145084-28-2

中文名称 (R)-N-[2,3-DIHYDRO-1-[2-(2-METHYLPHENYL)-2-OXOETHYL]-2-OXO-5-PHENYL-1H-1,4-BENZODIAZEPIN-3-YL]-N'-(3-METHYLPHENYL)-UREA

英文名称 (R)-N-[2,3-DIHYDRO-1-[2-(2-METHYLPHENYL)-2-OXOETHYL]-2-OXO-5-PHENYL-1H-1,4-BENZODIAZEPIN-3-YL]-N'-(3-METHYLPHENYL)-UREA

CAS 145084-28-2

分子式 C32H28N4O3

分子量 516.59

MOL 文件 145084-28-2.mol

145084-28-2 结构式

基本信息物理化学性质安全数据 (R)-N-[2,3-DIHYDRO-1-[2-(2-METHYLPHENYL)-2-OXOETHYL]-2-OXO-5-PHENYL-1H-1,4-BENZODIAZEPIN-3-YL]-N'-(3-METHYLPHENYL)-UREA价格(试剂级) 常见问题列表

基本信息

中文别名

化合物 T17274

英文别名

YM 022
YM 022 >=98% (HPLC)
(R)-N-(2,3-Dihydro-1-(2-(2-methylphenyl)-2-oxoethyl)-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl)-N'-(3-methylphenyl)urea
(R)-N-[2,3-DIHYDRO-1-[2-(2-METHYLPHENYL)-2-OXOETHYL]-2-OXO-5-PHENYL-1H-1,4-BENZODIAZEPIN-3-YL]-N'-(3-METHYLPHENYL)-UREA
N-[(3R)-2,3-Dihydro-1-[2-(2-methylphenyl)-2-oxoethyl]-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N′-(3-methylphenyl)-urea
Urea, N-[(3R)-2,3-dihydro-1-[2-(2-methylphenyl)-2-oxoethyl]-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)-

物理化学性质

储存条件Store at RT

溶解度DMSO：可溶，5mg/mL（澄清溶液）

形态粉末

颜色白色至米色

旋光性 (optical activity)[α]/D -128 to -140 (c = 1, DCM)

安全数据

危险性符号(GHS)

GHS06

警示词危险

危险性描述H301

防范说明P301+P310

危险品标志T

危险类别码25

安全说明45

危险品运输编号UN 2811 6.1 / PGIII

WGK Germany3

常见问题列表

生物活性

YM022 是一种高效，选择性和口服活性胃泌素/胆囊收缩素(CCK)-B 受体 (CCK-BR) 拮抗剂。 YM022 显示CCK-B 和 CCK-A 受体的 Ki 值分别为 68 pM 和 63 nM。 YM022 在体内可以抑制胃泌素诱导的胃酸分泌和组氨酸脱羧酶的活化。

靶点

CCR1

68 pM (Ki)

CCR2

63 nM (Ki)

体外研究

YM022 inhibits binding to canine pancreas CCK-A receptor in a dose-dependent manner, with an IC ₅₀ value for [ ³ H]devazepide binding of 136 nM.
YM022 inhibits the binding of [ ¹²⁵ I]CCK-8 to canine cloned gastrin/CCK-B receptor in a dose-dependent manner, with an IC ₅₀ value for [ ¹²⁵ I]CCK-8 binding of 0.73 nM.
Selectivity [ratio of (IC ₅₀ for gastrin/CCK-B receptor)/(IC ₅₀ for CCK-A receptor)] of YM022 is 186.

体内研究

YM022 (intravenous injection; 0.01-1 μM/kg) dose-dependently inhibits pentagastrin- and peptone meal-induced acid secretion with ED ₅₀ values of 0.0261 and 0.0654 μmol/kg, respectively, without affecting histamine- or methacholine-induced acid secretion.
YM022 (subcutaneous injection; 300 μmol/kg; single dose) lowers the oxyntic mucosal HDC activity and raises the serum gastrin concentration in a dose-dependent manner (measured 24 h after dosage). Maximum enzyme inhibition is achieved at a dose of 300 μmol/kg for YM022 and the inhibition of HDC lasts for 4 weeks. At sacrifice, drug residues can be seen at the injection site for as long as 4 (YM022) weeks after injection in rat.
YM022 is suspended in 2% Methocel for oral ingestion and in PEG300 for subcutaneous injection.

Animal Model:	Rat
Dosage:	300 μmol/kg
Administration:	Subcutaneous injection; 300 μmol/kg; single dose
Result:	Suppressed the ECL cell activity for at least 4 as manifested in greatly reduced HDC activity, greatly elevated serum gastrin level.