中文名称: | YM022 | ||||
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英文名称: | YM022 | ||||
别名: | YM022 YM-022;3-(3-methylphenyl)-1-[(3R)-1-[2-(2-methylphenyl)-2-oxoethyl]-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]urea | ||||
CAS No: | 145084-28-2 | 分子式: | C32H28N4O3 | 分子量: | 516.59 |
CAS No: | 145084-28-2 | ||||
分子式: | C32H28N4O3 | ||||
分子量: | 516.59 |
基本信息
产品编号:Y10035 |
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产品名称:YM022 |
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CAS: |
145084-28-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量: |
516.59 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
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Ethanol |
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Water |
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体内(现配现用) |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
1.9358mL |
9.6789mL |
19.3577mL |
5mM |
0.3872mL |
1.9358mL |
3.8715mL |
10mM |
0.1936mL |
0.9679mL |
1.9358mL |
生物活性
产品描述 |
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 68pM 和 63nM。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/IC50 |
CCR2 |
CCR1 63nM (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 IC50 value for [3H]devazepide binding of 136nM.YM022 inhibits the binding of [125I]CCK-8 to canine cloned gastrin/CCK-B receptor in a dose-dependent manner,with an IC50 value for [125I]CCK-8 binding of 0.73nM.Selectivity [ratio of (IC50 for gastrin/CCK-B receptor)/(IC50for CCK-A receptor)] of YM022 is 186. |
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体内研究 |
YM022 (intravenous injection;0.01-1μM/kg) dose-dependently inhibits pentagastrin-and peptone meal-induced acid secretion with ED50 values of 0.0261 and 0.0654μmol/kg,respectively,without affecting histamine- or methacholineinduced acid secretion.YM022 (subcutaneous injection;300μmol/kg;single dose) lowers the oxyntic mucosal HDC activity and raises the serum gastrin concentration in a dose-dependent manner (measured 24h after dosage).Maximum enzyme inhibition is achieved at a dose of 300μmol/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. |
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Animal Model: |
Rat |
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Dosage: |
300μmol/kg |
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Administration: |
Subcutaneous injection;300μmol/kg;single dose |
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Result: |
Suppressed the ECL cell activity for at least 4 as manifested in greatly reduced HDC activity, greatly elevated serum gastrin level. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )