Fasitibant chloride hydrochloride
Fasitibant chloride hydrochloride Basic information
- Product Name:
- Fasitibant chloride hydrochloride
- Synonyms:
-
- 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
- Fasitibant chloride (HCl salt)
- MEN 16132
- MEN16132
- MEN-16132
- CAS:
- 869880-33-1
- MF:
- C36H50Cl4N6O6S
- MW:
- 836.6958
- Mol File:
- 869880-33-1.mol
Fasitibant chloride hydrochloride Usage And Synthesis
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