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.
别名:
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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About This Item
推荐产品
品質等級
化驗
≥95% (HPLC)
形狀
solid
製造商／商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
off-white
溶解度
DMSO: 5 mg/mL
運輸包裝
ambient
儲存溫度
2-8°C
一般說明
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.
包裝
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重構
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他說明
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.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 1
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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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