruitment domain (ASC), interfere with the formation of NLRP3 inflammasome complex[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Usnoflast (10-60 mg/kg, po, twice daily for 5 weeks) improves the motor dysfunction of mice, and reduces the abnormal accumulation of α-synuclein in MPTP (HY-15608)-induced Parkinson's disease model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MPTP (HY-15608)-induced mouse Parkinson's disease model[2]
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Dosage:10-60 mg/kg
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Administration:po, twice daily for 5 weeks
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Result:Improved the motor dysfunction of mice, reduced the abnormal accumulation of α-synuclein, increased the number of tyrosine hydroxylase (TH)-positive dopaminergic neurons.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2455519-86-3
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Appearance Solid
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분자량 403.54
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화학식 C21H29N3O3S
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Color White to off-white
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SMILES
C[C@]1(N(CCC1)C)/C=C/S(NC(NC2=C3C(CCC3)=CC4=C2CCC4)=O)(=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 62.5 mg/mL (154.88 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, 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)
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
순도&문서
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Data Sheet (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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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 | 2.4781 mL | 12.3903 mL | 24.7807 mL | 61.9517 mL |
| 5 mM | 0.4956 mL | 2.4781 mL | 4.9561 mL | 12.3903 mL | |
| 10 mM | 0.2478 mL | 1.2390 mL | 2.4781 mL | 6.1952 mL | |
| 15 mM | 0.1652 mL | 0.8260 mL | 1.6520 mL | 4.1301 mL | |
| 20 mM | 0.1239 mL | 0.6195 mL | 1.2390 mL | 3.0976 mL | |
| 25 mM | 0.0991 mL | 0.4956 mL | 0.9912 mL | 2.4781 mL | |
| 30 mM | 0.0826 mL | 0.4130 mL | 0.8260 mL | 2.0651 mL | |
| 40 mM | 0.0620 mL | 0.3098 mL | 0.6195 mL | 1.5488 mL | |
| 50 mM | 0.0496 mL | 0.2478 mL | 0.4956 mL | 1.2390 mL | |
| 60 mM | 0.0413 mL | 0.2065 mL | 0.4130 mL | 1.0325 mL | |
| 80 mM | 0.0310 mL | 0.1549 mL | 0.3098 mL | 0.7744 mL | |
| 100 mM | 0.0248 mL | 0.1239 mL | 0.2478 mL | 0.6195 mL |