MB-05032

Details

Stereochemistry	ACHIRAL
Molecular Formula	C11H15N2O4PS
Molecular Weight	302.287
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)CC1=C(N=C(N)S1)C2=CC=C(O2)P(O)(O)=O

InChI

InChIKey=XJMYIJPPDSZOPN-UHFFFAOYSA-N

InChI=1S/C11H15N2O4PS/c1-6(2)5-8-10(13-11(12)19-8)7-3-4-9(17-7)18(14,15)16/h3-4,6H,5H2,1-2H3,(H2,12,13)(H2,14,15,16)

HIDE SMILES / InChI

Molecular Formula	C11H15N2O4PS
Molecular Weight	302.287
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Approval Year

Substance Class	Chemical Created by `admin` on `Sat Dec 16 18:33:25 UTC 2023` Edited by `admin` on `Sat Dec 16 18:33:25 UTC 2023`
Record UNII	9379MH4CAL
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

MB-05032

Code

English

(5-(2-AMINO-5-ISOBUTYL-1,3-THIAZOL-4-YL)-2-FURYL)PHOSPHONIC ACID

Systematic Name

English

2-AMINO-5-ISOBUTYL-4-(5-PHOSPHONO-2-FURANYL)THIAZOLE

Systematic Name

English

P-(5-(2-AMINO-5-(2-METHYLPROPYL)-4-THIAZOLYL)-2-FURANYL)PHOSPHONIC ACID

Systematic Name

English

PHOSPHONIC ACID, (5-(2-AMINO-5-(2-METHYLPROPYL)-4-THIAZOLYL)-2-FURANYL)-

Systematic Name

English

MB05032

Code

English

Code System Code Type Description

PUBCHEM

11289630

Created by admin on Sat Dec 16 18:33:26 UTC 2023 , Edited by admin on Sat Dec 16 18:33:26 UTC 2023

PRIMARY

FDA UNII

9379MH4CAL

Created by admin on Sat Dec 16 18:33:26 UTC 2023 , Edited by admin on Sat Dec 16 18:33:26 UTC 2023

PRIMARY

CAS

261365-11-1

Created by admin on Sat Dec 16 18:33:26 UTC 2023 , Edited by admin on Sat Dec 16 18:33:26 UTC 2023

PRIMARY

MANUFACTURER PRODUCT INFORMATION

MB-05032

Created by admin on Sat Dec 16 18:33:26 UTC 2023 , Edited by admin on Sat Dec 16 18:33:26 UTC 2023

PRIMARY

Description: IC50 Value: 16 nM (Human Liver FBPase) (1) MB05032 is a special and efficacious GNG inhibitor targeted the AMP binding site of fructose 1,6-bisphosphatase (FBPase) with an IC50 value of 16 nM. Oral delivery of MB05032 was achieved by using the bisamidate prodrug MB06322 (CS-917), which is converted to MB05032 in two steps through the action of an esterase and a phosphoramidase. in vitro: MB05032 inhibits human liver FBPase with a potency (IC50 = 16 +/- 1.5 nM) significantly greater than the natural inhibitor, AMP (IC50 = 1 .MU.M), and the most well characterized AMP mimetic, ZMP (IC50 = 12 +/- 1.4 .MU.M). MB05032 inhibits rat FBPase 3-fold weaker (IC50 of 61 +/- 4 nM) than human FBPase, whereas AMP is 20-fold weaker as an inhibitor.

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					3W93F83K7S

MANAGLINAT DIALANETIL

PRODRUG -> METABOLITE ACTIVE

Amount:

Related Record Type Details


					9379MH4CAL

MB-05032

ACTIVE MOIETY

Comments:

Class: Amino acid, Anti-hyperglycaemic, Organo-phosphorus compound and Small molecule; Mechanism of Action: Fructose bisphosphatase inhibitor and Gluconeogenesis inhibitor; Highest Development Phase: Discontinued Type 2 diabetes mellitus; Most Recent Events: 29 Jun 2007 Data presented at the 67th Scientific Sessions of the American Diabetes Association (ADA-2007), added to the Diabetes pharmacodynamics section, 26 Jun 2007 Daiichi Sankyo completes a phase IIb trial in Diabetes in the US