NIM811|143205-42-9|((Melle-4)cyclosporin; SDZ NIM811)-陌孚医药/Medlife

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NIM811 (Synonyms: (Melle-4)cyclosporin; SDZ NIM811)

目录号: PL05739 纯度: ≥99%

CAS No. :143205-42-9

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中文名称	NIM811
中文别名	[MeIle]4-环孢素;(melle-4)cyclosporin
英文名称	NIM811
英文别名	Cyclosporin A,9-(N-methyl-L-isoleucine)-;(3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-24-[(2S)-butan-2-yl]-30-ethyl-33-[(E,1R,2R)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18-tris(2-methylpropyl)-3,21-di(propan-2-yl)-1,4;SDZ NIM811;(Melle-4)cyclosporin;30-ethyl-33-[(4E)-1-hydroxy-2-methylhex-4-en-1-yl]-1,4,7,10,12,15,19,25,28-nonamethyl-3,21-bis(1-methylethyl)-24-(1-methylpropyl)-6,9,18-tris(2-methylpropyl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone;9-(N-Methyl-L-isoleucine)cyclosporin A;NIM 811;Sdz-nim-811;NIM811
Cas No.	143205-42-9
分子式	C₆₂H₁₁₁N₁₁O₁₂
分子量	1202.61
包装储存	Stored under nitrogen, away from moisturePowder -80°C 2 years；-20°C 1 year

产品详情

NIM811 ((Melle-4)cyclosporin; SDZ NIM811) 是一种具有口服活性的线粒体渗透转换 (mitochondrial permeability transition) 和亲环蛋白 (cyclophilin) 双抑制剂，对丙型肝炎病毒 (HCV) 具有很强的体外活性。

生物活性

NIM811 ((Melle-4)cyclosporin; SDZ NIM811) is an orally bioavailable mitochondrial permeability transition and cyclophilin dual inhibitor, which exhibits potent in vitro activity against hepatitis C virus (HCV) .

性状

Solid

IC50 & Target[1][2]

Cyclophilin, Mitochondrial Permeability Transition Inhibitor

体外研究(In Vitro)

NIM811 induces a concentration-dependent reduction of HCV RNA in the replicon cells with an IC50 of 0.66 μM at 48 h. In addition, the combination of NIM811 with alpha IFN significantly enhances anti-HCV activities without causing any increase of cytotoxicity. NIM811 blocks the mitochondrial permeability transition induced by calcium and inorganic phosphate. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

NIM811 prevents mitochondrial depolarization thereby attenuates liver injury, stimulates regeneration and improves liver function and survival. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Stored under nitrogen, away from moisturePowder -80°C 2 years；-20°C 1 year

ClinicalTrial

参考文献

[1]. Ma S, et al. NIM811, a cyclophilin inhibitor, exhibits potent in vitro activity against hepatitis C virus alone or in combination with alpha IFN. Antimicrob Agents Chemother. 2006 Sep;50(9):2976-82.
[2]. Waldmeier PC, et al. Inhibition of the mitochondrial permeability transition by the nonimmunosuppressive cyclosporin derivative NIM811. Mol Pharmacol. 2002 Jul;62(1):22-9.

溶解度数据	In Vitro: DMSO : 200 mg/mL (166.30 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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