Sealed storage, away from moisture and lightPowder -80°C 2 years;-20°C 1 year
产品详情
Men 10376 TFA 是一种有效的选择性的 tachykinin NK-2 受体拮抗剂,对大鼠小肠 NK-2 受体的 Ki 值为 4.4 μM。
生物活性
Men 10376 TFA is a selective tachykinin NK-2 receptor antagonist, with a K i of 4.4 μM for rat small intestine NK-2 receptor.
性状
Solid
IC50 & Target[1][2]
Ki: 4.4 μM (NK-2 receptor, rat small intestine)
体外研究(In Vitro)
Men 10376 is a selective tachykinin NK-2 receptor, with a Ki of 4.4 μM, and shows low selectivity for NK-1 and NK-3 receptors (Ki, >10 μM). Men 10376 shows pA2s of 5.66 and 8.08 for NK-1 (guinea-pig ileum) and NK-2 receptors (endothelium-deprived rabbit pulmonary artery). Men 10376 shows no effect on NK-3 receptor (Ki, >10 μM). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Men 10376 (1 and 3 μmol/kg) antagonizes increase in bladder motility produced by the NK-2 receptor agonist in rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisture and lightPowder -80°C 2 years;-20°C 1 year
SequenceShortening
DY-{d-Trp}-V-{d-Trp}{d-Trp}-K-NH2
Sequence
Asp-Tyr-{d-Trp}-Val-{d-Trp}-{d-Trp}-Lys-NH2
参考文献
[1]. Quartara L, et al. N-terminal truncated analogs of men 10376 as tachykinin NK-2 receptor antagonists. Life Sci. 1992;51(25):1929-36.[2]. Maggi CA, et al. In vivo evidence for tachykininergic transmission using a new NK-2 receptor-selective antagonist, MEN 10,376. J Pharmacol Exp Ther. 1991 Jun;257(3):1172-8.
溶解度数据
In Vitro: H2O : 1.43 mg/mL (1.20 mM; Need ultrasonic)配制储备液