Fasitibant chloride hydrochloride

Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, high affinity, and longlasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant chloride hydrochloride has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis, et al.

Product information

CAS Number: 869880-33-1

Molecular Weight: 836.70

Formula: C36H50Cl4N6O6S

Chemical Name: [(4S)-4-amino-5-{4-[4-(2,4-dichloro-3-{[(2,4-dimethylquinolin-8-yl)oxy]methyl}benzenesulfonamido)oxane-4-carbonyl]piperazin-1-yl}-5-oxopentyl]trimethylazanium hydrochloride chloride

Smiles: [Cl-].Cl.CC1C=C(C)N=C2C(=CC=CC=12)OCC1C(Cl)=CC=C(C=1Cl)S(=O)(=O)NC1(CCOCC1)C(=O)N1CCN(CC1)C(=O)[C@@H](N)CCC[N+](C)(C)C

InChiKey: QIAWOUUTKDMGTE-UJXPALLWSA-M

InChi: InChI=1S/C36H49Cl2N6O6S.2ClH/c1-24-22-25(2)40-33-26(24)8-6-10-30(33)50-23-27-28(37)11-12-31(32(27)38)51(47,48)41-36(13-20-49-21-14-36)35(46)43-17-15-42(16-18-43)34(45)29(39)9-7-19-44(3,4)5;;/h6,8,10-12,22,29,41H,7,9,13-21,23,39H2,1-5H3;2*1H/q+1;;/p-1/t29-;;/m0../s1

Technical Data

Appearance: Solid Power

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

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:

Fasitibant exhibits high affinity for the BK binding site, pKi values 8.9 in intact cells and 10.17-Ki 0.067 nM in cell membrane in synovial cells.Fasitibant also echibits high antagonist potency in blocking the effects produced by BK in these cells both after 1 h-(phospholipase C activation, pKB=9.9) and 24 h-incubation (release of IL-6 and IL-8, pIC50 8.1 and 8.4, respectively). Fasitibant chloride hydrochloride (1 μM; 30 min preincubation before BK) prevents BK-induced sustained production of PGE2 and transient COX-2 gene expression in synovial fibroblasts. Fasitibant chloride hydrochloride completely prevents the potentiating effect of BK on IL-1β, both in terms of PGE2 production and COX-2 gene expression in synovial fibroblasts.

In Vivo:

Fasitibant chloride hydrochloride (injection into the knee joint ;100 µg per knee; combines with dexamethasone) is more effective than each agent administered alone in inhibiting knee joint inflammation and release of inflammatory mediators. Fasitibant chloride alone reaches a comparable maximal inhibitory effect of about 40–45% on the carrageenan-induced joint pain, however, Combination administration achieves full inhibition in male Wistar rats with inflammatory arthritis.

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