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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.59%
- CAS 番号: 2455519-86-3
- 分子式: C21H29N3O3S
- 分子量:403.54
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
NLRP3[1]
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2455519-86-3
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性状 Solid
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分子量 403.54
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
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 |