| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
| Targets |
M084 hydrochloride targets TRPC4 and TRPC5 channels, which are members of the transient receptor potential canonical (TRPC) family of non-selective cation channels. TRPC4 and TRPC5 are predominantly expressed in the brain and are involved in regulating neuronal excitability, synaptic plasticity, and calcium signaling. These channels are activated by G protein-coupled receptors and phospholipase C signaling, and they play roles in various physiological and pathological processes, including mood regulation, pain, and cardiovascular function. M084 hydrochloride is a channel blocker that inhibits TRPC4 with an IC50 of 10.3 μM and TRPC5 with an IC50 of 8.2 μM. By blocking these channels, the compound modulates neuronal excitability and calcium homeostasis, leading to its antidepressant and anxiolytic effects.
|
|---|---|
| ln Vitro |
In vitro, M084 hydrochloride blocks TRPC4 and TRPC5 channels with IC50 values of 10.3 μM and 8.2 μM, respectively. The compound's activity can be assessed in electrophysiological studies using cells expressing recombinant TRPC4 or TRPC5 channels. Whole-cell patch-clamp or fluorescence-based membrane potential assays can be used to measure the inhibition of channel activity. M084 hydrochloride has antidepressant and anxiolytic effects, which can be studied in cell-based models of neuronal function. However, specific cell-based and in vivo data beyond the IC50 values have not been extensively reported in the available literature. The compound is used in research on mood disorders and TRPC channel function.
|
| ln Vivo |
In vivo, M084 hydrochloride has antidepressant and anxiolytic effects. These effects are likely mediated through its blockade of TRPC4 and TRPC5 channels in the brain. However, specific animal model studies, dosing regimens, and quantitative outcomes have not been extensively reported in the available literature. The compound's ability to cross the blood-brain barrier and its pharmacokinetic properties would be important considerations for in vivo applications. Further in vivo studies would be required to characterize its efficacy, safety, and pharmacokinetic properties in animal models of depression and anxiety.
|
| Enzyme Assay |
In vitro electrophysiological assay protocols for M084 hydrochloride typically involve measuring its inhibition of TRPC4 and TRPC5 channel activity. A standard protocol would involve using HEK293 cells or other cell lines stably expressing recombinant TRPC4 or TRPC5 channels. Whole-cell patch-clamp recordings are performed to measure channel currents in the presence of varying concentrations of M084 hydrochloride (typically 0.1-100 μM). The inhibition of current amplitude is plotted against compound concentration to determine IC50 values. Alternatively, fluorescence-based membrane potential assays or calcium imaging assays using calcium-sensitive dyes can be used for higher-throughput screening. Appropriate controls include vehicle-treated cells and cells treated with a known TRPC channel blocker.
|
| Cell Assay |
In vitro cell-based assay protocols for M084 hydrochloride would typically involve assessing its effects on neuronal function or signaling pathways. A standard protocol would involve treating neuronal cell lines or primary neuronal cultures with varying concentrations of M084 hydrochloride (typically 0.1-100 μM) for a defined period. Neuronal excitability can be assessed by measuring action potential firing or calcium influx. Cell viability is assessed using MTT or similar assays to ensure that observed effects are not due to cytotoxicity. For studies of antidepressant and anxiolytic effects, the compound's effects on neurotransmitter release or signaling pathways can be assessed. Appropriate controls include vehicle-treated cells.
|
| Animal Protocol |
In vivo animal experimental protocols for M084 hydrochloride have not been extensively reported in the available literature. Based on its antidepressant and anxiolytic effects, potential studies might involve using mouse models of depression (e.g., forced swim test, tail suspension test) or anxiety (e.g., elevated plus maze, open field test). A hypothetical protocol would involve administering M084 hydrochloride via oral gavage or intraperitoneal injection at doses determined from preliminary studies. Behavioral tests are performed after compound administration, and the effects on depressive- and anxiety-like behaviors are assessed. Appropriate controls include vehicle-treated groups and groups treated with a known antidepressant or anxiolytic for comparison.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of M084 hydrochloride have not been characterized in published studies. The compound has a molecular weight of 225.72 and a molecular formula of C11H16ClN3. It should be stored desiccated at room temperature. Specific PK parameters such as half-life, Cmax, AUC, bioavailability, volume of distribution, and clearance have not been reported. The compound's ability to cross the blood-brain barrier, which is critical for CNS applications, has not been assessed. The compound's metabolism, protein binding, and routes of elimination remain to be characterized. Further pharmacokinetic studies would be required to understand its absorption, distribution, metabolism, and excretion profile.
|
| References |
|
| Additional Infomation |
M084 hydrochloride is a research-grade compound that functions as a TRPC4/5 channel blocker with IC50 values of 10.3 μM and 8.2 μM, respectively. It has antidepressant and anxiolytic effects and is used in research on mood disorders and TRPC channel function. The compound has not entered clinical trials and is not approved for any therapeutic indication. Its mechanism of action involves blockade of TRPC4 and TRPC5 channels, modulating neuronal excitability and calcium homeostasis. The compound is available exclusively for research purposes and is not intended for diagnostic, therapeutic, or human applications.
|
| Molecular Formula |
C11H16CLN3
|
|---|---|
| Molecular Weight |
225.717841148376
|
| Exact Mass |
225.103
|
| CAS # |
1992047-63-8
|
| PubChem CID |
121513894
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
15
|
| Complexity |
172
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl.N(C1=NC2C=CC=CC=2N1)CCCC
|
| InChi Key |
DMLSYUAQEOLJQC-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C11H15N3.ClH/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);1H
|
| Chemical Name |
N-butyl-1H-benzimidazol-2-amine;hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
Typically soluble in DMSO (e.g. 10 mM)
|
|---|---|
| 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 | 4.4303 mL | 22.1513 mL | 44.3027 mL | |
| 5 mM | 0.8861 mL | 4.4303 mL | 8.8605 mL | |
| 10 mM | 0.4430 mL | 2.2151 mL | 4.4303 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
