Clemastine Fumarate,14976-57-9

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YZ剂描述：

产品名称：Clemastine Fumarate

产品别名：富马酸氯马斯汀

英文别名：Meclastine fumarate

靶点：Histamine H1 receptor

CAS：14976-57-9

纯度：>98%

外观：白色或类白色结晶性粉末

保存方法：-20°C

描述：

Clemastine Fumarate是一种选择性组胺H1受体拮抗剂，IC50为3 nM。Clemastine Fumarate作用于HL-60细胞，更有效YZ组胺诱导的[Ca²⁺]_iZG，IC50为3 nM，而Chlorpheniramine或Diphenhydramine作用时，IC50分别为20 nM 和 100 nM。 Clemastine Fumarate浓度≥25 μM时, 作用于人红白血病细胞系K562和人B-成淋巴细胞系SB，分别显著YZ淋巴细胞的NK 和ADCC。 Clemastine Fumarate YZ组胺诱导的豚鼠回肠收缩，IC50为231 nM。

溶解性：DMSO ：23 mg/mL (50 mM)

体外研究：

Clemastine Fumarate inhibits histamine induced rise in i in HL-60 cells with an IC50 of 3 nM as compared with that of chlorpheniramine or diphenhydramine with IC50 values of 20 nM and 100 nM, respectively. At concentrations of ≥25 μM, Clemastine Fumarate significantly blocks NK and ADCC reactions of lymphocytes against the human erythroleukemia cell line K562 and human B-lymphoblast cell line SB, respectively. Clemastine Fumarate inhibits histamine-induced contraction of guinea pig ileum with an IC50 of 231 nM. Clemastine Fumarate potently inhibits the HERG K+ channel in a concentration-dependent manner in HEK 293 cells stably expressing HERG channels with an IC50 of 12 nM, which can be attenuated by the Y652A or F656A mutation of HERG. Clemastine Fumarate significantly potentiates ATP-induced increase in i in HEKhP2X7 cells not relying on histamine receptor blockage but on sensitizing P2X7 receptor in a concentration-dependent manner with an EC50 of 10 μM, and increases the IL-1β release from LPS-induced human macrophages.

体内研究：Administration of Clemastine Fumarate (5-20 mg/kg) displays significantly inhibitory effect on simultaneously induced zymosan paw oedema and croton oil ear oedema in rats in a dose-dependent manner, with the inhibition of 53.6% and 46.8%, respectively, at the dose of 20 mg/kg, and with ID50 values of 18.0 mg/kg and 20.5 mg/kg, respectively. Clemastine Fumarate treatment strongly reduces innate immune responses to Listeria monocytogenes in mice by interfering with the extracellular signal-regulated kinase (ERK)-mediated production of proinflammatory cytokines such as TNF-α and IL-6 surprisingly not dependent on blocking the histamine H1 receptor, leading to significantly higher mortality.

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