114606-56-3

中文名称 SDZ-MKS 492

英文名称 SDZ MKS 492

CAS 114606-56-3

分子式 C20H27N5O6

分子量 433.46

MOL 文件 114606-56-3.mol

114606-56-3 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 T12873

英文别名

MKS 492
SDZ MKS 492
1H-Purine-2,6-dione, 8-[[(1R)-1-(3,4-dimethoxyphenyl)-2-hydroxyethyl]amino]-3,7-dihydro-7-(2-methoxyethyl)-1,3-dimethyl-

物理化学性质

沸点648.7±65.0 °C(Predicted)

密度1.36±0.1 g/cm3(Predicted)

储存条件-20°C储存

溶解度DMSO : 250 mg/mL (576.75 mM; Need ultrasonic)

酸度系数(pKa)14.25±0.10(Predicted)

形态Solid

颜色White to off-white

常见问题列表

生物活性

SDZ-MKS 492 (MKS 492) 一种选择性的环状 GMP 抑制的磷酸二酯酶 (III 型 PDE) 抑制剂。SDZ-MKS 492 抑制豚鼠和大鼠中抗原或血小板活化因子 (PAF) 诱导的支气管收缩和过敏反应。

靶点

type III phosphodiesterase

体外研究

MKS 492 relaxes airway smooth muscle in vitro.

体内研究

MKS-492 (3-10 mg/kg; i.v.) inhibits antigen-induced bronchoconstriction in guinea pigs.
MKS-492 (1-3 mg/kg; i.v.) inhibits PAF-induced bronchoconstriction and the increase in airway responsiveness to histamine in guinea pigs.
MKS-492 (30-100 mg/kg; i.p.) inhibits leukotriene B4 (LTB4)-induced airway eosinophilia in guinea pigs.
MKS-492 (10-100 mg/kg; i.p.) inhibits passive cutaneous anaphylaxis and mediator-induced skin reactions in rats.

Animal Model:	Female Hartley guinea pigs (250-300 g) were passively sensitized with anti-BPO BGG guinea pig serum
Dosage:	3, 10 mg/kg
Administration:	I.v. 5 min before antigen challenge
Result:	Inhibited antigen-induced bron choconstriction in a dose-related manner.