ML204
Based on 8 publication(s) in Google Scholar
ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca2+ channels.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.45%
- No. CAS: 5465-86-1
- Fòrmula: C15H18N2
- Peso molecular:226.32
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ML204
More- Int J Biol Sci. 2024 Sep 16;20(12):4922-4940. [Abstract]
- J Transl Med. 2025 Nov 10;23(1):1254. [Abstract]
- J Ethnopharmacol. 2022 May 23:290:115105. [Abstract]
- Neuropharmacology. 2024 Jul 1:252:109946. [Abstract]
- Exp Cell Res. 2022 Dec 1;421(1):113374. [Abstract]
- Neurosci Res. 2024 Feb:199:48-56. [Abstract]
- Biochem Biophys Res Commun. 2025 Apr 1:755:151566. [Abstract]
- Biol Pharm Bull. 2023;46(6):864-868. [Abstract]
Actividad biológica
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TRPC4 |
TRPC5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.96 μM
Compound: 3; ML204
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Inhibition of mouse TRPC4 beta expressed in HEK293 cells co-expressing mu-opioid receptor assessed as reduction in DAMGO-induced intracellular calcium level in presence of mu-opioid receptor agonist DAMGO by Fluo-4AM dye based fluorescence assay
Inhibition of mouse TRPC4 beta expressed in HEK293 cells co-expressing mu-opioid receptor assessed as reduction in DAMGO-induced intracellular calcium level in presence of mu-opioid receptor agonist DAMGO by Fluo-4AM dye based fluorescence assay
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[PMID: 30943030] |
| HEK293 | IC50 |
17.9 μM
Compound: 3; ML204
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Inhibition of HA-tagged mouse TRPC6 expressed in HEK293 cells assessed as reduction in acetylcholine-induced membrane potential by FLIPR membrane potential dye based assay
Inhibition of HA-tagged mouse TRPC6 expressed in HEK293 cells assessed as reduction in acetylcholine-induced membrane potential by FLIPR membrane potential dye based assay
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[PMID: 30943030] |
| HEK293 | IC50 |
2.6 μM
Compound: 3; ML204
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Inhibition of mouse TRPC4 beta expressed in HEK293 cells co-expressing mu-opioid receptor assessed as reduction in DAMGO-induced current by QPatch clamp assay
Inhibition of mouse TRPC4 beta expressed in HEK293 cells co-expressing mu-opioid receptor assessed as reduction in DAMGO-induced current by QPatch clamp assay
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[PMID: 30943030] |
ML204 inhibits TRPC4β-mediated intracellular Ca2+ rise with an IC50 value of 0.96 μM (HEK293 cells) and exhibits 19-fold selectivity against muscarinic receptor-coupled TRPC6 channel activation[1].
ML204 blocks TRPC4β activity induced through either Gi/o stimulation by μ-opioid, 5HT1A serotonin, and M2 muscarinic receptors or Gq/11 stimulation by the endogenous M3-like muscarinic receptors[1].
ML204 blocks LPS-induced TRPC5 channel activity[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nonfasted male C57BL/6 (2-3 months)[4]
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Dosage:1 mg/kg
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Administration:Subcutaneous injection, twice a day, for 5 days (prior to LPS injection)
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Result:Induced mortality associated with increased hypothermia in mice with LPS-induced systemic inflammatory response.
Chemical Information
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No. CAS 5465-86-1
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Appearance Oil
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Peso molecular 226.32
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Fòrmula C15H18N2
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Color Light yellow to yellow
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SMILES
CC1=CC(N2CCCCC2)=NC3=CC=CC=C13
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (8)
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Journal Impact Factor
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Most Recent
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Int J Biol Sci
Pharmacological manipulation of TRPC5 by kaempferol attenuates metastasis of gastrointestinal cancer via inhibiting calcium involved in the formation of filopodia. [Abstract]2024 Sep 16;20(12):4922-4940. PMID: 39309444 -
J Transl Med
Peroxynitrite regulates ER stress-mediated Ca2+ flux to mitochondria characterizing cardiac microvascular ischemia-reperfusion injury associated with hyperhomocysteinemia. [Abstract]2025 Nov 10;23(1):1254. PMID: 41214689 -
J Ethnopharmacol
Magnolol and honokiol target TRPC4 to regulate extracellular calcium influx and relax intestinal smooth muscle. [Abstract]2022 May 23:290:115105. PMID: 35157953 -
Neuropharmacology
GLP-1 modulated the firing activity of nigral dopaminergic neurons in both normal and parkinsonian mice. [Abstract]2024 Jul 1:252:109946. PMID: 38599494 -
Exp Cell Res
Inhibition of TRPC6 suppressed TGFβ-induced fibroblast-myofibroblast transdifferentiation in renal interstitial NRK-49F cells. [Abstract]2022 Dec 1;421(1):113374. PMID: 36206825 -
Neurosci Res
Exendin-4 increases the firing activity of hippocampal CA1 neurons through TRPC4/5 channels. [Abstract]2024 Feb:199:48-56. PMID: 37595875 -
Biochem Biophys Res Commun
TRPC1 downregulation enhances catecholamine secretion in adrenal chromaffin cells under metabolic syndrome conditions. [Abstract]2025 Apr 1:755:151566. PMID: 40043610 -
Biol Pharm Bull
Inhibition of TRPC4/5 Channel Is Effective in Protecting against Histamine-Induced Hyperpermeability by Blocking Ca2+ Influx in Lung Microvascular Endothelial Cells. [Abstract]2023;46(6):864-868. PMID: 37258152
Solvente y solubilidad
Ethanol : 50 mg/mL (220.93 mM; Need ultrasonic)
DMSO : ≥ 37 mg/mL (163.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (11.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (11.05 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (293 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Miller M, et al. Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels. J Biol Chem. 2011 Sep 23;286(38):33436-46. [Content Brief]
[2]. Miller MR, et al. Novel Chemical Inhibitor of TRPC4 Channels. Probe Reports from the NIH Molecular Libraries Program [Internet]. [Content Brief]
[3]. Thomas Schaldecker, et al. Inhibition of the TRPC5 ion channel protects the kidney filter. J Clin Invest. 2013 Dec 2; 123(12): 5298–5309. [Content Brief]
[4]. Domingos M S Pereira, et al. Transient Receptor Potential Canonical Channels 4 and 5 Mediate Escherichia coli-Derived Thioredoxin Effects in Lipopolysaccharide-Injected Mice. Oxid Med Cell Longev. 2018 Jun 10;2018:4904696. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / Ethanol | 1 mM | 4.4185 mL | 22.0926 mL | 44.1852 mL | 110.4631 mL |
| 5 mM | 0.8837 mL | 4.4185 mL | 8.8370 mL | 22.0926 mL | |
| 10 mM | 0.4419 mL | 2.2093 mL | 4.4185 mL | 11.0463 mL | |
| 15 mM | 0.2946 mL | 1.4728 mL | 2.9457 mL | 7.3642 mL | |
| 20 mM | 0.2209 mL | 1.1046 mL | 2.2093 mL | 5.5232 mL | |
| 25 mM | 0.1767 mL | 0.8837 mL | 1.7674 mL | 4.4185 mL | |
| 30 mM | 0.1473 mL | 0.7364 mL | 1.4728 mL | 3.6821 mL | |
| 40 mM | 0.1105 mL | 0.5523 mL | 1.1046 mL | 2.7616 mL | |
| 50 mM | 0.0884 mL | 0.4419 mL | 0.8837 mL | 2.2093 mL | |
| 60 mM | 0.0736 mL | 0.3682 mL | 0.7364 mL | 1.8411 mL | |
| 80 mM | 0.0552 mL | 0.2762 mL | 0.5523 mL | 1.3808 mL | |
| 100 mM | 0.0442 mL | 0.2209 mL | 0.4419 mL | 1.1046 mL |
ML204 Related Classifications
HY-12949 Related Classifications
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