CRA-2059

CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ).

Product information

CAS Number: 256649-36-2

Molecular Weight: 750.80

Formula: C34H46N12O8

Chemical Name: (3R,6R)-6-(4-{[(4-carbamimidamidophenyl)methyl]carbamoyl}piperazine-1-carbonyloxy)-hexahydrofuro[3,2-b]furan-3-yl 4-{[(4-carbamimidamidophenyl)methyl]carbamoyl}piperazine-1-carboxylate

Smiles: NC(=N)NC1C=CC(CNC(=O)N2CCN(CC2)C(=O)O[C@@H]2COC3C2OC[C@H]3OC(=O)N2CCN(CC2)C(=O)NCC2C=CC(=CC=2)NC(N)=N)=CC=1

InChiKey: SDKLWMXBZVGUHI-XPALAHHGSA-N

InChi: InChI=1S/C34H46N12O8/c35-29(36)41-23-5-1-21(2-6-23)17-39-31(47)43-9-13-45(14-10-43)33(49)53-25-19-51-28-26(20-52-27(25)28)54-34(50)46-15-11-44(12-16-46)32(48)40-18-22-3-7-24(8-4-22)42-30(37)38/h1-8,25-28H,9-20H2,(H,39,47)(H,40,48)(H4,35,36,41)(H4,37,38,42)/t25-,26-,27?,28?/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Tryptase is a trypsin-like serine protease found as a major protein component in human mast cell secretory granules. CRA-2059 has the potential for inflammatory bowel disease research.

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.
2. Selwood T, et al. Potent bivalent inhibition of human tryptase-beta by a synthetic inhibitor. Biol Chem. 2003;384(12):1605-1611.

Products are for research use only. Not for human use.