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

目录号: HY-P0025 纯度: 99.88%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

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。

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Custom Peptide Synthesis

NIM811 Chemical Structure

CAS No. : 143205-42-9

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规格	价格	是否有货
1 mg	￥2800	In-stock
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50 mg		询价

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Customer Review

MCE 顾客使用本产品发表的 12 篇科研文献

NIM811 相关产品

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Cyclophilin A Cyclophilin B Cyclophilin C Cyclophilin D Cyclophilin G Cyclophilin E

生物活性
实验参考方法
纯度 & 产品资料
参考文献

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) ^[1]^[2].

IC₅₀ & Target

Cyclophilin^[1], Mitochondrial Permeability Transition Inhibitor^[2]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
Huh-7	EC₅₀	0.084 μM Compound: NIM811	Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis	[PMID: 20176894]
Huh-7	EC₅₀	0.12 μM Compound: NIM811	Antiviral activity against wild type HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis Antiviral activity against wild type HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis	[PMID: 20176894]
Huh-7	EC₅₀	0.17 μM Compound: NIM811	Antiviral activity against HCV subtype 1b Con1 infected in cyclosporine A/NIM-resistant human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis Antiviral activity against HCV subtype 1b Con1 infected in cyclosporine A/NIM-resistant human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis	[PMID: 20176894]
Huh-7	EC₅₀	0.23 μM Compound: NIM811	Antiviral activity against HCV subtype 1b Con1 harboring wild type protease infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis Antiviral activity against HCV subtype 1b Con1 harboring wild type protease infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis	[PMID: 20176894]
Huh-7	EC₅₀	0.83 μM Compound: NIM811	Antiviral activity against cyclosporine A-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay Antiviral activity against cyclosporine A-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay	[PMID: 20176894]
Huh-7	EC₅₀	0.94 μM Compound: NIM811	Antiviral activity against HCV subtype 1b Con1 harboring NS5A C575G mutant protease infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis Antiviral activity against HCV subtype 1b Con1 harboring NS5A C575G mutant protease infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis	[PMID: 20176894]
Huh-7	EC₅₀	1.14 μM Compound: NIM811	Antiviral activity against HCV subtype 1b Con1 harboring NS5A and NS5B C575G mutant protease infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis Antiviral activity against HCV subtype 1b Con1 harboring NS5A and NS5B C575G mutant protease infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis	[PMID: 20176894]
Huh-7	EC₅₀	1.5 μM Compound: NIM811	Antiviral activity against cyclosporine A/NIM811-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis Antiviral activity against cyclosporine A/NIM811-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis	[PMID: 20176894]
Huh-7	EC₅₀	3.5 μM Compound: NIM811	Antiviral activity against cyclosporine A/NIM-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay Antiviral activity against cyclosporine A/NIM-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay	[PMID: 20176894]
MT4	IC₅₀	0.31 μM Compound: NIM811	Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay	[PMID: 18212100]
MT4	CC₅₀	13 μM Compound: 2, NIM811	Cytotoxicity against human MT4 cells by CDCF probe based assay Cytotoxicity against human MT4 cells by CDCF probe based assay	[PMID: 25310383]
MT4	EC₅₀	47 nM Compound: 9, NIM-811, [MeIle]4CsA	Antiviral activity against HIV1 3B infected in human MT4 cells coinfected with HTLV1 assessed as reduction in virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells coinfected with HTLV1 assessed as reduction in virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 23849880]
PBMC	IC₅₀	2.4 μM Compound: 2, NIM811	Cytotoxicity against PHA-stimulated human PBMC by 5-bromo-2'-deoxyuridine incorporation assay Cytotoxicity against PHA-stimulated human PBMC by 5-bromo-2'-deoxyuridine incorporation assay	[PMID: 25310383]

体外研究
(In Vitro)

NIM811 诱导复制子细胞中 HCV RNA 的浓度依赖性减少，48 小时的 IC₅₀ 值为 0.66 μM。此外，NIM811 与 α-IFN 的组合可显著增强抗 HCV 活性，而不会增加细胞毒性^[1]。NIM811 阻断钙和无机磷酸盐诱导的线粒体通透性转变^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

NIM811 可防止线粒体去极化，从而减轻肝损伤、刺激再生并改善肝功能和存活率^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

1202.61

Formula

C₆₂H₁₁₁N₁₁O₁₂

CAS 号

143205-42-9

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (83.15 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.8315 mL	4.1576 mL	8.3152 mL
5 mM	0.1663 mL	0.8315 mL	1.6630 mL
10 mM	0.0832 mL	0.4158 mL	0.8315 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (4.16 mM); 悬浊液; 超声助溶

此方案可获得 5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (4.16 mM); 澄清溶液

此方案可获得 ≥ 5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
方案三

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 2.5 mg/mL (2.08 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.88%

选择批次：

Data Sheet (649 KB) SDS (252 KB)

COA (298 KB) HNMR (537 KB) RP-HPLC (270 KB) LCMS (98 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

[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. [Content Brief]

[3]. Rehman H, et al. NIM811 prevents mitochondrial dysfunction, attenuates liver injury, and stimulates liverregeneration after massive hepatectomy. Transplantation. 2011 Feb 27;91(4):406-12. [Content Brief]

Cell Assay ^[1]	The antiviral activity and cytotoxicity of compounds are determined using an HCV replicon cell line (Huh-Luc/neo-ET) containing a luciferase reporter gene. Briefly, 5,000 replicon cells are seeded in each well of 96-well tissue culture plates and are allowed to attach in complete culture medium without G418 overnight. On the next day, the culture medium is replaced with medium containing serially diluted NIM811 in the presence of 10% FBS and 0.5% DMSO. After a 48-h NIM811 treatment, the remaining luciferase activities in the cells are determined^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Mice: Male C57BL/6 mice (8-12 weeks) are gavaged with NIM811, 10 mg/kg or an equal volume of vehicle containing 8.3% polyethoxylated castor oil and 8.3% ethanol at 2 h before surgery. Mice undergo massive hepatectomy or sham-operation under ether anesthesia. NIM811 (5 mg/kg) or vehicle is gavaged daily post-operatively for 2 days. Mice are observed for 21 days for survival^[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief] [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. [Content Brief] [3]. Rehman H, et al. NIM811 prevents mitochondrial dysfunction, attenuates liver injury, and stimulates liverregeneration after massive hepatectomy. Transplantation. 2011 Feb 27;91(4):406-12. [Content Brief]

NIM811 相关分类

Inflammation/Immunology Infection

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	0.8315 mL	4.1576 mL	8.3152 mL	20.7881 mL
	5 mM	0.1663 mL	0.8315 mL	1.6630 mL	4.1576 mL
	10 mM	0.0832 mL	0.4158 mL	0.8315 mL	2.0788 mL
	15 mM	0.0554 mL	0.2772 mL	0.5543 mL	1.3859 mL
	20 mM	0.0416 mL	0.2079 mL	0.4158 mL	1.0394 mL
	25 mM	0.0333 mL	0.1663 mL	0.3326 mL	0.8315 mL
	30 mM	0.0277 mL	0.1386 mL	0.2772 mL	0.6929 mL
	40 mM	0.0208 mL	0.1039 mL	0.2079 mL	0.5197 mL
	50 mM	0.0166 mL	0.0832 mL	0.1663 mL	0.4158 mL
	60 mM	0.0139 mL	0.0693 mL	0.1386 mL	0.3465 mL
	80 mM	0.0104 mL	0.0520 mL	0.1039 mL	0.2599 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NIM811143205-42-9(Melle-4)cyclosporin SDZ NIM811NIM 811NIM-811SDZ NIM811SDZ NIM 811SDZ NIM-811CyclophilinMitochondrial MetabolismHCVHepatitis C virusInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

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

Customer Review

MCE 顾客使用本产品发表的 12 篇科研文献