| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
| Targets |
M-084 targets TRPC4 and TRPC5 channels. It acts as a channel blocker, inhibiting the function of these non-selective cation channels. The compound also has off-target effects, including the inhibition of mitochondrial respiration and the activation of the mitochondrial unfolded protein response (UPRmt) and AMPK. These effects contribute to its unique pharmacological profile.
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| ln Vitro |
In vitro, M-084 has been shown to block TRPC4 and TRPC5 channels with IC50 values of 10.3 µM and 8.2 µM, respectively. It also inhibits mitochondrial respiration and activates the mitochondrial unfolded protein response (UPRmt) and AMPK. These activities have been confirmed in various cell-based assays.
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| ln Vivo |
In vivo, M-084 has demonstrated antidepressant and anxiolytic effects in animal models. It also delays the aging process in C. elegans. These effects are mediated through its actions on TRPC4/5 channels and mitochondrial function.
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| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for M-084 involve studying its interaction with TRPC4 and TRPC5 channels. Membrane preparations from cells expressing the channels are incubated with a radiolabeled ligand, and the ability of the compound to displace the ligand is measured. The compound's effects on mitochondrial respiration can be measured using an oxygen consumption assay with isolated mitochondria.
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| Cell Assay |
In vitro cell-based assays for M-084 are performed using cells expressing TRPC4 or TRPC5 channels. Cells are loaded with a calcium-sensitive fluorescent dye and stimulated with a TRPC agonist. The inhibition of the calcium response by M-084 is measured as a functional readout of channel blockade. The compound's effects on mitochondrial function are assessed by measuring oxygen consumption rate (OCR) and ATP levels.
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| Animal Protocol |
In vivo animal experiments for M-084 are conducted using rodent models of depression and anxiety, such as the forced swim test and the elevated plus maze. The compound is administered, and its effects on behavior are assessed. The anti-aging effects are studied in C. elegans by measuring lifespan and healthspan.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of M-084 have been characterized to support its use as a research tool. The compound has a molecular weight of 189.26 and a formula of C₁₁H₁₅N₃. It is soluble in DMSO. Specific PK parameters, such as half-life and bioavailability, are determined in preclinical studies via LC-MS/MS analysis of plasma samples.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for M-084 are typical of a research compound. It is generally well-tolerated at effective doses. The safety profile is being evaluated in the context of its use as a research tool to study TRPC channels and aging.
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| References | |
| Additional Infomation |
N-Butyl-1H-benzimidazole-2-amine is a member of the benzimidazole class of compounds.
Other information: M-084 is a research compound used to study TRPC4/5 channels, depression, anxiety, and aging. It is available from chemical suppliers for preclinical research purposes. |
| Molecular Formula |
C11H15N3
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|---|---|
| Molecular Weight |
189.2569
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| Exact Mass |
189.127
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| CAS # |
51314-51-3
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| PubChem CID |
284016
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| Appearance |
White to light yellow solid powder
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| Density |
1.153g/cm3
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| Boiling Point |
344.8ºC at 760 mmHg
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| Flash Point |
162.3ºC
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| Index of Refraction |
1.653
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| LogP |
2.847
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
14
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| Complexity |
172
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OKKUCNXCFWODOE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H15N3/c1-2-3-8-12-11-13-9-6-4-5-7-10(9)14-11/h4-7H,2-3,8H2,1H3,(H2,12,13,14)
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| Chemical Name |
N-butyl-1H-benzimidazol-2-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 |
| 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 (~660.47 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.08 mg/mL (10.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (10.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.2837 mL | 26.4187 mL | 52.8374 mL | |
| 5 mM | 1.0567 mL | 5.2837 mL | 10.5675 mL | |
| 10 mM | 0.5284 mL | 2.6419 mL | 5.2837 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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