(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号:145084-28-2
- 英文名:(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
- 中文名:(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
- CBNumber:CB5302859
- 分子式:C32H28N4O3
- 分子量:516.59
- MOL File:145084-28-2.mol
- 熔点 :187-190 °C
- 沸点 :735.4±60.0 °C(Predicted)
- 密度 :1.23±0.1 g/cm3(Predicted)
- 储存条件 :Store at RT
- 溶解度 :DMSO: soluble5mg/mL (clear solution)
- 形态 :powder
- 酸度系数(pKa) :11.61±0.40(Predicted)
- 颜色 :white to beige
- 旋光性 (optical activity) :[α]/D -128 to -140 (c = 1, DCM)
(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性质、用途与生产工艺
- 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。
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靶点
CCR1
68 pM (Ki)
CCR2
63 nM (Ki)
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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.
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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.
- 更新日期:2024/11/08
- 产品编号:HY-103355
- 产品名称:YM022
- CAS编号:
- 包装:1 mg
- 价格:1590元
- 更新日期:2024/11/08
- 产品编号:HY-103355
- 产品名称:(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 YM022
- CAS编号:145084-28-2
- 包装:5mg
- 价格:3500元
- 公司名称:Service Chemical Inc.
- 联系电话:--
- 电子邮件:sales@chemos-group.com
- 国家:德国
- 产品数:6350
- 优势度:71
- 公司名称:BIOTREND Chemicals AG
- 联系电话:--
- 电子邮件:info@biotrend.ch
- 国家:德国
- 产品数:1250
- 优势度:62