| Identification | Back Directory | [Name]
Fasitibant chloride hydrochloride | [CAS]
869880-33-1 | [Synonyms]
MEN16132
MEN-16132
MEN 16132
Fasitibant chloride (HCl salt)
Fasitibant chloride hydrochloride
[(4S)-4-amino-5-[4-[4-[[2,4-dichloro-3-[(2,4-dimethylquinolin-8-yl)oxymethyl]phenyl]sulfonylamino]oxane-4-carbonyl]piperazin-1-yl]-5-oxopentyl]-trimethylazanium:chloride:hydrochloride | [Molecular Formula]
C36H50Cl4N6O6S | [MDL Number]
MFCD30343541 | [MOL File]
869880-33-1.mol | [Molecular Weight]
836.696 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
Fasitibant chloride hydrochloride (100 μg; knee injection; single dose) significantly reduces the release of IL-1b, IL-6, GRO/PINC-1 synovial cytokines, the formation of PGE metabolites, the activity of myeloperoxidase (MPO) induced by Carrageenan (HY-125474) in rats, and the effect was more significant when combined with Dexamethasone (HY-14648)[2].
| Animal Model: | Male wistar rats?with inflammatory arthritis[2] | | Dosage: | 100 μg per knee | | Administration: | Injection into the knee joint; 100 μg per knee; combines with dexamethasone | | Result: | Was more effective than each drug administered alone in inhibiting knee joint inflammation.
Reduced joint pain and diminished joint oedema. |
| Animal Model: | Male Wistar rats?with inflammatory arthritis[2] | | Dosage: | 100 μg per knee | | Administration: | Injection into the knee joint; 100 μg per knee; combines with dexamethasone | | Result: | Was more effective than each drug administered alone in inhibiting knee joint inflammation.
Reduced joint pain and diminished joint oedema. |
| [IC 50]
Bradykinin B2 Receptor (B2R) | [References]
[1] S Meini, et al. Fasitibant prevents the bradykinin and interleukin 1β synergism on prostaglandin E? release and cyclooxygenase 2 expression in human fibroblast-like synoviocytes. Naunyn Schmiedebergs Arch Pharmacol. 2012 Aug;385(8):777-86. DOI:10.1007/s00210-012-0762-y
[2] Claudio Valenti, et al. Fasitibant chloride, a kinin B? receptor antagonist, and dexamethasone interact to inhibit carrageenan-induced inflammatory arthritis in rats. Br J Pharmacol. 2012 Jun;166(4):1403-10. DOI:10.1111/j.1476-5381.2012.01861.x |
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