346021
Glucokinase Activator, Cpd A
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.
동의어(들):
Glucokinase Activator, Cpd A, Hexokinase D Activator, Hexokinase IV Activator, 2-Amino-5-(4-methyl-4H-(1,2,4)-triazole-3-yl-sulfanyl)-N-(4-methyl-thiazole-2-yl)benzamide, Compound A
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C14H14N6OS2
CAS Number:
Molecular Weight:
346.43
UNSPSC 코드:
41121706
NACRES:
NA.77
추천 제품
Quality Level
분석
≥95% (HPLC)
형태
solid
제조업체/상표
Calbiochem®
저장 조건
OK to freeze
protect from light
색상
off-white
solubility
DMSO: 5 mg/mL
배송 상태
ambient
저장 온도
2-8°C
일반 설명
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.
포장
Packaged under inert gas
경고
Toxicity: Standard Handling (A)
재구성
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
기타 정보
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. Structure12, 429.
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. Structure12, 429.
법적 정보
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 1
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
Ryota Inoue et al.
iScience, 25(7), 104603-104603 (2022-07-09)
Uncoupling protein 2 (UCP2), a mitochondrial protein, is known to be upregulated in pancreatic islets of patients with type 2 diabetes (T2DM); however, the pathological significance of this increase in UCP2 expression is unclear. In this study, we highlight the
Sophie L Lewandowski et al.
Cell metabolism, 32(5), 736-750 (2020-11-05)
Pancreatic β cells couple nutrient metabolism with appropriate insulin secretion. Here, we show that pyruvate kinase (PK), which converts ADP and phosphoenolpyruvate (PEP) into ATP and pyruvate, underlies β cell sensing of both glycolytic and mitochondrial fuels. Plasma membrane-localized PK
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