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346021 Sigma-AldrichGlucokinase Activator, Cpd A - CAS 603108-44-7 - Calbiochem

The Glucokinase Activator, Cpd A, also referenced under CAS 603108-44-7, modulates Glucokinase. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
分析证书
参考
Data Sheet

同义词: 2-Amino-5-(4-methyl-4H-(1,2,4)-triazole-3-yl-sulfanyl)-N-(4-methyl-thiazole-2-yl)benzamide, Compound A, Hexokinase D Activator, Hexokinase IV Activator

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
603108-44-7	C₁₄H₁₄N₆OS₂

价格及供货情况

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Description
Overview	A cell-permeable thiazolylamide glucokinase (GK; Hexokinase IV/D) activator that reversibly targets a allosteric site that is only exposed for binding in the glucose-bound GK conformation, but not in the unbound "super-open" GK conformation or the GKRP- (GK Regulatory Protein) bound GK, and effectively stabilizes GK in an active conformation as well as prevents its interaction with and nuclear sequestration by GKRP, while exhibiting little effect against Hexokinase I/II/III. Compound A is shown to activate GK activity in cell-free assays (EC₅₀ = 0.42 and 0.14 µM in the presence of 2.5 mM and 10 mM of glucose, respectively) and effectively induce cellular GK activation and increase glucose metabolism both in in rats (10 to 30 mg/kg, p.o.) in vivo and in rat islets and hepatocytes cultures (10 to 30 µM) in vitro.
Catalogue Number	346021
Brand Family	Calbiochem®
Synonyms	2-Amino-5-(4-methyl-4H-(1,2,4)-triazole-3-yl-sulfanyl)-N-(4-methyl-thiazole-2-yl)benzamide, Compound A, Hexokinase D Activator, Hexokinase IV Activator

References
References	Iino, T., et al. 2009. Bioorg. Med. Chem. Lett. 19, 5531. Mitsuya, M., et al. 2009. Bioorg. Med. Chem. Lett. 19, 2718. Nishimura, T., et al. 2009. Bioorg. Med. Chem. Lett. 19, In press. Futamura, M., et al. 2006. J. Biol. Chem. 281, 1357. Kamata, K., et al. 2004. Structure 12, 429.

Product Information
CAS number	603108-44-7
Form	Off-white solid
Hill Formula	C₁₄H₁₄N₆OS₂
Chemical formula	C₁₄H₁₄N₆OS₂
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Purity	≥95% by HPLC

Physicochemical Information

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information
S Phrase	S: 22-24/25-36 Do not breathe dust. Avoid contact with skin and eyes. Wear suitable protective clothing.

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Standard Handling
Storage	+2°C to +8°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
346021-5MGCN	04055977214628

Documentation

Glucokinase Activator, Cpd A - CAS 603108-44-7 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

Glucokinase Activator, Cpd A - CAS 603108-44-7 - Calbiochem 分析证书

标题	批号
346021	输入批号

参考

参考信息概述
Iino, T., et al. 2009. Bioorg. Med. Chem. Lett. 19, 5531. Mitsuya, M., et al. 2009. Bioorg. Med. Chem. Lett. 19, 2718. Nishimura, T., et al. 2009. Bioorg. Med. Chem. Lett. 19, In press. Futamura, M., et al. 2006. J. Biol. Chem. 281, 1357. Kamata, K., et al. 2004. Structure 12, 429.

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	08-April-2011 RFH
Synonyms	2-Amino-5-(4-methyl-4H-(1,2,4)-triazole-3-yl-sulfanyl)-N-(4-methyl-thiazole-2-yl)benzamide, Compound A, Hexokinase D Activator, Hexokinase IV Activator
Description	A cell-permeable thiazolylamide glucokinase (GK; Hexokinase IV/D) activator that reversibly targets a allosteric site that is only exposed for binding in the glucose-bound GK conformation, but not in the unbound "super-open" GK conformation or the GKRP- (GK Regulatory Protein) bound GK, and effectively stabilizes GK in an active conformation as well as prevents its interaction with and nuclear sequestration by GKRP, while exhibiting little effect against Hexokinase I/II/III. Compound A is shown to activate GK activity in cell-free assays (EC₅₀ = 0.42 and 0.14 µM in the presence of 2.5 mM and 10 mM of glucose, respectively) and effectively induce cellular GK activation and increase glucose metabolism both in in rats (10 to 30 mg/kg, p.o.) in vivo and in rat islets and hepatocytes cultures (10 to 30 µM) in vitro.
Form	Off-white solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	603108-44-7
Chemical formula	C₁₄H₁₄N₆OS₂
Structure formula
Purity	≥95% by HPLC
Solubility	DMSO (5 mg/ml)
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity	Standard Handling
References	Iino, T., et al. 2009. Bioorg. Med. Chem. Lett. 19, 5531. Mitsuya, M., et al. 2009. Bioorg. Med. Chem. Lett. 19, 2718. Nishimura, T., et al. 2009. Bioorg. Med. Chem. Lett. 19, In press. Futamura, M., et al. 2006. J. Biol. Chem. 281, 1357. Kamata, K., et al. 2004. Structure 12, 429.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Activators > Other Activators/Agonists

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