BCX 1470 methanesulfonate

Short Summary : Serine protease inhibitor

Category : Proteases|Serine Protease

Purity : 0.98

CAS Number : 217099-44-0

Formula : C15H14N2O5S3

Molecular Weight : 398.48

SMILE : CS(=O)(=O)O.C1=CSC(=C1)C(=O)OC2=CC3=C(C=C2)C=C(S3)C(=N)N

Solubility : Soluble in DMSO

Storage : Store at -20°C

Description : BCX 1470 is a serine protease inhibitor with the IC50 of 96 nM for factor D and 1.6 nM for C1s [1].Serine proteases are enzymes that cleave peptide bonds in proteins which are found ubiquitously in both eukaryotes and prokaryotes and serine serves as the nucleophilic amino acid at the active site. According to structure, serine proteases are divided into trypsin-like (chymotrypsin-like) family and subtilisin-like family. It is reported that serine proteases play an important role in various physiological functions, including digestion, immune response, blood coagulation and reproduction. [2] [3].BCX 1470 is a potent serine protease inhibitor and functions on the complement enzymes CIs and factor D sites. By determining the ability of enzyme to hydrolyze appropriate synthetic substrates, the result showed that BCX 1470 inhibited the factor D and C1s esterolytic activity which were important in the function of serine protease [1].In induced dermal RPA reaction rat model, administration of BCX 1470 markedly abbrogated the RPA reaction via inhibiting edema development and complement activity by inactivation of C1s and factor D enzymatic activity [1].It is also reported that BCX 1470 inhibited Trypsin with the IC50 value of 326 nM [1].References: [1]. Szalai, A.J., et al., The Arthus reaction in rodents: species-specific requirement of complement. J Immunol, 2000. 164(1): p. 463-8.[2]. Srivastava, A. and Q. Dong, Regulation of a serine protease homolog by the JNK pathway during thoracic development of Drosophila melanogaster. FEBS Open Bio, 2015. 5: p. 117-23.[3]. Yamasaki, K., et al., Increased serine protease activity and cathelicidin promotes skin inflammation in rosacea. Nat Med, 2007. 13(8): p. 975-80.

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