Art. -Nr.: HY-P0025

NIM811

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

16 Cited Publications

Kundenbewertung

Based on 16 publication(s) in Google Scholar

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) .

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.93%
CAS. Nr.: 143205-42-9
Formel: C₆₂H₁₁₁N₁₁O₁₂
Molecular Weight:1202.61

Speicherung:

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)

NIM811 Chemical Structure

CAS. Nr.: 143205-42-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (16)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

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

Alle Cyclophilin Isoform-spezifische Produkte anzeigen :

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	210 nM Compound: 2, NIM811	Antiviral activity against HCV subtype 1b in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene in presence of 40% human serum Antiviral activity against HCV subtype 1b in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene in presence of 40% human serum	[PMID: 25310383]
Huh-7	EC₅₀	217 nM Compound: 2, NIM811	Antiviral activity against HCV subtype 1a in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene Antiviral activity against HCV subtype 1a in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene	[PMID: 25310383]
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]
Huh-7	EC₅₀	97 nM Compound: 2, NIM811	Antiviral activity against HCV subtype 1b in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene Antiviral activity against HCV subtype 1b in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene	[PMID: 25310383]
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]
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]
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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 143205-42-9
Appearance Solid
Molecular Weight 1202.61
Formel C₆₂H₁₁₁N₁₁O₁₂
Color White to off-white
Synonyms

(Melle-4)cyclosporin; SDZ NIM811
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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)

Publications (16)

All OthersCell Imaging/StainingIn Vivo Efficacy StudyCell Proliferation/Viability Assay

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Journal Impact Factor

Adv Sci (Weinh)

CypD Dependent mPTP Opening Is Crucial for Oxidized Mitochondrial DNA Release in Ferroptosis. [Abstract]

2026 Apr;13(20):e02239. PMID: 41700459
Cell Death Differ

Ca2+-mediated mitochondrial inner membrane permeabilization induces cell death independently of Bax and Bak. [Abstract]

2022 Jul;29(7):1318-1334. PMID: 35726022

NIM811 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2022 Jul;29(7):1318-1334. [Abstract]

The IncuCyte imaging system was used to quantitatively analyze cell death in HeLa cells after treatment with 25 μM m-3M3FBS combined with 20 μM cyclosporine A (CsA), 20 μM NIM-811, or 20 μM Alisporivir for 6 hours.
Acta Pharmacol Sin

Alkalization of the intracellular pH reprograms TNF-α signaling from inflammatory NF-κB activation to tumoricidal RIP kinase-dependent necroptosis in cancer cells. [Abstract]

2026 Apr 8. PMID: 41951772
EMBO J

Cyclophilin D plays a critical role in the survival of senescent cells. [Abstract]

2024 Dec;43(23):5972-6000. PMID: 39448884

NIM811 purchased from MedChemExpress. Usage Cited in: EMBO J. 2024 Dec;43(23):5972-6000. [Abstract]

Survival curves obtained with increasing concentrations of NIM811 in IMR90, proliferating or senescent, compared to vehicle (DMSO). Senescence was induced by treatment with doxorubicin (IMR90) or bleomycin (A549) for 7 days before the initiation of NIM811 treatment for 6 days.
Biochem Pharmacol

CypA inhibition attenuates diabetic hypoglycemia-induced cognitive impairment via the CD147/NF-κB/MMP-9 pathway. [Abstract]

2026 Mar 21:249:117917. PMID: 41871720
Commun Biol

Mitochondrial permeability transition dictates mitochondrial maturation upon switch in cellular identity of hematopoietic precursors. [Abstract]

2024 Aug 9;7(1):967. PMID: 39122870

NIM811 purchased from MedChemExpress. Usage Cited in: Commun Biol. 2024 Aug 9;7(1):967. [Abstract]

Seahorse assays showed that AGM cells treated with NIM811 exhibited increased oxygen consumption rate (OCR) and extracellular acidification rate (ECAR), indicating enhanced bioenergetic status.
Sci Rep

The cyclophilin inhibitor NIM-811 increases muscle cell survival with hypoxia in vitro and improves gait performance following ischemia-reperfusion in vivo. [Abstract]

2021 Mar 17;11(1):6152. PMID: 33731782
J Physiol

Novel mitochondrial transition pore inhibitor N-methyl-4-isoleucine cyclosporin is a new therapeutic option in acute pancreatitis. [Abstract]

2019 Dec;597(24):5879-5898. PMID: 31631343

NIM811 purchased from MedChemExpress. Usage Cited in: J Physiol. 2019 Dec;597(24):5879-5898. [Abstract]

In CCCP-treated catheters, we found no significant difference in TOM20 staining levels between the NIM811 (2 μM) treated group and the untreated group. Compared with the WT control group, NIM811 itself did not alter the TOM20 staining level.

NIM811 purchased from MedChemExpress. Usage Cited in: J Physiol. 2019 Dec;597(24):5879-5898. [Abstract]

Administration of 10 mg/kg NIM811 after injury significantly reduced edema and leukocyte infiltration levels compared to the WT CER treatment group.
iScience

BRCA1 mediates protein homeostasis through the ubiquitination of PERK and IRE1. [Abstract]

2022 Nov 19;25(12):105626. PMID: 36471805
Liver Res

Protective effects of cyclosporine and its analog NIM-811 in a murine model of hepatic ischemia-reperfusion injury. [Abstract]

2024 Mar 5;8(1):46-53. PMID: 39959032
J Biol Chem

BL-918 activates PINK1/Parkin signaling pathway to ameliorate the progression of Parkinson's disease. [Abstract]

2024 Aug;300(8):107543. PMID: 38992440
Neurodegener Dis

Suppression of NLRP3 Inflammasome, Pyroptosis, and Cell Death by NIM811 in Rotenone-Exposed Cells as an in vitro Model of Parkinson's Disease. [Abstract]

2020;20(2-3):73-83. PMID: 33176317
Karolinska Institutet

2026.
Res Sq

2025 Aug 11.
bioRxiv

2023 Jun 28.
University of Szeged

2019.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

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].

MedChemExpress (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].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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

Keywords

NIM811

16 Cited Publications

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NIM811

Macrocyclic Compound Library

Peptide Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) NIM811

Alle Cyclophilin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (16)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NIM811

Macrocyclic Compound Library

Peptide Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) NIM811

Alle Cyclophilin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (16)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NIM811 Related Classifications

HY-P0025 Related Classifications