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| SKU | Size | Availability |
Price | Qty |
|---|---|---|---|---|
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E646947-5mg
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5mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$150.90
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E646947-10mg
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10mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$250.90
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E646947-25mg
|
25mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$550.90
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E646947-50mg
|
50mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$850.90
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E646947-100mg
|
100mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$1,350.90
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| Specifications & Purity | ≥99% |
|---|---|
| Biochemical and Physiological Mechanisms | ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 ( IC 50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation. |
| Storage Temp | Protected from light,Store at -80°C |
| Shipped In |
Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available. |
| Product Description |
ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 ( IC 50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 8.4 μM (EPAC2), EPAC1 |
Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organosulfur compounds |
| Class | Thioethers |
| Subclass | Aryl thioethers |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Aryl thioethers |
| Alternative Parents | p-Xylenes Pyrimidones Alkylarylthioethers Hydropyrimidines Vinylogous amides Heteroaromatic compounds Sulfenyl compounds Nitriles Azacyclic compounds Organopnictogen compounds Organooxygen compounds Organic oxides Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteromonocyclic compounds |
| Substituents | Aryl thioether - P-xylene - Xylene - Pyrimidone - Alkylarylthioether - Monocyclic benzene moiety - Hydropyrimidine - Pyrimidine - Benzenoid - Heteroaromatic compound - Vinylogous amide - Sulfenyl compound - Nitrile - Carbonitrile - Organoheterocyclic compound - Azacycle - Organic nitrogen compound - Hydrocarbon derivative - Organic oxide - Organopnictogen compound - Organooxygen compound - Organonitrogen compound - Organic oxygen compound - Aromatic heteromonocyclic compound |
| Description | This compound belongs to the class of organic compounds known as aryl thioethers. These are organosulfur compounds containing a thioether group that is substituted by an aryl group. |
| External Descriptors | Not available |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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| IUPAC Name | 4-cyclohexyl-2-[(2,5-dimethylphenyl)methylsulfanyl]-6-oxo-1H-pyrimidine-5-carbonitrile |
|---|---|
| INCHI | InChI=1S/C20H23N3OS/c1-13-8-9-14(2)16(10-13)12-25-20-22-18(15-6-4-3-5-7-15)17(11-21)19(24)23-20/h8-10,15H,3-7,12H2,1-2H3,(H,22,23,24) |
| InChIKey | LSHOSZQLVLPEGG-UHFFFAOYSA-N |
| Smiles | CC1=CC(=C(C=C1)C)CSC2=NC(=C(C(=O)N2)C#N)C3CCCCC3 |
| Isomeric SMILES | CC1=CC(=C(C=C1)C)CSC2=NC(=C(C(=O)N2)C#N)C3CCCCC3 |
| PubChem CID | 135473051 |
| Molecular Weight | 353.48 |
| Solubility | DMSO : 100 mg/mL (282.90 mM; ultrasonic and warming and heat to 60°C) |
|---|---|
| Molecular Weight | 353.500 g/mol |
| XLogP3 | 4.500 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 4 |
| Exact Mass | 353.156 Da |
| Monoisotopic Mass | 353.156 Da |
| Topological Polar Surface Area | 90.600 Ų |
| Heavy Atom Count | 25 |
| Formal Charge | 0 |
| Complexity | 624.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |