| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Exchange protein directly activated by cAMP (Epac), specifically the Epac1 isoform. Epac1 is a guanine nucleotide exchange factor (GEF) for the small GTPases Rap1 and Rap2. 8-CPT-2Me-cAMP is a selective agonist of this PKA-independent cAMP sensor.
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| ln Vitro |
In cell-based assays, 8-CPT-2Me-cAMP stimulates Epac-mediated Ca2+ release in pancreatic beta cells in vitro. It also activates Epac1 with an EC50 of 2.2 microM in biochemical assays and upregulates mTORC2 activation in prostate cancer cells, leading to increased p-Akt levels.
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| ln Vivo |
Not reported. As an Epac-selective agonist, this compound is used in vivo to dissect Epac-specific functions from those of PKA. It has been shown to enhance 2-AG-mediated synaptic depression in ventral tegmental area (VTA) dopamine neurons via activation of PLCε, suggesting it has activity in the mouse brain.
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| Enzyme Assay |
A cell-free assay for Epac1 activation is performed using purified recombinant Epac1 and a fluorescently labeled Rap1 protein. The exchange reaction is monitored as an increase in fluorescence upon binding of GTP to Rap1. The compound is added at varying concentrations, and the EC50 (2.2 microM) for Epac1 activation is calculated by measuring the rate of nucleotide exchange.
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| Cell Assay |
HEK293 cells stably expressing Epac1 and a cAMP-responsive reporter (e.g., Epac1-based FRET sensor) are seeded in 96-well plates. Cells are treated with varying concentrations of 8-CPT-2Me-cAMP, and the FRET signal (indicative of Epac activation) is measured in real-time using a fluorescence plate reader. For Ca2+ release assays, pancreatic beta-cells are loaded with Fluo-4 and stimulated, and fluorescence is measured.
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| Animal Protocol |
8-CPT-2Me-cAMP is typically administered via intracerebroventricular (ICV) injection in rodents. In a typical experiment, it is infused directly into the VTA of the brain, and its effect on synaptic transmission is measured using whole-cell patch-clamp electrophysiology. Endpoints include changes in inhibitory postsynaptic current frequency and amplitude.
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| ADME/Pharmacokinetics |
Not reported. As a cyclic nucleotide analog, 8-CPT-2Me-cAMP is expected to be cell-permeable, but its systemic pharmacokinetics are not well-characterized. It is typically used in in vitro settings or via direct injection into target tissues (e.g., brain) due to potential rapid metabolism and low bioavailability.
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| Toxicity/Toxicokinetics |
Not reported. The toxicological profile of 8-CPT-2Me-cAMP is not characterized for systemic use. As an Epac-selective agonist, high doses could disrupt normal cellular signaling. However, its high selectivity for Epac over PKA minimizes the risk of PKA-mediated side effects, making it a safer tool for dissecting cAMP signaling.
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| References |
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| Additional Infomation |
8-CPT-2Me-cAMP is a key chemical tool for understanding the specific functions of Epac proteins, which are involved in diverse processes including insulin secretion, cell adhesion, exocytosis, and cardiac contractility. By selectively activating Epac without affecting PKA, this compound has helped clarify the distinct roles of these two major cAMP effectors. It is particularly valuable for studying diseases where cAMP signaling is dysregulated, such as diabetes, heart failure, and cancer.
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| Molecular Formula |
C17H16CLN5NAO6PS
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|---|---|
| Molecular Weight |
507.82
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| Exact Mass |
525.025
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| CAS # |
634207-53-7
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| PubChem CID |
9913268
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| Appearance |
White to off-white solid powder
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| Melting Point |
235.5-237.5 ℃(lit.)
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| LogP |
3.596
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
708
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CO[C@@H]1[C@H]2[C@@H](COP(=O)(O2)O)O[C@H]1N3C4=NC=NC(=C4N=C3SC5=CC=C(C=C5)Cl)N
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| InChi Key |
BCGHHRAUZWOTNH-XNIJJKJLSA-N
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| InChi Code |
InChI=1S/C17H17ClN5O6PS/c1-26-13-12-10(6-27-30(24,25)29-12)28-16(13)23-15-11(14(19)20-7-21-15)22-17(23)31-9-4-2-8(18)3-5-9/h2-5,7,10,12-13,16H,6H2,1H3,(H,24,25)(H2,19,20,21)/t10-,12-,13-,16-/m1/s1
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| Chemical Name |
9-[(4aR,6R,7R,7aR)-2-hydroxy-7-methoxy-2-oxo-4a,6,7,7a-tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinin-6-yl]-8-(4-chlorophenyl)sulfanylpurin-6-amine
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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 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)
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| Solubility (In Vitro) |
DMSO: 125 mg/mL (246.15 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9692 mL | 9.8460 mL | 19.6920 mL | |
| 5 mM | 0.3938 mL | 1.9692 mL | 3.9384 mL | |
| 10 mM | 0.1969 mL | 0.9846 mL | 1.9692 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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