117928-94-6
中文名稱
雷帕替奈
英文名稱
GLYX 13
CAS
117928-94-6
分子式
C18H31N5O6
分子量
413.47
MOL 文件
117928-94-6.mol
更新日期
2024/12/23 10:30:26
117928-94-6 結(jié)構(gòu)式
基本信息
中文別名
雷帕替奈醋酸雷帕替奈
雷帕替奈, >99%
RAPASTINEL游離態(tài)
H-THR-PRO-PRO-THR-NH2
(S)-N-((2S,3R)-1-氨基-3-羥基-1-氧代丁-2-基)-1-((S)-1-((2S,3R)-2-氨基-3-羥基丁?；?吡咯烷-2-羰基)吡咯烷-2-甲酰胺
英文別名
GLYX 13GIYX-13
CS-1640
Rapastinel
TPPT-amide
UNII-6A1X56B95E
NRX-1074 GLYX-13
GLYX13(Rapastinel)
Rapastinel(GLYX-13)
Thr-Pro-Pro-Thr-NH2
所屬類別
生物化工：激動(dòng)劑抑制劑物理化學(xué)性質(zhì)
沸點(diǎn)844.2±65.0 °C(Predicted)
密度1.370±0.06 g/cm3(Predicted)
儲(chǔ)存條件?20°C
儲(chǔ)存條件Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度DMF: 25 mg/ml; DMSO: 15 mg/ml; Ethanol: 10 mg/ml; PBS (pH 7.2): 5 mg/ml
酸度系數(shù)(pKa)12.26±0.45(Predicted)
形態(tài)粉末
顏色白色至棕褐色
水溶解性Soluble to 2 mg/ml in water
應(yīng)用領(lǐng)域
用途1
一種NMDAR(N-甲基-D-天冬氨酸受體)調(diào)節(jié)劑, 具有部分激動(dòng)劑特性。Rapastinel is a novel antidepressant drug approved as an adjunctive therapy for the treatment of treatment-resistant major depressive disorder. It is a centrally active, intravenously administered (non-orally active) amidated tetrapeptide (Thr-Pro-Pro-Thr-NH2) that acts as a selective, weak partial agonist (mixed antagonist/agonist) of an allosteric site at the glycine site of the NMDA receptor complex (Emax ≈ 25%).The drug is a rapid-acting and long-lasting antidepressant as well as robust cognitive enhancer by virtue of its ability to both inhibit and enhance NMDA receptor-mediated signal transduction.