| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
AM6701 targets the endocannabinoid-metabolizing enzymes fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). Inhibition of these two key enzymes leads to elevated levels of their respective endogenous cannabinoid substrates, anandamide and 2-arachidonoylglycerol. By preventing the breakdown of these endocannabinoids, AM6701 enhances endocannabinoid signaling, which is involved in a wide range of physiological processes including neuroprotection, pain modulation, and inflammation.
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| ln Vitro |
In vitro, AM6701 inhibits both FAAH and MAGL with high and equivalent potency (equipotent inhibitory IC50 = 1.2 nM). This dual inhibition results in a significant increase in the levels of endocannabinoids, such as anandamide and 2-arachidonoylglycerol. The compound's ability to inhibit both enzymes with similar potency makes it a valuable tool for studying the combined effects of FAAH and MAGL blockade.
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| ln Vivo |
In vivo, AM6701 exhibits neuroprotective effects by modulating endogenous cannabinoids and inhibiting calpain-mediated excitotoxic brain injury. It has shown efficacy in models of neurodegenerative conditions where excitotoxicity and neuroinflammation play a key role. By raising endocannabinoid levels, it can reduce the overactivation of glutamate receptors and subsequent calcium influx, thereby protecting neurons from damage.
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| Enzyme Assay |
FAAH and MAGL enzyme activities are measured using in vitro assays with recombinant human enzymes. The enzymes are incubated with a fluorescent or radiolabeled substrate (e.g., anandamide for FAAH). The inhibition of product formation by AM6701 is measured to determine the IC50, which for this compound is 1.2 nM for both targets.
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| Cell Assay |
The effects of AM6701 on neuronal cells are evaluated in vitro. Cells are treated with the compound and subjected to excitotoxic injury. Cell viability, levels of endocannabinoids, and markers of apoptosis are measured to assess neuroprotection. The compound's ability to protect against cell death in these models is a key indicator of its neuroprotective potential.
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| Animal Protocol |
Neuroprotective efficacy is evaluated in animal models of excitotoxic brain injury or neurodegenerative disease. AM6701 is administered systemically, and neurological outcomes, histopathology, and biochemical markers are assessed. The compound's ability to reduce brain damage and improve functional recovery in these models is measured.
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| ADME/Pharmacokinetics |
As a small molecule, AM6701 is expected to be orally bioavailable and to cross the blood-brain barrier to exert its central nervous system effects. Its pharmacokinetic profile is being investigated in preclinical studies. Its LogP value of 2.15 suggests moderate lipophilicity, which is favorable for blood-brain barrier penetration.
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| Toxicity/Toxicokinetics |
Dual inhibition of FAAH and MAGL may lead to adverse effects such as hypothermia, catalepsy, and other cannabinoid-mediated central nervous system effects, depending on the degree of endocannabinoid elevation. These effects are typically mild and reversible but can be more pronounced at higher doses.
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| References | |
| Additional Infomation |
AM6701 is a research compound being studied for its neuroprotective potential. It serves as a valuable tool to investigate the therapeutic potential of dual FAAH/MAGL inhibition in neurodegenerative diseases and neuroinflammation. By modulating the endocannabinoid system, it offers a novel approach to treating conditions like stroke, traumatic brain injury, and chronic neurodegenerative disorders.
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| Molecular Formula |
C17H17N5O
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|---|---|
| Molecular Weight |
307.357
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| Exact Mass |
307.143
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| CAS # |
1010096-65-7
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| PubChem CID |
24795576
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
506.1±53.0 °C at 760 mmHg
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| Flash Point |
259.9±30.9 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.640
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| LogP |
2.15
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
388
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N1N=C(CC2=CC=C(C3=CC=CC=C3)C=C2)N=N1)N(C)C
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| InChi Key |
VBVLSXPOMAONNK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17N5O/c1-21(2)17(23)22-19-16(18-20-22)12-13-8-10-15(11-9-13)14-6-4-3-5-7-14/h3-11H,12H2,1-2H3
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| Chemical Name |
N,N-dimethyl-5-[(4-phenylphenyl)methyl]tetrazole-2-carboxamide
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| Synonyms |
AM-6701; AM 6701; AM6701
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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: ~100 mg/mL (~325.4 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.13 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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2535 mL | 16.2676 mL | 32.5351 mL | |
| 5 mM | 0.6507 mL | 3.2535 mL | 6.5070 mL | |
| 10 mM | 0.3254 mL | 1.6268 mL | 3.2535 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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