SAR114137 is a potent inhibitor of human cathepsin S (Ki: 6 nM) and is 3- to 4-fold less active against cathepsin K (Ki: 16 nM). Cathepsin S inhibition was confirmed in vivo as oral administration of SAR114137 to mice inhibited the cathepsin S-dependent processing of MHCII in spleen. Shows analgesic-like properties in chronic pain models induced by inflammation/cartilage degradation or by nerve injury. Robust pain lowering efficacy in range <1 μg to <1 mg/kg in mouse with efficacy seen at 1 mg/kg in all tested species. Has a rapid onset of action in pain models (1-2 h) and a long duration of action (i.e., 3 days after last admin.) but no PK/PD relationship (short half-life). It is active in a wide range from (1, 10 mg/kg) and shows no anti-inflammatory activity. Note: Many web page listed mistakenly listed CAS#537706-31-3 was SAR-114137. However, the correct structure was published in Eur J Pharm Biopharm. 2013 Apr;83(3):436-48. It has CAS#958853-11-7. SAR114137-analog structure is completely different than SAR114137.
MedKoo Cat#: 556060
Name: SAR-114137
CAS#: 958853-11-7
Chemical Formula: C17H24F2N4O2
Exact Mass: 354.1867
Molecular Weight: 354.40
Elemental Analysis: C, 57.61; H, 6.83; F, 10.72; N, 15.81; O, 9.03
The following data is based on the product molecular weight 354.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
