TRPC6 inhibitorCAS# 1333207-63-8 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1333207-63-8 | SDF | Download SDF |
| PubChem ID | 53378752 | Appearance | Powder |
| Formula | C21H24Cl3N3O | M.Wt | 440.79 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Rezulin;CS-045;Noscal,SAR 7334 | ||
| Solubility | Soluble in DMSO | ||
| Chemical Name | 4-[[(1R,2R)-2-[(3R)-3-aminopiperidin-1-yl]-2,3-dihydro-1H-inden-1-yl]oxy]-3-chlorobenzonitrile | ||
| SMILES | C1CC(CN(C1)C2CC3=CC=CC=C3C2OC4=C(C=C(C=C4)C#N)Cl)N | ||
| Standard InChIKey | RLKRLNQEXBPQGQ-OZOXKJRCSA-N | ||
| Standard InChI | InChI=1S/C21H22ClN3O/c22-18-10-14(12-23)7-8-20(18)26-21-17-6-2-1-4-15(17)11-19(21)25-9-3-5-16(24)13-25/h1-2,4,6-8,10,16,19,21H,3,5,9,11,13,24H2/t16-,19-,21-/m1/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent TRPC6 inhibitor (IC50 values are 9.5, 226 and 282 nM for TRPC6, TRPC7 and TRPC3-mediated Ca2+ influx). Exhibits no significant activity at TRPC4 and TRPC5 channels. Suppresses TRPC6-dependent acute hypoxic pulmonary vasoconstriction (HPV) in the isolated perfused mouse lung. Orally bioavailable. |
TRPC6 inhibitor Dilution Calculator
TRPC6 inhibitor Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2687 mL | 11.3433 mL | 22.6865 mL | 45.3731 mL | 56.7164 mL |
| 5 mM | 0.4537 mL | 2.2687 mL | 4.5373 mL | 9.0746 mL | 11.3433 mL |
| 10 mM | 0.2269 mL | 1.1343 mL | 2.2687 mL | 4.5373 mL | 5.6716 mL |
| 50 mM | 0.0454 mL | 0.2269 mL | 0.4537 mL | 0.9075 mL | 1.1343 mL |
| 100 mM | 0.0227 mL | 0.1134 mL | 0.2269 mL | 0.4537 mL | 0.5672 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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TRPC6 inhibitor is a potent TRPC6(Transient receptor potential cation channel, subfamily C, member 6) inhibitor.
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Identification and Validation of Larixyl Acetate as a Potent TRPC6 Inhibitor.[Pubmed:26500253]
Mol Pharmacol. 2016 Jan;89(1):197-213.
Classical or canonical transient receptor potential 6 (TRPC6), a nonselective and Ca(2+)-permeable cation channel, mediates pathophysiological responses within pulmonary and renal diseases that are still poorly controlled by current medication. Thus, controlling TRPC6 activity may provide a promising and challenging pharmacological approach. Recently identified chemical entities have demonstrated that TRPC6 is pharmacologically targetable. However, isotype-selectivity with regard to its closest relative, TRPC3, is difficult to achieve. Reasoning that balsams, essential oils, or incense materials that are traditionally used for inhalation may contain biologic activities to block TRPC6 activity, we embarked on a natural compound strategy to identify new TRPC6-blocking chemical entities. Within several preparations of plant extracts, a strong TRPC6-inhibitory activity was found in conifer balsams. The biologic activity was associated with nonvolatile resins, but not with essential oils. Of various conifers, the larch balsam was unique in displaying a marked TRPC6-prevalent mode of action. By testing the main constituents of larch resin, we identified larixol and larixyl acetate as blockers of Ca(2+) entry and ionic currents through diacylglycerol- or receptor-activated recombinant TRPC6 channels, exhibiting approximately 12- and 5-fold selectivity compared with its closest relatives TRPC3 and TRPC7, respectively. No significant inhibition of more distantly related TRPV or TRPM channels was seen. The potent inhibition of recombinant TRPC6 by larixyl acetate (IC50 = 0.1-0.6 microM) was confirmed for native TRPC6-like [Ca(2+)]i signals in diacylglycerol-stimulated rat pulmonary artery smooth muscle cells. In isolated mouse lungs, larix-6-yl monoacetate (CAS 4608-49-5; larixyl acetate; 5 microM) prevented acute hypoxia-induced vasoconstriction. We conclude that larch-derived labdane-type diterpenes are TRPC6-selective inhibitors and may represent a starting point for pharmacological TRPC6 modulation within experimental therapies.
