Product Overview
C1s 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). 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 surgery.
Synonyms
Thrombin inhibitor; BCX 1470; BCX-1470;
Molecular Formula
C14H10N2O2S2
Chemical Name
(2-carbamimidoyl-1-benzothiophen-6-yl) thiophene-2-carboxylate
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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.
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.
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