Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
HJC0350 is a potent and selective antagonist/inhibitor of EPAC2 with IC50 of 0.3 μM, it exhibited no inhibition on Epac1. Under both physiological and pathological conditions, the isoforms of exchange proteins directly activated by cAMP (EPAC), EPAC1 and EPAC2, react to the second messenger cAMP and control a host of intracellular functions. HJC 0350 competed with 8-NBD-cAMP in binding recombinant fusion protein EPAC2 with IC50 value of 0.3 μM and exhibited 133-fold more potent than cAMP, which competed with 8-NBD-cAMP in binding EPAC2 with IC50 value of 40 μM. HJC 0350 (25 μM) demonstrated EPAC2-specific antagonist properties as it inhibited EPAC2 GEF activity but had no effect on EPAC1-mediated Rap1-GDP exchange activity or cAMP-mediated PKA activation.
Targets |
EPAC2 ( IC50 = 0.3 µM )
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
HJC 0350 is a potent and selective antagonist of EPAC2. HJC 0350 competed with 8-NBD-cAMP in binding recombinant fusion protein EPAC2 with IC50 value of 0.3 μM and exhibited 133-fold more potent than cAMP, which competed with 8-NBD-cAMP in binding EPAC2 with IC50 value of 40 μM. HJC 0350 (25 μM) inhibited EPAC2 GEF activity in the presence of 25 μM cAMP, but did not affect cAMP-mediated PKA activation or EPAC1-mediated Rap1-GDP exchange activity. This suggests that HJC 0350 is an EPAC2-specific antagonist.
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Cell Assay |
HJC 0350 (10 μM) completely inhibited the decrease of FRET in HEK293/EPAC2-FL cells induced by 007-AM (a membrane permeable EPAC selective cAMP analogue) in HEK293 cells expressing EPAC1- or EPAC2-based fluorescence resonance energy transfer (FRET) sensor (EPAC2-FL or EPAC1-FL). However, it had no effect on HEK293/EPAC1-FL cells.
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Animal Protocol |
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References |
Molecular Formula |
C15H19NO2S
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Molecular Weight |
277.38
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Exact Mass |
277.11
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Elemental Analysis |
C, 64.95; H, 6.90; N, 5.05; O, 11.54; S, 11.56
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CAS # |
885434-70-8
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
CC1=CC(=C(C(=C1)C)S(=O)(=O)N2C=C(C=C2C)C)C
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InChi Key |
AFZWZVLPIMHLSE-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C15H19NO2S/c1-10-6-12(3)15(13(4)7-10)19(17,18)16-9-11(2)8-14(16)5/h6-9H,1-5H3
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Chemical Name |
2,4-dimethyl-1-(2,4,6-trimethylphenyl)sulfonylpyrrole
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Synonyms |
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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 |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.01 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 | 3.6052 mL | 18.0258 mL | 36.0516 mL | |
5 mM | 0.7210 mL | 3.6052 mL | 7.2103 mL | |
10 mM | 0.3605 mL | 1.8026 mL | 3.6052 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.
Relative potency of EPAC2 antagonist 20i(HJC0350).J Med Chem.2013 Feb 14;56(3):952-62. th> |
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Specificity of EPAC antagonists 1, 14c and 20i.J Med Chem.2013 Feb 14;56(3):952-62. td> |
Effects of 20i on 007-AM mediated cellular activation of EPAC.J Med Chem.2013 Feb 14;56(3):952-62. td> |
Effects of 20i on 8-Br-cAMP-AM mediated cellular activation of PKA.J Med Chem.2013 Feb 14;56(3):952-62. th> |
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J Med Chem.2013 Feb 14;56(3):952-62. td> |