Fasitibant chloride

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Fasitibant chloride

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1157852-02-2

MEN16132 free base

Fasitibant chloride (MEN16132 free base) 是一种有效的，选择性的非肽缓激肽 B2 受体 (B2R) 拮抗剂。Fasitibant chloride 在角叉菜胶诱发的关节炎大鼠模型中可减轻关节疼痛并减轻关节水肿。

生物活性

Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptidebradykinin B2 receptor (B2R)antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model^[1]^[2]^[3].

IC₅₀& Target

B2R^[1]^[2]

体外研究
(In Vitro)

Fasitibant chloride (MEN16132 free base; 1 μM; pre-treatment 30 min before BK) produces a consistent reduction of the FGF-2 expression (BK induced) and decrement of BK induced-FGFR-1 phosphorylation^[2].
Fasitibant chloride inhibits the phosphorylation of FRSα, ERK1/2, STAT3 (BK induced; 1 μM; for 15 min), except AKT in HUVEC^[2].

Cell Viability Assay^[2]

Cell Line:	human umbilical vein endothelial cells (HUVEC)
Concentration:	1 μM
Incubation Time:	Pre-treatment 30 min before Bradykinin (BK; 1 μM; for 24 h)
Result:	Produced a consistent reduction of the FGF-2 expression (BK induced) and decrement of BK induced-FGFR-1 phosphorylation (without affecting FGFR-2 activity).

体内研究
(In Vivo)

Fasitibant chloride (MEN16132 free base; 100 μg per knee; injection into the knee; 30 min before λ-carrageenan) inhibits about 40-45% on the carrageenan-induced joint pain and knee joint oedema^[1].

Animal Model:	Male Wistar rats weighing 250-300 g^[1]
Dosage:	100 μg per knee
Administration:	Injection into the knee; 30 min before λ-carrageenan
Result:	Inhibited about 40-45% on the carrageenan-induced joint pain and knee joint oedema. Reduced the neutrophil infiltration in the synovium by about 60% and the release of prostaglandins by about 30%.

Clinical Trial

分子量

800.23

Formula

C₃₆H₄₉Cl₃N₆O₆S

CAS 号

1157852-02-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.