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

Name: NIM811
Brand: MedChemExpress
SKU: HY-P0025
Rating: 5.0 (12 reviews)

Cat. No.: HY-P0025 Purity: 99.88%: FAQs
Data Sheet SDS COA Handling Instructions

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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) .

For research use only. We do not sell to patients.

Custom Peptide Synthesis

NIM811 Chemical Structure

CAS No. : 143205-42-9

Size	Price	Stock	Quantity
1 mg	USD 336	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 1188	In-stock	Estimated Time of Arrival: December 31
10 mg		Get quote
50 mg		Get quote

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Customer Review

Based on 12 publication(s) in Google Scholar

12 Publications Citing Use of MCE NIM811

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View All Cyclophilin Isoform Specific Products:

View All Isoforms

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

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

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

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]

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 a-IFN significantly enhances anti-HCV activities without causing any increase of cytotoxicity^[1]. NIM811 blocks the mitochondrial permeability transition induced by calcium and inorganic phosphate^[2].

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

In Vivo

NIM811 prevents mitochondrial depolarization thereby attenuates liver injury, stimulates regeneration and improves liver function and survival^[3].

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

Clinical Trial

Molecular Weight

1202.61

Formula

C₆₂H₁₁₁N₁₁O₁₂

CAS No.

143205-42-9

Appearance

Solid

Color

White to off-white

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (83.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (4.16 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (4.16 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 2.5 mg/mL (2.08 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.88%

Select Batch:

Data Sheet (284 KB) SDS (252 KB)

COA (261 KB) HNMR (537 KB) RP-HPLC (270 KB) LCMS (98 KB)

Handling Instructions (2659 KB)

References

[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.
References	[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

NIM811 Related Classifications

Inflammation/Immunology Infection

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

Customer Review

NIM811 Related Antibodies

12 Publications Citing Use of MCE NIM811

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Cyclophilin Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

NIM811 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

NIM811 Related Classifications

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