MK-3577

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C30H30ClFN2O3
Molecular Weight	521.022
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CCC[C@@H]([C@@H](C1=CNC2=C(F)C=C(C)C=C12)C3=CC=C(Cl)C=C3)C4=CC=C(C=C4)C(=O)NCCC(O)=O

InChI

InChIKey=FYRJJCYFYLLOSC-LXFBAYGMSA-N

InChI=1S/C30H30ClFN2O3/c1-3-4-23(19-5-7-21(8-6-19)30(37)33-14-13-27(35)36)28(20-9-11-22(31)12-10-20)25-17-34-29-24(25)15-18(2)16-26(29)32/h5-12,15-17,23,28,34H,3-4,13-14H2,1-2H3,(H,33,37)(H,35,36)/t23-,28+/m1/s1

HIDE SMILES / InChI

Molecular Formula	C30H30ClFN2O3
Molecular Weight	521.022
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description

MK 3577 is an orally active glucagon receptor antagonist which was under development by Merck & Co for the treatment of type 2 diabetes mellitus. MK 3577 demonstrate activity in cellular models and preclinical trials. In phase II clinical trials MK 3577 shows good efficacy and acceptable level of adverse events, but no further development reports were published.

Originator

Approval Year

PubMed

Show entries

Title	Date	PubMed
A semi-mechanistic model for the effects of a novel glucagon receptor antagonist on glucagon and the interaction between glucose, glucagon, and insulin applied to adaptive phase II design.	2014 Nov	25160589

Showing 1 to 1 of 1 entries

Previous1Next

Patents

Sample Use Guides

In Vivo Use Guide

MK-3577 oral tablets totaling 6 mg in the evening (PM), 10 mg in the morning (AM), or 25 mg twice daily (BID) depending upon randomization, administered during a 4 week treatment period.

Route of Administration: Oral

Substance Class	Chemical
Record UNII	03TW1410NL
Record Status	`Validated (UNII)`
Record Version

Show entries

Name

Type

Language

MK-3577

Common Name

English

.BETA.-ALANINE, N-(4-((1S)-1-((R)-(4-CHLOROPHENYL)(7-FLUORO-5-METHYL-1H-INDOL-3-YL)METHYL)BUTYL)BENZOYL)-

Systematic Name

English

N-(4-((1S)-1-((R)-(4-CHLOROPHENYL)(7-FLUORO-5-METHYL-1H-INDOL-3-YL)METHYL)BUTYL)BENZOYL)-.BETA.-ALANINE

Systematic Name

English

N-(4-((1S)-1-((R)-(4-CHLOROPHENYL)(7-FLUORO-5-METHYL-1H-INDOL-3-YL)METHYL)BUTYL)BENZOYL)-.BETA.-ALANINE, (-)-

Systematic Name

English

Showing 1 to 4 of 4 entries

Previous1Next

Show entries

Code System

Code

Type

Description

PUBCHEM

46240797

PRIMARY

DRUG BANK

DB14957

PRIMARY

FDA UNII

03TW1410NL

PRIMARY

CAS

1019112-29-8

PRIMARY

Showing 1 to 4 of 4 entries

Previous1Next

Show entries

Related Record

Type

Details


					G2BWF9H576

GLUCAGON RECEPTOR

TARGET -> INHIBITOR

Comments:

More complete GCGr blockade led to better glycemic control, but also LDL-C increases, whereas partial GCGr blockade led to smaller effects on glycemic control and LDL-C.

Showing 1 to 1 of 1 entries

Previous1Next

Show entries

Related Record

Type

Details


					03TW1410NL

MK-3577

ACTIVE MOIETY

Comments:

Purpose: This study will assess the safety and efficacy of MK3577 when given in the morning, the evening, or twice a day as compared to placebo and to metformin.


					03TW1410NL

MK-3577

ACTIVE MOIETY

Comments:

Originator: Merck & Co; Class: Anti-hyper-glycaemic; Mechanism of Action: Glucagon receptor antagonist; Orphan Drug Status: No; On Fast track: No; New Molecular Entity: Yes; Highest Development Phase: Discontinued for Type 2 diabetes mellitus; Most Recent Event: 08 Mar 2010 MK 3577 is still in phase II development

Showing 1 to 2 of 2 entries

Previous1Next