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Cantharidic Acid (sodium salt) Sale

目录号 : GC12082

A protein phosphatase inhibitor

Cantharidic Acid (sodium salt) Chemical Structure

Cas No.:1465-77-6

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5mg
¥619.00
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10mg
¥967.00
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25mg
¥2,253.00
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50mg
¥3,918.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

Cantharidic acid, an inhibitor of protein phosphatases, is first isolated from Chinese blister beetles. Cantharidic acid is a hydrolysis product of cantharidin.

Protein phosphatases, account for virtually all of the phosphatase activity toward phosphoproteins, have been involved in controlling glycogen metabolism, glycolysis, gluconeogenesis, fatty acid synthesis, cholesterol synthesis, and protein synthesis. Protein phosphatases participate in protein phosphorylation, a principal regulatory mechanism in the control of almost all cellular processes [2].

In vitro: Cantharidic acid exihibited inhibitory effects on the protein phosphatases PP1 and PP2A with IC50 values of 0.6 and 0.05 μM, respectively. Cantharidic acid showed no effect on the activity of PP2B or PP2C [1].

In vivo: Intraperitoneal administration of cantharidic acid (10 mg/kg) to mice for 45 min caused extreme liver enlargement and congestion. Treatment with cantharidic acid increased hepatic glycogenolysis, elevated blood glucose and hepatic glycogen phosphorylase levels, reduced hepatic glycogen content and glycogen synthase activity. Cantharidic acid endothal decreased microsomal Mg2+-ATPase levels [3].

References:
[1] McCluskey A, Sim A T R, Sakoff J A.  Serine threonine protein phosphatase inhibitors: Development of potential therapeutic strategies[J]. Journal of medicinal chemistry, 2002, 45(6): 1151-1175.
[2] Ingebritsen T S, Cohen P.  Protein phosphatases: properties and role in cellular regulation[J]. Science, 1983, 221(4608): 331-338.
[3] Graziano M J, Casida J E.  Comparison of the acute toxicity of endothal and cantharidic acid on mouse liver in vivo[J]. Toxicology letters, 1987, 37(2): 143-148.

Chemical Properties

Cas No. 1465-77-6 SDF
化学名 (1R,2S,3R,4S)-rel-2,3-dimethyl-7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic acid, disodium salt
Canonical SMILES OC([C@@]1(C)[C@](C(O)=O)(C)[C@@H]2CC[C@H]1O2)=O.[Na+].[Na+]
分子式 C10H12O5 • 2Na 分子量 258.2
溶解度 ≤2mg/ml in PBS(pH7.2) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.873 mL 19.3648 mL 38.7297 mL
5 mM 0.7746 mL 3.873 mL 7.7459 mL
10 mM 0.3873 mL 1.9365 mL 3.873 mL
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