1. Anti-infection
    Metabolic Enzyme/Protease
  2. HCV
    Mitochondrial Metabolism
  3. NIM811

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

Cat. No.: HY-P0025 Purity: 99.55%
Handling Instructions

NIM811 ((Melle-4)cyclosporin; SDZ NIM811) is a potent and 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.

NIM811 Chemical Structure

NIM811 Chemical Structure

CAS No. : 143205-42-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 3143 In-stock
Estimated Time of Arrival: December 31
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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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

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  • References

Description

NIM811 ((Melle-4)cyclosporin; SDZ NIM811) is a potent and 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]

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 interferon 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].

In Vivo

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

Clinical Trial
Storage
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (83.15 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (2.29 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (2.29 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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
Molecular Weight

1202.61

Formula

C₆₂H₁₁₁N₁₁O₁₂

CAS No.

143205-42-9

SMILES

C/C=C/C[[email protected]]([[email protected]@H](O)[[email protected]@]1(N(C)C([[email protected]]([H])(C(C)C)N(C)C([[email protected]](CC(C)C)N(C)C([[email protected]]([H])(CC(C)C)N(C)C([[email protected]@H](C)NC([[email protected]](C)NC([[email protected]@H](N(C([[email protected]@]([H])(NC([[email protected]@]([H])(N(C(CN(C([[email protected]@H](NC1=O)CC)=O)C)=O)C)[[email protected]](CC)C)=O)C(C)C)=O)C)CC(C)C)=O)=O)=O)=O)=O)=O)[H])C

Shipping

Room temperature in continental US; may vary elsewhere

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Cat. No.: HY-P0025