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Sepimostat

Chemical Structure : Sepimostat

CAS No.: 103926-64-3

Sepimostat (FUT-187, FUT187)

Catalog No.: PC-20173Not For Human Use, Lab Use Only.

Sepimostat (FUT-187) is a potent multi-protease inhibitor with IC50 of 0.097 uM for trypsin, 0.029 uM for pancreatic kallikrein, 0.61 uM for plasma kallikrein, 0.57uM for plasmin, 2.5 uM for thrombin, 20.4 uM for factor Xa and 6.4 uM for C1r.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Sepimostat (FUT-187) is a potent multi-protease inhibitor with IC50 of 0.097 uM for trypsin, 0.029 uM for pancreatic kallikrein, 0.61 uM for plasma kallikrein, 0.57uM for plasmin, 2.5 uM for thrombin, 20.4 uM for factor Xa and 6.4 uM for C1r.
Sepimostat (FUT-187) acts as a noncompetitive inhibitor for factor XIIa and an uncompetitive inhibitor for C1s with Ki value of 0.021 and 0.18 uM, respectively.
Sepimostat (FUT-187) inhibits the kinin formation by glandular kallikrein in the rat plasma with IC50 of 0.024 uM.
Sepimostat (FUT-187) also inhibits the complement-mediated hemolyses in the classical and alternative pathways with IC50 of 0.17 and 3.5 uM, respectively.
Sepimostat (FUT-187) is a potent and selective inhibitor of trypsin-like serine proteases, and its inhibitory activities are stronger than those of camostat on glandular kallikrein, factor XIIa and C1s in complement pathway.

Physicochemical Properties

M.Wt 373.42
Formula C21H19N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(6-carbamimidoylnaphthalen-2-yl) 4-(4,5-dihydro-1H-imidazol-2-ylamino)benzoate

References

1. Fuwa M, et al. Sci Rep. 2019 Dec 31;9(1):20409.

2. Zhigulin AS, et al. Eur J Pharmacol. 2023 Jan 5;938:175394.

3. Nakamura K, et al. Yakugaku Zasshi. 1995 Mar;115(3):201-12.

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