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Fasitibant (chloride hydrochloride)

Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant chloride hydrochloride has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis[1].

Product Specifications

CAS Number

[869880-33-1]

Product Name Alternative

MEN16132

UNSPSC

12352005

Target

Bradykinin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/fasitibant-chloride-hydrochloride.html

Solubility

10 mM in DMSO

Smiles

O=C(N(CC1)CCN1C([C@@H](N)CCC[N+](C)(C)C)=O)C2(CCOCC2)N[S](=O)(C(C=CC(Cl)=C3COC4=CC=CC(C(C)=C5)=C4N=C5C)=C3Cl)=O.[Cl-].Cl

Molecular Formula

C36H50Cl4N6O6S

Molecular Weight

836.70

References & Citations

[1]S Meini, et al. Fasitibant prevents the bradykinin and interleukin 1β synergism on prostaglandin E₂ release and cyclooxygenase 2 expression in human fibroblast-like synoviocytes. Naunyn Schmiedebergs Arch Pharmacol. 2012 Aug;385 (8) :777-86.|[2]Claudio Valenti, et al. Fasitibant chloride, a kinin B₂ receptor antagonist, and dexamethasone interact to inhibit carrageenan-induced inflammatory arthritis in rats. Br J Pharmacol. 2012 Jun;166 (4) :1403-10.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

Bradykinin B2 Receptor (B2R)

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