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| 25mg |
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Purity: ≥98%
ESI-05 (also known as NSC 116966) is a novel, potent and specific antagonist of EPAC2 (exchange protein directly activated by cAMP 2), with an IC50 of 0.4 µM. ESI-05 prevents both EAPC2-mediated Rap1 activation and cAMP-mediated EPAC2 activation.
| Targets |
EPAC2 ( IC50 = 0.43 μM )
|
|---|---|
| ln Vitro |
ESI-05 (0.01 μM-1 nM) inhibits cAMP-mediated EPAC2 GEF activity with an IC50 of 0.43 μM, but is completely blank in inhibiting EPAC1 GEF activity [1]. ESI-05 (1, 5, 10, and 25 μM; 5 Western Blot Analysis[1] Cell Line: HEK293 cells Concentration: 1, 5, 10, and 25 μM Incubation Time: 5 min Results: Results in dose-dependent manner. EPAC Selection A cAMP analog (007-AM) induces a reduction in Rap1 activation.
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| ln Vivo |
ESI-05 (2, 4 and 8 mg/kg) reduces neuronal cells in vivo by inhibiting p38/BIM [2]. Animal model: Intracranial hemorrhage (ICH) model [2] Dosage: 2, 4, 8 mg/kg Administration: Results: Decreased apoptosis rate of cortical nerve cells, phosphorylated p38, Bcl-2like protein 11 (BIM) and caspase- 3 Protein expression decreased accordingly.
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| Cell Assay |
Cell Line: HEK293 cells
Concentration: 1, 5, 10, and 25 μM Incubation Time: 5 min Result: Led to a dose-dependent reduction of the EPAC-selective cAMP analog (007-AM) induced Rap1 activation. |
| Animal Protocol |
Intracranial hemorrhage (ICH) model
2, 4, and 8 mg/kg |
| References |
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| Molecular Formula |
C16H18O2S
|
|---|---|
| Molecular Weight |
274.37792
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| Exact Mass |
274.103
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| Elemental Analysis |
C, 70.04; H, 6.61; O, 11.66; S, 11.68
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| CAS # |
5184-64-5
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| PubChem CID |
272513
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| Appearance |
White to off-white solid powder
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| Density |
1.129g/cm3
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| Boiling Point |
426.7ºC at 760mmHg
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| Flash Point |
250ºC
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| Index of Refraction |
1.562
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| LogP |
4.833
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
|
| Heavy Atom Count |
19
|
| Complexity |
376
|
| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=C(C=C1)S(=O)(=O)C2=C(C=C(C=C2C)C)C
|
| InChi Key |
CGPHOZWFSFNOEQ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H18O2S/c1-11-5-7-15(8-6-11)19(17,18)16-13(3)9-12(2)10-14(16)4/h5-10H,1-4H3
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| Chemical Name |
1,3,5-trimethyl-2-(4-methylphenyl)sulfonylbenzene
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| Synonyms |
ESI-05; NSC-116966; ESI05; NSC116966; ESI 05; NSC 116966
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 50~55 mg/mL (182.2~200.5 mM)
Ethanol: ~55 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6446 mL | 18.2229 mL | 36.4458 mL | |
| 5 mM | 0.7289 mL | 3.6446 mL | 7.2892 mL | |
| 10 mM | 0.3645 mL | 1.8223 mL | 3.6446 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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