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Product Name:Fasitibant chloride hydrochloride
CAS:869880-33-1
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| | 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 | | EINECS: | | | Product Categories: | | | Mol File: | 869880-33-1.mol |  |
| | Fasitibant chloride hydrochloride Chemical Properties |
| | 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 |
| | Fasitibant chloride hydrochloride Preparation Products And Raw materials |
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