114606-56-3
114606-56-3 結(jié)構(gòu)式
基本信息
中文別名
化合物 T12873 英文別名
MKS 492SDZ 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-
物理化學(xué)性質(zhì)
沸點(diǎn)648.7±65.0 °C(Predicted)
密度1.36±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO : 250 mg/mL (576.75 mM; Need ultrasonic)
酸度系數(shù)(pKa)14.25±0.10(Predicted)
形態(tài)Solid
顏色White to off-white
常見(jiàn)問(wèn)題列表
生物活性
SDZ-MKS 492 (MKS 492) 一種選擇性的環(huán)狀 GMP 抑制的磷酸二酯酶 (III 型 PDE) 抑制劑。SDZ-MKS 492 抑制豚鼠和大鼠中抗原或血小板活化因子 (PAF) 誘導(dǎo)的支氣管收縮和過(guò)敏反應(yīng)。靶點(diǎn)
type III phosphodiesterase
體外研究
MKS 492 relaxes airway smooth muscle in vitro.
體內(nèi)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. |