| 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 |
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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].
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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 ring assembly and a member of pyrazoles.
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| 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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