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SID 26681509 is a selective, reversible and competitive human cathepsin L inhibitor (IC50 of 56 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $60 | In Stock | |
5 mg | $147 | In Stock | |
10 mg | $228 | In Stock | |
25 mg | $459 | In Stock | |
50 mg | $687 | In Stock | |
100 mg | $979 | In Stock | |
1 mL x 10 mM (in DMSO) | $175 | In Stock |
Description | SID 26681509 is a selective, reversible and competitive human cathepsin L inhibitor (IC50 of 56 nM). |
Targets&IC50 | P. falciparum:15.4 μM , Cathepsin L (human):56 nM , Leishmania major:12.5 μM |
In vitro | After a 4-hour preincubation with cathepsin L, SID 26681509 becomes more potent (IC50: 1.0 nM). SID 26681509 acts as a slow-binding, slowly reversible competitive inhibitor with inhibition rate constants kon = 24,000 M^-1s^-1 and koff = 2.2 × 10^-5 s^-1 (Ki = 0.89 nM), as determined through transient kinetic analysis for single-step reversibility. Molecular docking studies, using the X-ray crystal structure of papain/CLIK-148[1], show that SID 26681509 inhibits papain and cathepsins B, K, S, and V with IC50 values ranging from 618 nM to 8.442 μM after one hour[1]. |
In vivo | survival in murine models of sepsis significantly improved SID 26681509 by and reduces liver damage following warm liver ischemia/reperfusion (I/R) models[2]. |
Molecular Weight | 539.65 |
Formula | C27H33N5O5S |
Cas No. | 958772-66-2 |
Smiles | CCc1ccccc1NC(=O)CSC(=O)NNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C |
Relative Density. | 1.298 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/ml (101.92 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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