| Bioactivity | 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]. |
| Invitro | Fasitibant chloride hydrochloride (1 µM；30 min) 减少了滑膜细胞中 BK 诱导的 PGE2 形成和 COX-2 基因表达[1]。 |
| In Vivo | Fasitibant chloride hydrochloride (100 µg；膝盖注射；单剂量) 显著降低了大鼠中卡拉胶 (Carrageenan，HY-125474) 诱导的 IL-1b、IL-6、GRO/CINC-1 滑膜细胞因子的释放，PGE 代谢产物的形成，髓过氧化物酶 (MPO) 的活性，当与地塞米松 (Dexamethasone，HY-14648) 联用时效果更显著[2]。 Animal Model: |
| Name | Fasitibant chloride hydrochloride |
| CAS | 869880-33-1 |
| Formula | C36H50Cl4N6O6S |
| Molar Mass | 836.70 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
Fasitibant chloride hydrochloride
CAS: 869880-33-1 F: C36H50Cl4N6O6S W: 836.70
Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, high affinity, and long-lasting nonpeptide bradykin
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This product is for research use only, not for human use. We do not sell to patients.