122956-68-7
122956-68-7 結(jié)構(gòu)式
基本信息
中文別名
外消旋-莫地帕泛 英文別名
UK-74505Modipefant
rac-Modipafant
ethyl 4-(2-chlorophenyl)-6-methyl-2-(4-(2-methyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl)-5-(pyridin-2-ylcarbamoyl)-1,4-dihydropyridine-3-carboxylate(WXG02205)
4-(2-Chlorophenyl)-1,4-dihydro-6-Methyl-2-[4-(2-Methyl-1H-iMidazo[4,5-c]pyridin-1-yl)phenyl]-5-[(2-pyridinylaMino)carbonyl]-3-pyridinecarboxylic Acid Ethyl Ester
2-[4-(2-Methyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]-4-(2-chlorophenyl)-5-[(2-pyridinylamino)carbonyl]-6-methyl-1,4-dihydropyridine-3-carboxylic acid ethyl ester
3-Pyridinecarboxylic acid, 4-(2-chlorophenyl)-1,4-dihydro-6-methyl-2-[4-(2-methyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]-5-[(2-pyridinylamino)carbonyl]-, ethyl ester
物理化學(xué)性質(zhì)
密度1.34±0.1 g/cm3 (20 ºC 760 Torr)
儲(chǔ)存條件-20°C儲(chǔ)存
酸度系數(shù)(pKa)12.14±0.70(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
常見(jiàn)問(wèn)題列表
生物活性
(Rac)-Modipafant (UK-74505) 是一種口服的、選擇性的、長(zhǎng)效的不可逆血小板活化因子受體 (PAFR) 受體拮抗劑。(Rac)-Modipafant 預(yù)防嚴(yán)重登革熱感染。體內(nèi)研究
(Rac)-Modipafant (UK-74505) (10 mg/kg; p.o.; twice a day until day 10) prevents Severe Dengue Infection.
(Rac)-Modipafant exhibits highly selective, time-dependent inhibition of PAF-induced aggregation of rabbit washed platelets (IC
50
=26.3 and 1.12 nM after 0.25 and 60 min preincubation, respectively).
(Rac)-Modipafant (5-20 mg/kg; p.o.) dose-dependently inhibits the Zymosan -induced articular hyperalgesia.
| Animal Model: | 8- to 10-week-old BALB/c mice (DEN-2 strain infected) |
| Dosage: | 10 mg/kg |
| Administration: | P.o.; twice a day (started on days 0, 3, 5, or 7) until day 10 |
| Result: | Decreased by approximately 50% the lethality associated with DEN-2 infection. |
| Animal Model: | Male BALB/C (8- to 10- week-old) wild-type mice |
| Dosage: | 5, 10 and 20 mg/kg |
| Administration: | P.o. |
| Result: | Dose-dependently inhibited the Zymosan -induced articular hyperalgesia. |