| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
PKCε
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|---|---|
| ln Vitro |
Epsilon-V1-2 (ε-V1-2), a peptide generated from PKCε that has its particular receptor for activated C kinase (RACK) sited therein, inhibits PKCε translocation and decreases the insulin response to glucose[1]. Cardiomyocytes treated with Epsilon-V1 -2 (ε-V1-2; 1 µM, 24 hours) show considerable inhibition of Oleic acid (OA)-induced connexin 43 (Cx43) Ser368 phosphorylation and prevention of OA-induced gap junction disassembly[2].
|
| ln Vivo |
In a mouse heterotopic transplantation paradigm, Epsilon-V1-2 (20 mg/kg/day; osmotic pumps; daily; for 4 weeks) therapy dramatically increases the beating score. Epsilon-V1-2 lessens parenchymal fibrosis and the infiltration of T lymphocytes and macrophages into cardiac grafts. The increase in pro-fibrotic cytokine TGF-β and monocyte recruitment chemokine MCP-1 levels is nearly completely eliminated by epsilon-V1-2 treatment[3].
|
| Animal Protocol |
Animal/Disease Models: C57BL/6J mice transplanted the hearts of FVB mice[3]
Doses: 20 mg/kg/day Route of Administration: 0.1 mL osmotic pumps implanted subcutaneously (sc); daily; for 4 weeks Experimental Results: Dramatically improved the beating score throughout the treatment. |
| References |
[1]. M Yedovitzky, et al. Translocation inhibitors define specificity of protein kinase C isoenzymes in pancreatic beta-cells. J Biol Chem. 1997 Jan 17;272(3):1417-20.
[2]. Yuahn-Sieh Huang, et al. Mechanism of oleic acid-induced gap junctional disassembly in rat cardiomyocytes. J Mol Cell Cardiol. 2004 Sep;37(3):755-66. [3]. Tomoyoshi Koyanagi, et al. Pharmacological inhibition of epsilon PKC suppresses chronic inflammation in murine cardiac transplantation model. J Mol Cell Cardiol. 2007 Oct;43(4):517-22. |
| Molecular Formula |
C37H65N9O13
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|---|---|
| Molecular Weight |
843.96
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| CAS # |
182683-50-7
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| SMILES |
O=C([C@H](CCCCN)NC([C@H](CC(C)C)NC([C@H](CO)NC([C@H](C(C)C)NC([C@H](C)NC([C@H](CCC(=O)O)N)=O)=O)=O)=O)=O)N1CCC[C@H]1C(N[C@H](C(=O)O)[C@@H](C)O)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : 50 mg/mL (59.24 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (118.49 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1849 mL | 5.9245 mL | 11.8489 mL | |
| 5 mM | 0.2370 mL | 1.1849 mL | 2.3698 mL | |
| 10 mM | 0.1185 mL | 0.5924 mL | 1.1849 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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