CAS 870823-12-4|MK 0893

Introduction：Basic information about CAS 870823-12-4|MK 0893, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. MK 0893 BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	MK 0893
CAS Number	870823-12-4	Molecular Weight	588.481
Density	1.3±0.1 g/cm3	Boiling Point	814.0±65.0 °C at 760 mmHg
Molecular Formula	C₃₂H₂₇Cl₂N₃O₄	Melting Point	/
MSDS	/	Flash Point	446.1±34.3 °C

Names

Name	3-[[4-[(1S)-1-[3-(3,5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)pyrazol-1-yl]ethyl]benzoyl]amino]propanoic acid
Synonym	More Synonyms

MK 0893 BiologicalActivity

Description	MK 0893 is a potent, selective glucagon receptor antagonist with IC50 of 6.6 nM, and > 200 fold selectivity against GIPR, PAC1, GLP-1R, VPAC1 and VPAC2.
Related Catalog	Signaling Pathways >>GPCR/G Protein >>Glucagon ReceptorResearch Areas >>Metabolic Disease
Target	IC50: 6.6 nM (glucagon receptor)
In Vitro	MK 0893 is selective for glucagon receptor relative to other family B GPCRs, showing IC50 values of 1020 nM for GIPR, 9200 nM for PAC1, and >10000 nM for GLP-1R, VPAC1, and VPAC2. MK 0893 is active against the rhesus monkey GCGR, showing an IC50 of 56 nM in a cAMP assay with CHO cells expressing the rhesus GCGR[1].
In Vivo	MK 0893 blunts glucagon-induced glucose elevation in hGCGR mice and rhesus monkeys. It also lowers ambient glucose levels in both acute and chronic mouse models: in hGCGR ob/ob mice it reduces glucose (AUC 0-6 h) by 32% and 39% at 3 and 10 mpk single doses, respectively. In hGCGR mice on a high fat diet, MK 0893 at 3, and 10 mpk po in feed lowers blood glucose levels by 89% and 94% at day 10, respectively, relative to the difference between the vehicle control and lean hGCGR mice[1].
Cell Assay	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.
References	[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;

Chemical & Physical Properties

Density	1.3±0.1 g/cm3
Boiling Point	814.0±65.0 °C at 760 mmHg
Molecular Formula	C₃₂H₂₇Cl₂N₃O₄
Molecular Weight	588.481
Flash Point	446.1±34.3 °C
Exact Mass	587.137878
PSA	93.45000
LogP	6.97
Vapour Pressure	0.0±3.1 mmHg at 25°C
Index of Refraction	1.649
InChIKey	DNTVJEMGHBIUMW-IBGZPJMESA-N
SMILES	COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1

Synonyms

N-(4-{(1S)-1-[3-(3,5-Dichlorophenyl)-5-(6-methoxy-2-naphthyl)-1H-pyrazol-1-yl]ethyl}benzoyl)-β-alanine

cs-0324

mk 0893||mk-0893

β-Alanine, N-[4-[(1S)-1-[3-(3,5-dichlorophenyl)-5-(6-methoxy-2-naphthalenyl)-1H-pyrazol-1-yl]ethyl]benzoyl]-

mk-0893

MK 0893

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