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145084-28-2

中文名稱 (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
英文名稱 (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 結(jié)構(gòu)式 145084-28-2 結(jié)構(gòu)式

基本信息

中文別名
化合物 T17274
英文別名
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)-

物理化學(xué)性質(zhì)

儲存條件Store at RT
溶解度DMSO:可溶,5mg/mL(澄清溶液)
形態(tài)粉末
顏色白色至米色
旋光性 (optical activity)[α]/D -128 to -140 (c = 1, DCM)

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS06
警示詞危險
危險性描述H301
防范說明P301+P310
危險品標(biāo)志T
危險類別碼25
安全說明45
危險品運輸編號UN 2811 6.1 / PGIII
WGK Germany3

常見問題列表

生物活性
YM022 是一種高效,選擇性和口服活性胃泌素/膽囊收縮素(CCK)-B 受體 (CCK-BR) 拮抗劑。 YM022 顯示CCK-B 和 CCK-A 受體的 Ki 值分別為 68 pM 和 63 nM。 YM022 在體內(nèi)可以抑制胃泌素誘導(dǎo)的胃酸分泌和組氨酸脫羧酶的活化。
靶點

CCR1

68 pM (Ki)

CCR2

63 nM (Ki)

體外研究

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.

體內(nèi)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.
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