1. Metabolic Enzyme/Protease
  2. Cathepsin

MIV-247 

Cat. No.: HY-112583
Handling Instructions

MIV-247 is a selective cathepsin S inhibitor with Kis of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively.

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

MIV-247 Chemical Structure

MIV-247 Chemical Structure

CAS No. : 1352817-76-5

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

MIV-247 is a selective cathepsin S inhibitor with Kis of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively.

IC50 & Target

IC50: 2.1 nM (Human Cathepsin S), 4.2 nM (Mouse Cathepsin S), 7.5 nM (Cynomolgus monkey Cathepsin S)[1]

In Vivo

Oral administration of MIV-247 (100-200 µmol/kg) dose-dependently attenuates mechanical allodynia by up to approximately 50% reversal when given as a single dose or when given twice daily for 5 days. Cathepsin S inhibition with MIV-247 exerts significant antiallodynic efficacy alone, and also enhances the effect of gabapentin and pregabalin without increasing side effects or inducing pharmacokinetic interactions[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5550 mL 12.7750 mL 25.5500 mL
5 mM 0.5110 mL 2.5550 mL 5.1100 mL
10 mM 0.2555 mL 1.2775 mL 2.5550 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]

MIV-247 is administered via oral gavage to Male C57BL/6 mice (20-30 g) at a dose volume of 5 ml/kg at doses up to 200 µmol/kg. In the PK studies, seven blood samples (20 µL) are drawn from the lateral saphenous vein of each mouse at 15 minutes, 30 minutes, 1 hour, 2 hours, 3 hours, 5 hours, and 7 hours postdose[1].

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

References
Molecular Weight

391.39

Formula

C₁₇H₂₄F₃N₃O₄

CAS No.

1352817-76-5

SMILES

FC1(-;@C-;@C-;@C-;@C-;@1)C[[email protected]](NC(C(F)(F)C)=O)C(NC2(-;@C-;@C-;@C-;@2)C(C(N)=O)=O)=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
MIV-247
Cat. No.:
HY-112583
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MIV-247

Cat. No.: HY-112583