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SKU | Size | Availability | Price | Qty |
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T646512-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $480.90 | |
T646512-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $800.90 | |
T646512-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,700.90 | |
T646512-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,800.90 | |
T646512-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $4,200.90 |
Specifications & Purity | ≥99% |
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Biochemical and Physiological Mechanisms | TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC 50 of 4.66 μM. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC 50 of 4.66 μM. In Vitro TRPC6-IN-1 (compound 4o) rises in the TRPC6 cells in a concentration dependent manner, with a mean EC 50 value of 4.66±0.03 μM, demonstrating a comparable activity of the compound on TRPC6 as the original lead. TRPC6-IN-1 is also tested on HEK293 cells that co-expressed μ opioid receptor (MOR) and TRPC4β, which belongs to a different subgroup of TRPC channels than TRPC3/6/7. Upon stimulation by a μ agonist, these cells show a robust increase in [Ca 2+ ] i . TRPC6-IN-1 also evokes whole-cell currents in HEK293 cells that express human TRPC3. TRPC6-IN-1 elicits concentration dependent current increases in the TRPC7 cells. Different from TRPC6, the currents show some desensitization in the high TRPC6-IN-1 concentrations (10 and 30 μM) at both negative and positive potentials even though the low Ca 2+ (0.1 mM) bath solution is used. Nonetheless, a stepwise increase in the TRPC7 currents is still detected at <10 μM TRPC6-IN-1. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:EC50: 0.45 μM (TRPC3), 1.13 μM (TRPC7), 4.66 μM(TRPC3) |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC 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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INCHI | 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 |
InChi Key | OXPMSNBGJOEGSC-UHFFFAOYSA-N |
Canonical SMILES | CCOC(=O)N1CCC(CC1)C2=CC(=O)N3C(=N2)C(=C(N3)C)C4=CC=C(C=C4)F |
Isomeric SMILES | CCOC(=O)N1CCC(CC1)C2=CC(=O)N3C(=N2)C(=C(N3)C)C4=CC=C(C=C4)F |
PubChem CID | 5308428 |
Molecular Weight | 398.43 |
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Solubility | DMSO : 100 mg/mL (250.99 mM; Need ultrasonic) |
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