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| Targets |
TRPC6-IN-1 targets the Transient Receptor Potential Canonical 6 (TRPC6) channel, a non-selective cation channel that mediates calcium influx in response to various stimuli. TRPC6 is involved in multiple physiological processes including smooth muscle contraction, neuronal excitability, and immune cell function. The compound also shows activity against TRPC3.
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| ln Vitro |
Compound 4o, TRPC6-IN-1, demonstrated concentration-dependent growth in TRPC6 cells, with an average EC50 value of 4.66±0.03 μM suggesting that the compound's anti-TRPC6 action was equivalent to that of the original lead chemical. Additionally, TRPC6-IN-1 was examined in HEK293 cells that also expressed TRPC4β, a subtype of TRPC channels distinct from TRPC3/6/7, and the mu opioid receptor (MOR). μ agonist activation resulted in a considerable rise in the [Ca2+]i of these cells. Additionally, in HEK293 cells expressing human TRPC3, TRPC6-IN-1 produced whole-cell currents. In TRPC7 cells, TRPC6-IN-1 increases current in a concentration-dependent manner. Despite using low Ca2+ (0.1 mM) bath solutions, currents at high TRPC6-IN-1 concentrations (10 and 30 μM) demonstrated some degree of desensitization at both negative and positive potentials, in contrast to TRPC6. However, it was found that at less than 10 μM TRPC6-IN-1, TRPC7 current increased gradually[1].
In vitro, TRPC6-IN-1 demonstrates concentration-dependent inhibition of TRPC6 activity. It has an EC50 of 4.66 µM in TRPC6-expressing cells. The compound's anti-TRPC6 action is equivalent to that of the original lead chemical. It also shows activity against TRPC3 with an EC50 of 0.45 µM. |
| ln Vivo |
In vivo activity data for TRPC6-IN-1 are limited, as the compound is primarily used as a research tool for in vitro calcium signaling studies. TRPC6 channels are involved in various physiological processes, and inhibition of TRPC6 may have therapeutic potential in conditions such as cardiovascular disease and neurological disorders. Further in vivo studies are needed.
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| Enzyme Assay |
In vitro channel inhibition assays for TRPC6-IN-1 are performed using cells expressing TRPC6 channels. Calcium influx is measured using fluorescence-based calcium indicators such as Fura-2 or Fluo-4. Cells are treated with increasing concentrations of the compound, and the EC50 (4.66 µM) is calculated from the inhibition curve. These assays provide quantitative data on the compound's potency.
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| Cell Assay |
In vitro cellular assays for TRPC6-IN-1 are performed using cells expressing TRPC6 channels. Cells are treated with the compound, and calcium influx is measured using fluorescence-based calcium indicators. The EC50 value (4.66 µM) is determined from concentration-response curves. These assays characterize the compound's inhibitory activity at TRPC6 channels.
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| Animal Protocol |
In vivo animal experimental protocols for TRPC6-IN-1 are not extensively documented in the available literature. As a research compound, in vivo studies would typically involve administration to animal models to study the role of TRPC6 channels in various physiological processes. The compound would be administered via appropriate routes.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of TRPC6-IN-1 have not been systematically characterized. The compound has a molecular weight of 398.43 and molecular formula C21H23FN4O3. It is soluble in DMSO. Further PK studies are needed to determine its absorption, distribution, metabolism, and excretion profile.
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| Toxicity/Toxicokinetics |
Toxicological data for TRPC6-IN-1 are not extensively reported. As a research-use compound, its safety profile has not been formally evaluated in comprehensive toxicology studies. The compound is intended for research purposes only. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
4-[3-(4-fluorophenyl)-2-methyl-7-oxo-1H-pyrazolo[1,5-a]pyrimidin-5-yl]-1-piperidinecarboxylic acid ethyl ester is a cyclic compound belonging to the pyrazole class of compounds.
TRPC6-IN-1 (compound 4o) is a TRPC6 channel inhibitor with CAS number 901715-05-7, molecular formula C21H23FN4O3, and molecular weight 398.43. It has an EC50 of 4.66 µM in TRPC6-expressing cells and also shows activity against TRPC3 (EC50: 0.45 µM). It is used as a pharmacological tool for investigating TRPC channel function and calcium signaling. |
| Molecular Formula |
C21H23FN4O3
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|---|---|
| Molecular Weight |
398.430728197098
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| Exact Mass |
398.175
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| CAS # |
901715-05-7
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| PubChem CID |
5308428
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
775
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N1CCC(C2C=C(O)N3C(=C(C(C)=N3)C3C=CC(F)=CC=3)N=2)CC1)OCC
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| InChi Key |
OXPMSNBGJOEGSC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H23FN4O3/c1-3-29-21(28)25-10-8-14(9-11-25)17-12-18(27)26-20(23-17)19(13(2)24-26)15-4-6-16(22)7-5-15/h4-7,12,14,24H,3,8-11H2,1-2H3
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| Chemical Name |
ethyl 4-[3-(4-fluorophenyl)-2-methyl-7-oxo-1H-pyrazolo[1,5-a]pyrimidin-5-yl]piperidine-1-carboxylate
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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 (~250.99 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.22 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 (5.22 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (5.22 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 | 2.5099 mL | 12.5493 mL | 25.0985 mL | |
| 5 mM | 0.5020 mL | 2.5099 mL | 5.0197 mL | |
| 10 mM | 0.2510 mL | 1.2549 mL | 2.5099 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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