256649-36-2
256649-36-2
Chemical Structure
CRA-2059
- CAS No.: 256649-36-2
- Formula:C34H46N12O8
- Molecular Weight:750.80
IUPAC Name: (3R,6R)-hexahydrofuro[3,2-b]furan-3,6-diyl bis(4-((4-guanidinobenzyl)carbamoyl)piperazine-1-carboxylate)
InChIKey: SDKLWMXBZVGUHI-XPALAHHGSA-N
SMILES: NC(NC1=CC=C(CNC(N2CCN(C(O[C@@H]3COC4[C@H](OC(N5CCN(C(NCC6=CC=C(NC(N)=N)C=C6)=O)CC5)=O)COC34)=O)CC2)=O)C=C1)=N
Biological Activity: CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ)[1][2].
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CRA-2059 | CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ). | |||||||||||||||||||||
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References
- [1]. Tremaine WJ, et al. Treatment of mildly to moderately active ulcerative colitis with a tryptase inhibitor (APC 2059): an open-label pilot study. Aliment Pharmacol Ther. 2002;16(3):407-413. [Content Brief]
- [2]. Selwood T, et al. Potent bivalent inhibition of human tryptase-beta by a synthetic inhibitor. Biol Chem. 2003;384(12):1605-1611. [Content Brief]
