135306-85-3
中文名稱
(TYR5,D-TRP6·8·9,LYS-NH210)-NEUROKININ A (4-10)
英文名稱
H-ASP-TYR-D-TRP-VAL-D-TRP-D-TRP-LYS-NH2
CAS
135306-85-3
分子式
C57H68N12O10
分子量
1081.22
MOL 文件
135306-85-3.mol
135306-85-3 結(jié)構(gòu)式
基本信息
中文別名
MEN 10376肽 英文別名
MEN 10376MEN-10,376 ≥95%
MEN-10,376, ≥95% (HPLC)
MEN-10,376 , ≥95% (HPLC)
M.W. 1081.24 C57H68N12O10
Neurokinin-2 receptor antagonist
ASP-TYR-D-TRP-VAL-D-TRP-D-TRP-LYS-NH2
H-ASP-TYR-D-TRP-VAL-D-TRP-D-TRP-LYS-NH2
tyr(5)-trp(6,8,9)-lys(10)-neurokinina(4-10
[TYR5, D-TRP6,8,9, LYS10]NEUROKININ A (4-10)
物理化學性質(zhì)
沸點1555.4±65.0 °C(Predicted)
密度1.361±0.06 g/cm3(Predicted)
儲存條件-20°C
溶解度Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
酸度系數(shù)(pKa)3.71±0.10(Predicted)
形態(tài)solid
顏色white
序列Asp-Tyr-{d-Trp}-Val-{d-Trp}-{d-Trp}-Lys-NH2
InChIKeyQQHOFZNACVKNHK-UHFFFAOYSA-N
SMILESCC(C)C(NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)C(Cc3ccc(O)cc3)NC(=O)C(N)CC(O)=O)C(=O)NC(Cc4c[nH]c5ccccc45)C(=O)NC(Cc6c[nH]c7ccccc67)C(=O)NC(CCCCN)C(N)=O
常見問題列表
生物活性
Men 10376 是一種有效的選擇性的 tachykinin NK-2 受體拮抗劑，對大鼠小腸 NK-2 受體的 Ki 值為 4.4 μM。靶點
Ki: 4.4 μM (NK-2 receptor, rat small intestine)
體外研究
Men 10376 is a selective tachykinin NK-2 receptor, with a K i of 4.4 μM, and shows low selectivity for NK-1 and NK-3 receptors (K i , >10 μM). Men 10376 shows pA 2 s 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 (K i , >10 μM).
體內(nèi)研究
Men 10376 (1 and 3 μmol/kg) antagonizes increase in bladder motility produced by the NK-2 receptor agonist in rats.