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西那司特

西那司特用途

Ro 24-5913(Cinalukast)是一种口服活性和有效的LTD4拮抗剂,IC50值为6.4nM。Ro 24-5913可用于哮喘研究[1]。

西那司特名称

[ CAS 号 ]:
128312-51-6

[ 中文名 ]:
西那司特

[ 英文名 ]:
Cinalukast

[英文别名 ]:

Cinalukast

西那司特生物活性

[ 描述 ]:

Ro 24-5913(Cinalukast)是一种口服活性和有效的LTD4拮抗剂,IC50值为6.4nM。Ro 24-5913可用于哮喘研究[1]。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 白三烯受体

研究领域 >> 炎症/免疫

[ 靶点 ]

IC50: 6.4 nM (LTD4)[1]

[体外研究]

Ro 24-5913与[3H]LTD4竞争其在豚鼠肺膜中的结合位点,IC50值为6.4nM[1]。Ro 24-5913显示了对LTD4诱导的收缩的有效拮抗剂效力,pKB值为9.3[1]。

[体内研究]

Ro 24-5913(静脉注射10 mg/kg和口服100 mg/kg；一次)抑制LTD4诱导的豚鼠支气管收缩,静脉注射和口服LD50分别为0.13和0.12 mg/kg[1]。动物模型：豚鼠[1]剂量：10 mg/kg给药：口服灌胃；结果：抑制LTD4诱导的豚鼠支气管收缩和抗原诱导的支气管收缩。

西那司特物理化学性质

[ 密度 ]:
1.258g/cm3

[ 分子式 ]:
C₂₃H₂₈N₂O₃S

[ 分子量 ]:
412.54500

[ 精确质量 ]:
412.18200

[ PSA ]:
107.53000

[ LogP ]:
5.87360

[ 折射率 ]:
1.655

西那司特安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

西那司特文献

Participation of leukotriene C(4) in the regulation of suicidal erythrocyte death.

J. Physiol. Pharmacol. 60(3) , 135-43, (2009)

Eryptosis, the suicidal death of erythrocytes, is characterized by cell shrinkage and cell membrane scrambling with phosphatidylserine exposure at the erythrocyte surface. Eryptosis is triggered by in...

Prolonged protection against exercise-induced bronchoconstriction by the leukotriene D4-receptor antagonist cinalukast.

J. Allergy Clin. Immunol. 99(2) , 210-5, (1997)

The degree and duration of protection against exercise-induced bronchoconstriction afforded by three doses of a specific leukotriene D4 receptor antagonist, cinalukast, were assessed after an initial ...

Heterogeneity of binding sites for ICI 198,615 in human lung parenchyma.

Biochem. Pharmacol. 44(7) , 1411-5, (1992)

We have identified and characterized two different subclasses of binding site for the novel peptido-leukotriene (LT) antagonist, [3H]ICI 198,615, in membranes from human lung parenchyma using a recept...

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