| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
EC50: 2.37 μM (TRPC6-expressing HEK293 cells)[1]
TRPC6-PAM-C20 targets the TRPC6 channel as a positive allosteric modulator (PAM). TRPC6 is a non-selective cation channel involved in calcium signaling, vascular smooth muscle contraction, and various physiological processes. As a PAM, the compound enhances channel activation by enabling low basal concentrations of diacylglycerol (DAG) to induce ion channel activation. It induces an increase in intracellular Ca2+ concentration in TRPC6-expressing cells with an EC50 of 2.37 μM. The compound also activates TRPA1. |
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| ln Vitro |
In vitro studies demonstrate that TRPC6-PAM-C20 is a selective positive allosteric modulator of TRPC6 channels. It is a potent enhancer of channel activation, enabling low basal concentrations of DAG to induce ion channel activation. The compound induces an increase in Ca2+ concentration in HEK293 cells expressing TRPC6 with an EC50 of 2.37 μM. It selectively activates TRPC6 over other TRP channels but also activates TRPA1. The compound provides a powerful tool for probing channel regulation, calcium dynamics, and disease mechanisms.
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| ln Vivo |
In vivo studies of TRPC6-PAM-C20 are limited in publicly available literature. By enhancing TRPC6 activity, the compound provides a tool for studying channel regulation, calcium dynamics, and disease mechanisms. Research highlights its applications in studying focal segmental glomerulosclerosis, pulmonary hypertension, and neurological disorders. However, specific in vivo efficacy data and detailed animal model studies are not extensively reported. Further research is needed to establish its in vivo activity profile, pharmacokinetic properties, and therapeutic potential. The compound remains a research tool for TRPC6 channel biology.
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| Enzyme Assay |
For TRPC6 channel assays, HEK293 cells expressing TRPC6 are cultured and loaded with calcium-sensitive fluorescent dyes (e.g., Fluo-4 or Fura-2). TRPC6-PAM-C20 is dissolved in DMSO and diluted in assay buffer to varying concentrations. Cells are treated with the compound and calcium flux is measured using fluorescence plate readers. EC50 values (e.g., 2.37 μM) are calculated from dose-response curves. For selectivity assays, similar protocols are used with cells expressing other TRP channels (e.g., TRPA1) to assess off-target activity. Assays are performed in replicate with appropriate vehicle controls and positive controls.
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| Cell Assay |
For in vitro cellular assays, HEK293 cells expressing TRPC6 or other relevant cell lines are cultured in appropriate media under standard conditions (37°C, 5% CO2). TRPC6-PAM-C20 is dissolved in DMSO and diluted in culture medium to desired concentrations. Cells are treated with compound for specified durations. Intracellular calcium levels are measured using fluorescent indicators. For functional studies, downstream signaling pathways (e.g., NFAT activation, gene expression) may be assessed. Cell viability and cytotoxicity are assessed using standard assays. Each concentration is tested in replicate wells with vehicle controls.
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| Animal Protocol |
For in vivo animal studies of TRPC6-PAM-C20, no specific published protocols are available. For general in vivo administration of TRPC6 modulators, compounds are typically formulated in suitable vehicles and administered via oral gavage, intraperitoneal (i.p.) injection, or intravenous (i.v.) injection. Dosing regimens vary by study objective. In disease models (e.g., focal segmental glomerulosclerosis, pulmonary hypertension), animals may be treated with compound and disease progression is monitored. Blood and tissue samples may be collected for pharmacokinetic analysis. All procedures must follow institutional animal care and use committee guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of TRPC6-PAM-C20 are characteristic of a small-molecule channel modulator. The compound has a CAS number of 667427-75-0. Molecular weight and formula are not extensively reported in publicly available sources. Storage: typically at -20°C for powder; in solvent at -80°C. Solubility: soluble in DMSO and other organic solvents. Specific pharmacokinetic parameters such as half-life, clearance, and bioavailability are not extensively reported. The compound is a research tool for studying TRPC6 and TRPA1 channels.
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| Toxicity/Toxicokinetics |
According to available safety information, TRPC6-PAM-C20 is intended for research purposes only. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment (gloves, lab coat, safety goggles). The compound should be handled in a well-ventilated area. Avoid dust formation and inhalation. In case of skin contact, wash with plenty of soap and water. In case of eye contact, rinse cautiously with water for several minutes. No clinical toxicity data are available.
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| References | |
| Additional Infomation |
TRPC6-PAM-C20 is a selective positive allosteric modulator of TRPC6 channels that enables low basal DAG concentrations to induce channel activation. It induces Ca2+ increase in TRPC6-expressing HEK293 cells with an EC50 of 2.37 μM. It selectively activates TRPC6 over other TRP channels but also activates TRPA1. It has applications in studying focal segmental glomerulosclerosis, pulmonary hypertension, and neurological disorders. It is for research use only.
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| Molecular Formula |
C22H21NO4
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|---|---|
| Molecular Weight |
363.406446218491
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| Exact Mass |
363.147
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| CAS # |
667427-75-0
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| PubChem CID |
1081484
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| Appearance |
White to off-white solid powder
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| LogP |
4
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
653
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C)C1C(=CC2C(C3C(=O)OC4C=CC=CC=4C=3)=NC(C)(C)CC=2C=1)OC
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| InChi Key |
SNICUMZYPOCXCO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H21NO4/c1-22(2)12-14-10-18(25-3)19(26-4)11-15(14)20(23-22)16-9-13-7-5-6-8-17(13)27-21(16)24/h5-11H,12H2,1-4H3
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| Chemical Name |
3-(6,7-dimethoxy-3,3-dimethyl-4H-isoquinolin-1-yl)chromen-2-one
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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: 33.33 mg/mL (91.71 mM)
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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 | 2.7517 mL | 13.7586 mL | 27.5171 mL | |
| 5 mM | 0.5503 mL | 2.7517 mL | 5.5034 mL | |
| 10 mM | 0.2752 mL | 1.3759 mL | 2.7517 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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