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

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

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

NIM811 (SDZ NIM811) is a potent mitochondrial permeability transition inhibitor. Sequence: Cyclo[{Aaa}-{Abu}-{Sar}-Ile-Val-Leu-Ala-{D-Ala}-Leu-Leu-Val].

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
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

NIM811 (SDZ NIM811) is a potent mitochondrial permeability transition inhibitor. Sequence: Cyclo[{Aaa}-{Abu}-{Sar}-Ile-Val-Leu-Ala-{D-Ala}-Leu-Leu-Val].

In Vitro

NIM811 is a potent inhibitor of HCV RNA replication in the replicon cells. NIM811 induces a concentration-dependent reduction of HCV RNA in the replicon cells with an IC50 of 0.66 μM at 48 h. Furthermore, a greater than three-log10 viral RNA reduction is achieved after treating the cells with as little as 1 μM of NIM811 for 9 days. 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. NIM811 blocks cell killing and prevents in situ mitochondrial inner membrane permeabilization and depolarization during tumor necrosis factor-α–induced apoptosis to cultured rat hepatocytes[2].

In Vivo

NIM811 significantly blunts mitochondrial depolarization. Prevention of mitochondrial depolarization by NIM811 attenuates liver injury, stimulates regeneration and improves liver function and survival[3].

Clinical Trial
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

Storage
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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NIM811
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NIM811

Cat. No.: HY-P0025