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(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
(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
英文别名:
YM 022;YM022,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)-
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
中文别名:
化合物 T17274
CBNumber:
CB5302859
分子式:
C32H28N4O3
分子量:
516.59
MOL File:
145084-28-2.mol

(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化学性质

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)
安全信息
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 Germany: 3

(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。

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.

(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 上下游产品信息

上游原料

下游产品

(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 试剂级价格

更新日期产品编号产品名称CAS编号包装价格
2024/04/30HY-103355YM0221 mg1590元
2024/04/30HY-103355(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
145084-28-25mg3500元

(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 生产厂家

供应商联系电话电子邮件国家产品数优势度
武汉易泰科技有限公司上海分公司 821-50328103-801 18930552037 3bsc@sina.com 中国 15848 69
Sigma-Aldrich西格玛奥德里奇(上海)贸易有限公司 021-61415566 800-8193336 orderCN@merckgroup.com 中国 51471 80
EMMX Biotechnology LLC 888-539-0666 info@emmx.com 美国 8449 60
TargetMol Chemicals Inc. +1-781-999-5354 +1-00000000000 marketing@targetmol.com 美国 19892 58
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济南思考化学有限公司 0531-0000 thinklifescience@163.com 中国 19690 58
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成都超九八生物科技有限公司 13348960310 13348960310 3003867561@qq.com 中国 10011 58
天津普西唐生物医药科技有限公司 010-60605840 psaitong@jm-bio.com 中国 29778 58
上海优宁维生物科技股份有限公司 18768175414 gaojun@univ-bio.com 中国 24998 58
TargetMol中国(陶术生物) 4008200310 marketing@tsbiochem.com 中国 24017 58
上海立崎生物医学研究中心 18014399201 sales@chemlab-tachizaki.com 中国 2494 58
上海陌孚医药科技有限公司 021-59167510 18117107507 vip@med-life.cn 中国 5019 58
Aladdin Scientific +1-+1(833)-552-7181 sales@aladdinsci.com 美国 52927 58
ApexBio技术 sales@apexbt.com 美国 6254 58
 

145084-28-2, (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 相关搜索:

  • Cholecystokinin (CCK) receptor
  • C32H28N4O3
  • 化合物 T17274
  • 145084-28-2
  • YM022,YM-022
  • YM 022 >=98% (HPLC)
  • 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)-
  • 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
  • YM 022
  • (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
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