NP3-742
NP3-742 is an orally active NLRP3 inhibitor that binds to the NLRP3 NACHT domain. NP3-742 inhibits IL-1β release with IC50s of 6 nM and 47 nM in both the cellular and whole blood assays, respectively. NP3-742 is highly selective against a panel of more than 50 enzymes, receptors and sodium and calcium channels. NP3-742 can be used for the study of gout, cardiovascular disease or osteoarthritis.
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。
- 分子式: C19H24N6
- 分子量:336.43
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
|
NLRP3 |
IL-1β 6 nM (IC50) |
| Species | Dose | Route | CL | Vss | T1/2 | F |
|---|---|---|---|---|---|---|
| Dog[1] | 0.1 mg/kg | i.v. | 10 mL/min/kg | 6.3 L/kg | 9.4 h | / |
| Dog[1] | 0.3 mg/kg | p.o. | 10 mL/min/kg | 6.3 L/kg | 9.4 h | 75 % |
| Mice[1] | 1 mg/kg | i.v. | 27 mL/min/kg | 2.9 L/kg | 2.0 h | / |
| Mice[1] | 3 mg/kg | p.o. | 27 mL/min/kg | 2.9 L/kg | 2.0 h | 54 % |
| Rat[1] | 0.3 mg/kg | i.v. | 29 mL/min/kg | 6.9 L/kg | 3.9 h | / |
| Rat[1] | 3 mg/kg | p.o. | / | 6.9 L/kg | 29 mL/min/kg | 93 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57BL6/JRj mice (7-13 weeks) were challenged with LPS (2.5 mg/kg) for 2 h[1]
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Dosage:0.3 mg/kg, 1 mg/kg, 3 mg/kg
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Administration:Oral; 1 h prior to LPS; once
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Result:Showed complete inhibition of IL-1β in the acute mouse peritonitis model when administered at 3 mg/kg p.o.
Lower doses of 1 and 0.3 mg/kg, resulted in 78 and 66% efficacy, respectively.
化学情報
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分子量 336.43
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分子式 C19H24N6
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SMILES
CC1=CC2=C(N1)N=C(C=C2)C3=C(C=C(N=N3)N[C@@H]4CCCN(C4)C)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
NP3-742 関連分類
HY-179024 関連分類
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