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| Targets |
6-MB-cAMP directly targets and activates Protein Kinase A (PKA), the primary intracellular receptor for cAMP. Upon entering the cell, it binds to the regulatory subunits of PKA, causing a conformational change that releases the catalytic subunits. These active catalytic subunits then phosphorylate various downstream substrates such as CREB (cAMP response element-binding protein), thereby regulating gene expression. Unlike natural cAMP, it is resistant to hydrolysis by phosphodiesterases, leading to prolonged target activation .
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| ln Vitro |
In vitro studies demonstrate that 6-MB-cAMP effectively stimulates long-lasting potentiation of postsynaptic responses in neuronal preparations, mimicking the effects of forskolin (an adenylyl cyclase activator). It is more potent than other analogs like 8-Br-cAMP in certain cell types due to its resistance to PDE degradation. In human primary cultured thyrocytes, it modulates cAMP-regulated gene expression. It also stimulates progesterone production in rabbit corpus luteum, confirming its bioactivity as a potent PKA activator. The effective concentration range is typically 10-500 microM .
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| ln Vivo |
In vivo, 6-MB-cAMP is used to investigate the physiological roles of cAMP. In animal models of cardiac function, intracardiac injection leads to increased heart rate and contractility by directly activating PKA in myocardial cells, independent of beta-adrenergic receptor stimulation. In the central nervous system, direct administration into brain regions (e.g., hippocampus) influences long-term potentiation (LTP), a cellular correlate of learning and memory. These effects are typically transient, lasting from 30 minutes to several hours depending on the dose and route of administration .
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| Enzyme Assay |
A non-cell experimental workflow involves the PKA Kinase Activity Assay. The catalytic subunit of PKA (5 ng) is incubated in a reaction buffer containing 20 mM Tris-HCl (pH 7.4), 10 mM MgCl2, 0.1 mg/mL BSA, and 50 uM ATP. A specific PKA substrate peptide (e.g., kemptide, LRRASLG) is added to a final concentration of 20 uM. 6-MB-cAMP (0-100 uM) is added to activate the holoenzyme complex. The reaction is carried out for 10 min at 30degC. Phosphate incorporation is measured by a luminescent ADP detection kit or by radiolabeled [gamma-32P]ATP .
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| Cell Assay |
HEK293 cells are seeded in 12-well plates at a density of 2×10⁵ cells/well and cultured in DMEM with 10% FBS for 24 hours. The medium is replaced with serum-free medium containing 0.5 mM IBMX (a PDE inhibitor) to prevent cAMP breakdown. Cells are treated with 6-MB-cAMP (50, 100, 250 uM) or 100 uM Forskolin (positive control) for 30-60 min at 37degC. After treatment, cells are lysed, and intracellular cAMP accumulation is quantified using a competitive ELISA kit. Alternatively, PKA activity is measured in cell lysates using a PKA activity assay kit .
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| Animal Protocol |
A rat model of Morris water maze is used to test spatial memory. Male Sprague-Dawley rats (250-300g) undergo cannula implantation into the CA1 region of the hippocampus. After recovery, rats receive intra-hippocampal injections of 6-MB-cAMP (10 ug/uL in artificial CSF, 2 uL per side) or vehicle 30 minutes prior to training trials over 5 days. Latency to find the hidden platform is recorded daily. A probe trial (60 sec) is conducted 24 hours after the last training day to assess memory retention .
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| ADME/Pharmacokinetics |
6-MB-cAMP is highly water-soluble (50 mg/mL) and stable in aqueous solutions. Upon tissue entry, it is partially metabolized by intracellular esterases to generate cAMP and butyric acid, though the analog itself is largely resistant to PDEs. Its half-life in biological systems is significantly longer than native cAMP (minutes vs. seconds). The sodium salt formulation (C14H17N5NaO7P) has a molecular weight of 445.28 g/mol. The compound should be stored desiccated at -20degC .
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| Toxicity/Toxicokinetics |
Acute toxicity studies show an LD50 > 1000 mg/kg in rodents via intraperitoneal injection. 6-MB-cAMP exhibits low cytotoxicity in cell culture at concentrations below 500 uM for 48 hours. Prolonged activation of PKA can potentially induce apoptosis in certain cell types (e.g., thyroid cells) or alter metabolic states. Safety data indicates it is a combustible solid (Storage Class Code 11) but is not classified as a hazardous substance under GHS for acute toxicity. No chronic toxicity data is available .
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| References | |
| Additional Infomation |
6-MB-cAMP is a research tool used exclusively for laboratory investigations. It is not approved for clinical use as a drug. However, it serves as a standard control in high-throughput screening assays for identifying novel GPCR ligands or PDE inhibitors. Its ability to bypass membrane receptors and directly activate PKA makes it invaluable for studying downstream cAMP signaling pathways without the need for upstream stimuli. It is also used to induce differentiation in neuronal and endocrine cell cultures .
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| Molecular Formula |
C14H17N5NAO7P
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| Molecular Weight |
421.28
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| CAS # |
70253-67-7
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
[Na+].CCCC(NC1N=CN=C2N(C3OC4COP(OC4C3O)(O)=O)C=NC=12)=O
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| Synonyms |
N6-Monobutyryl-cAMP
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.3737 mL | 11.8686 mL | 23.7372 mL | |
| 5 mM | 0.4747 mL | 2.3737 mL | 4.7474 mL | |
| 10 mM | 0.2374 mL | 1.1869 mL | 2.3737 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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