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YM 022

CCK2沉默拮抗剂,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

目录号: PC11150 纯度: ≥98%

CAS No. :145084-28-2

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中文名称

YM 022

英文名称

YM 022

英文别名

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,N-[(3R)-2,3-dihydro-1-[2-(2-methylphenyl)-2-oxoethyl]-2-oxo-5-phenyl-1H-1,4-benzodiazepin...;YM 022;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;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;(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 No.

145084-28-2

分子式

C₃₂H₂₈N₄O₃

分子量

516.59

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the K_i values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo.

性状

Solid

IC50 & Target[1][2]

CCR2

68 pM (Ki)

CCR1

63 nM (Ki)

体外研究(In Vitro)

YM022 inhibits binding to canine pancreas CCK-A receptor in a dose-dependent manner, with an IC₅₀ value for [H]devazepide binding of 136 nM.
YM022 inhibits the binding of [I]CCK-8 to canine cloned gastrin/CCK-B receptor in a dose-dependent manner, with an IC₅₀ value for [I]CCK-8 binding of 0.73 nM.
Selectivity [ratio of (IC₅₀ for gastrin/CCK-B receptor)/(IC₅₀for CCK-A receptor)] of YM022 is 186.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

YM022 (intravenous injection; 0.01-1 μM/kg) dose-dependently inhibits pentagastrin- and peptone meal-induced acid secretion with ED₅₀ 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Nishida A, et al. Pharmacological profile of (R)-1-[2,3-dihydro-1-(2-methylphenacyl)-2-oxo- 5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, 体外研究 and in vivo [Information]

[2]. Kitano M, et al. Long-lasting cholecystokinin(2) receptor blockade after a single subcutaneous injection of YF476 or YM022.Br J Pharmacol. 2000 Jun;130(3):699-705. [Information]

[3]. Beinborn M, et al. Small synthetic ligands of the cholecystokinin-B/gastrin receptor can mimic the function of endogenous peptide hormones.Yale J Biol Med. 1998 May-Aug;71(3-4):337-46. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (193.58 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9358 mL	9.6789 mL	19.3577 mL
5 mM	0.3872 mL	1.9358 mL	3.8715 mL
10 mM	0.1936 mL	0.9679 mL	1.9358 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.84 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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