TRPC6 inhibitor |
| カタログ番号GC13218 |
TRPC6 阻害剤は強力で特異的な TRPC6 阻害剤であり、7.9 nM の IC50 で TRPC6 電流を阻害します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1333207-63-8
Sample solution is provided at 25 µL, 10mM.
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SAR7334 hydrochloride is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.
SAR7334 inhibits TRPC6, TRPC3 and TRPC7-mediated Ca2+ influx into cells with IC50s of 9.5, 282 and 226 nM[1][2][3], whereas TRPC4 and TRPC5-mediated Ca2+ entry is not affected. SAR7334 (1 μM) results in a major block of the Ang II-evoked calcium influx in the podocytes[1]. SAR7334 (1 μM) has negligible effect on SOCE[2]. SAR7334 dose-dependently reduces TRPC6 currents with an IC50 of 7.9 nM. SAR7334 (100 nM) substantially reduces TRPC6 currents[3].
SAR7334 (10 mg/kg, p.o.) suppresses TRPC6-dependent acute HPV in isolated perfused lungs from mice. SAR7334 demonstrates that it is suitable for chronic oral administration. In an initial short-term study, SAR7334 does not change mean arterial pressure in spontaneously hypertensive rats (SHR)[3].
[1]. Ilatovskaya DV, et al. The Role of Angiotensin II in Glomerular Volume Dynamics and Podocyte Calcium Handling. Sci Rep. 2017 Mar 22;7(1):299.
[2]. Chauvet S, et al. Pharmacological Characterization of the Native Store-Operated Calcium Channels of Cortical Neurons from Embryonic Mouse Brain. Front Pharmacol. 2016 Dec 12;7:486.
[3]. Maier T, et al. Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels. Br J Pharmacol. 2015 Jul;172(14):3650-60.
Animal experiment: | Adult male (6 months old) spontaneously hypertensive rats (SHR) are treated on two consecutive days. On day one, the animals receive 1 mL/kg vehicle by oral gavage. After 24 h, rats receive either vehicle alone or are treated with 10 mg/kg SAR7334. Telemetric measurement of BP is performed. In brief, a telemetric device (TL11M2-C50-PXT PMP) is placed between the aorta and the vena cava and the catheter tip of the transmitter is inserted into the aorta. Systolic BP, diastolic BP and heart rate are acquired continuously at a sampling rate of 500 Hz and data are stored as 5 min averages. Mean arterial pressure is calculated from systolic and diastolic pressure and low-pass filtered using the fast Fourier transform function of the vendor software for better visualization of time-dependent BP variations. For statistical analysis, raw data are averaged over a 6 h period starting 2 h after application of vehicle or SAR7334. This interval corresponds to the maximal plasma levels of SAR7334. Baseline data are sampled over the same time interval on the day before treatment. |
References: [1]. Ilatovskaya DV, et al. The Role of Angiotensin II in Glomerular Volume Dynamics and Podocyte Calcium Handling. Sci Rep. 2017 Mar 22;7(1):299. | |
| Cas No. | 1333207-63-8 | SDF | |
| Chemical Name | 4-(((1R,2R)-2-((R)-3-aminopiperidin-1-yl)-2,3-dihydro-1H-inden-1-yl)oxy)-3-chlorobenzonitrile dihydrochloride | ||
| Canonical SMILES | ClC1=C(O[C@]2([H])C3=CC=CC=C3C[C@@]2([H])N4CCC[C@](N)([H])C4)C=CC(C#N)=C1.Cl.Cl | ||
| Formula | C21H24Cl3N3O | M.Wt | 440.79 |
| 溶解度 | DMF: 1 mg/mL,DMSO: 15 mg/mL,Ethanol: 25 mg/mL,Ethanol:PBS (pH 7.2) (1:5): 0.16mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2687 mL | 11.3433 mL | 22.6865 mL |
| 5 mM | 0.4537 mL | 2.2687 mL | 4.5373 mL |
| 10 mM | 0.2269 mL | 1.1343 mL | 2.2687 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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