BCX 1470

Short Summary : Serine protease inhibitor

Category : Proteases|Serine Protease

Purity : 0.98

CAS Number : 217099-43-9

Formula : C14H10N2O2S2

Molecular Weight : 302.38

SMILE : 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 : IC50: FD 96 nM, C1 1.6 nMC1s is an 80-kDa serine protease that mediates the proteolytic activity of the C1 complex by cleaving C2 and C4 both. BCX-1470, discovered in 1997 as a FD inhibitor (IC50=96 nM), was further found to be a very potent C1s inhibitor (IC50=1.6 nM).In vitro: BCX-1470 has the highest inhibitory activity of Factor D, with an IC50 of approx. 100 nM, which is two orders higher than the inhibitory activity of another commercially available general protease inhibitor, named FUT-175, when inhibting FD [1]. In vivo: BCX-1470 has been shown to be safe in animal toxicity studies and has blocked the development of reverse-passive Arthus reactioninduced oedema in rats [1]. Clinical trial: BCX-1470 has also been tested for safety in clinical trials with healthy volunteers but the outcome of these trials have not officially been published. Whereas no further clinical trials have been reported, a recent patent might indicate a future usage of the compound in the treatment of AMD. It suggests that BCX-1470 would be a candidate therapeutic for complement activation during cardiopulmonary bypass surgeryReference:[1] Morikis D, Lambris JD. Structural aspects and design of low-molecular-mass complement inhibitors. Biochem Soc Trans. 2002;30(Pt 6):1026-36.

Download datasheet