MK 0893

目录号: HY-50663 纯度: 99.86%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

MK 0893 是一种有效，选择性的胰高血糖素受体拮抗剂，IC₅₀ 值为 6.6 nM。

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MK 0893 Chemical Structure

CAS No. : 870823-12-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥4078	In-stock
1 mg	￥1431	In-stock
5 mg	￥3150	In-stock
10 mg	￥5301	In-stock
50 mg		询价
100 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

MK 0893 is a potent and selective glucagon receptor antagonist with an IC₅₀ of 6.6 nM.

IC₅₀ & Target

IC50: 6.6 nM (glucagon receptor)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CHO	IC₅₀	> 10000 nM Compound: 9m, MK0893	Antagonist activity at human GLP1R expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at human GLP1R expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
CHO	IC₅₀	1019 nM Compound: 9m, MK0893	Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
CHO	IC₅₀	104.5 nM Compound: 9m, MK0893	Antagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
CHO	IC₅₀	122 nM Compound: 9m, MK0893	Antagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
CHO	IC₅₀	12800 nM Compound: 9m, MK0893	Antagonist activity at human VPAC2 expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at human VPAC2 expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
CHO	IC₅₀	15.7 nM Compound: 9m, MK0893	Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
CHO	IC₅₀	55.5 nM Compound: 9m, MK0893	Antagonist activity at rhesus monkey GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation count Antagonist activity at rhesus monkey GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation count	[PMID: 22708876]
CHO	IC₅₀	6.6 nM Compound: 9m, MK0893	Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay	[PMID: 22708876]
CHO	IC₅₀	727 nM Compound: 9m, MK0893	Antagonist activity at rat GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at rat GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
HT-29	IC₅₀	11580 nM Compound: 9m, MK0893	Antagonist activity at human VPAC1 expressed in HT-29 cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at human VPAC1 expressed in HT-29 cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
NIH3T3	IC₅₀	9200 nM Compound: 9m, MK0893	Antagonist activity at human PAC1 expressed in mouse HIN 3T3 cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation cou Antagonist activity at human PAC1 expressed in mouse HIN 3T3 cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation cou	[PMID: 22708876]

体外研究
(In Vitro)

MK 0893对胰高血糖素受体具有选择性，对GIPR的 IC₅₀值为1020 nM，对PAC1的 IC₅₀为9200 nM，对GLP-1R、VPAC1和VPAC2的 IC₅₀ >10000 nM。MK 0893对恒河猴GCGR有活性，在表达恒河猴GCGR 的CHO细胞的cAMP实验中显示IC₅₀为56 nM ^[1]。

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

体内研究
(In Vivo)

MK 0893 在 hGCGR 小鼠和恒河猴中减弱胰高血糖素诱导的葡萄糖升高。它还降低急性和慢性小鼠模型中的环境葡萄糖水平：在 hGCGR ob/ob 小鼠中，它在 3 和 10 mpk 单剂量下分别将葡萄糖 (AUC 0-6 h) 降低 32% 和 39%。在高脂肪饮食的 hGCGR 小鼠中，相对于载体对照和瘦 hGCGR 小鼠之间的差异，饲料中 3 和 10 mpk po 的 MK 0893 在第 10 天分别降低了 89% 和 94% 的血糖水平^[1]。

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

Clinical Trial

分子量

588.48

Formula

C₃₂H₂₇Cl₂N₃O₄

CAS 号

870823-12-4

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 33.33 mg/mL (56.64 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6993 mL	8.4965 mL	16.9929 mL
5 mM	0.3399 mL	1.6993 mL	3.3986 mL
10 mM	0.1699 mL	0.8496 mL	1.6993 mL

查看完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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

方案一

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.25 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
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。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.86%

选择批次：

Data Sheet (638 KB) SDS (251 KB)

COA (198 KB) LCMS (93 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Xiong Y, et al. Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes.J Med Chem. 2012 Jul 12; [Content Brief]

Cell Assay ^[1]	CHO hGCGR cells are grown in Iscove's Modified Dulbecco’s Medium (IMDM), 10% FBS, 1 mM l-glutamine, penicillin-streptomycin (100 μ/mL), and 500μg G418/mL for 3-4 days before harvesting using Enzyme-Free Dissociation Media (EFDM). The cells are centrifuged at low speed and resuspended in stimulation buffer. Compounds are diluted from DMSO stocks and added to the assay at a final concentration of 5% DMSO. Cells are preincubated with compound or DMSO controls for 30 min. Glucagon (250 pM) is added, and the samples are incubated at room temperature for an additional 30 min. The assay is terminated with the addition of the FlashPlate kit detection buffer. The assay is then incubated for an additional 3 h at room temperature, and bound radioactivity is measured using a liquid scintillation counter. cAMP levels are determined as per manufacturer’s instructions. For Schild Plot analysis, aliquots of cells are preincubated with 56, 100, 178, 300, 560, and 1000 nM 9m for 30 min at room temperature prior to the addition of 0.001-1000 nM glucagon to initiate the assay. Data are analyzed using the linear and nonlinear regression analysis software GraphPad Prism, v4. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Xiong Y, et al. Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes.J Med Chem. 2012 Jul 12; [Content Brief]

Cell Assay
^[1]

CHO hGCGR cells are grown in Iscove's Modified Dulbecco’s Medium (IMDM), 10% FBS, 1 mM l-glutamine, penicillin-streptomycin (100 μ/mL), and 500μg G418/mL for 3-4 days before harvesting using Enzyme-Free Dissociation Media (EFDM). The cells are centrifuged at low speed and resuspended in stimulation buffer. Compounds are diluted from DMSO stocks and added to the assay at a final concentration of 5% DMSO. Cells are preincubated with compound or DMSO controls for 30 min. Glucagon (250 pM) is added, and the samples are incubated at room temperature for an additional 30 min. The assay is terminated with the addition of the FlashPlate kit detection buffer. The assay is then incubated for an additional 3 h at room temperature, and bound radioactivity is measured using a liquid scintillation counter. cAMP levels are determined as per manufacturer’s instructions. For Schild Plot analysis, aliquots of cells are preincubated with 56, 100, 178, 300, 560, and 1000 nM 9m for 30 min at room temperature prior to the addition of 0.001-1000 nM glucagon to initiate the assay. Data are analyzed using the linear and nonlinear regression analysis software GraphPad Prism, v4.

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

参考文献

[1]. Xiong Y, et al. Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes.J Med Chem. 2012 Jul 12; [Content Brief]

MK 0893 相关分类

Metabolic Disease

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6993 mL	8.4965 mL	16.9929 mL	42.4823 mL
	5 mM	0.3399 mL	1.6993 mL	3.3986 mL	8.4965 mL
	10 mM	0.1699 mL	0.8496 mL	1.6993 mL	4.2482 mL
	15 mM	0.1133 mL	0.5664 mL	1.1329 mL	2.8322 mL
	20 mM	0.0850 mL	0.4248 mL	0.8496 mL	2.1241 mL
	25 mM	0.0680 mL	0.3399 mL	0.6797 mL	1.6993 mL
	30 mM	0.0566 mL	0.2832 mL	0.5664 mL	1.4161 mL
	40 mM	0.0425 mL	0.2124 mL	0.4248 mL	1.0621 mL
	50 mM	0.0340 mL	0.1699 mL	0.3399 mL	0.8496 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MK 0893870823-12-4MK0893MK-0893GCGRGlucagon ReceptorInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

MK 0893

Customer Review

MCE 顾客使用本产品发表的 5 篇科研文献