NIM811
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) .
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.93%
- No. CAS: 143205-42-9
- Fòrmula: C62H111N11O12
- Peso molecular:1202.61
-
Almacenamiento:
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) NIM811
More- Adv Sci (Weinh). 2026 Apr;13(20):e02239. [Abstract]
- Cell Death Differ. 2022 Jul;29(7):1318-1334. [Abstract]
- Acta Pharmacol Sin. 2026 Apr 8. [Abstract]
- EMBO J. 2024 Dec;43(23):5972-6000. [Abstract]
- Biochem Pharmacol. 2026 Mar 21:249:117917. [Abstract]
- Commun Biol. 2024 Aug 9;7(1):967. [Abstract]
- Sci Rep. 2021 Mar 17;11(1):6152. [Abstract]
- J Physiol. 2019 Dec;597(24):5879-5898. [Abstract]
- iScience. 2022 Nov 19;25(12):105626. [Abstract]
- Liver Res. 2024 Mar 5;8(1):46-53. [Abstract]
- J Biol Chem. 2024 Aug;300(8):107543. [Abstract]
- Neurodegener Dis. 2020;20(2-3):73-83. [Abstract]
- Karolinska Institutet. 2026.
- Res Sq. 2025 Aug 11.
- bioRxiv. 2023 Jun 28.
- University of Szeged. 2019.
Customer Validation & Images
-
Cell Proliferation/Viability Assay
-
Others
-
Cell Proliferation/Viability Assay
-
Cell Imaging/Staining
-
In Vivo Efficacy Study
Ver todos los productos específicos de isoformas Cyclophilin
More
Actividad biológica
Cyclophilin[1], Mitochondrial Permeability Transition Inhibitor[2]
|
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] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 143205-42-9
-
Appearance Solid
-
Peso molecular 1202.61
-
Fòrmula C62H111N11O12
-
Color White to off-white
-
Synonyms
(Melle-4)cyclosporin; SDZ NIM811
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
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)
-
Journal Impact Factor
-
Most Recent
-
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
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
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 -
-
-
-
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal 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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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.
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.
Pureza y Documentación
-
Ficha de datos (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)
-
Instrucciones de manejo (2659 KB)
Referencias
[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
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.
| 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
HY-P0025 Related Classifications
Powered by Bioz