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ESI-08

Katalog-Nr.GC66473 Copy One-Click Copy Product Info

ESI-08 ist ein potenter und selektiver EPAC-Antagonist, der sowohl die EPAC1- als auch die EPAC2-AktivitÄt (IC50 von 8,4 μ M) vollstÄndig hemmen kann. ESI-08 blockiert selektiv die cAMP-induzierte EPAC-Aktivierung, hemmt jedoch nicht die cAMP-vermittelte PKA-Aktivierung.

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ESI-08 Chemische Struktur

Cas No.: 301177-43-5

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5mg
122,00 $
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10mg
203,00 $
Auf Lager
25mg
445,00 $
Auf Lager
50mg
688,00 $
Auf Lager
100mg
1.094,00 $
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Sample solution is provided at 25 µL, 10mM.



Description of ESI-08

IC50: 8.4 μM (EPAC2)[1]
EPAC1[1]

ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation[1].

Exchange proteins directly activated by cAMP (EPAC) are a family of guanine nucleotide exchange factors that regulate a wide variety of intracellular processes in response to second messenger cAMP. ESI-08 at 25 μM has been found not to alter cAMP-induced type I and II PKA holoenzymes activation while H89, a selective PKA inhibitor, blocked the type I or II PKA activities completely[1].

Chemical Properties of ESI-08

Cas No. 301177-43-5 SDF
Formula C20H23N3OS M.Wt 353.48
Löslichkeit DMSO : 100 mg/mL (282.90 mM; ultrasonic and warming and heat to 60°C) Storage 4°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of ESI-08

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.829 mL 14.1451 mL 28.2901 mL
5 mM 565.8 μL 2.829 mL 5.658 mL
10 mM 282.9 μL 1.4145 mL 2.829 mL
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In vivo Formulation Calculator (Clear solution) of ESI-08

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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