| Size | Price | Stock | Qty |
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| 5mg |
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| 25mg |
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Purity: ≥98%
SAR7334 is a novel, potent and orally bioavailable inhibitor of TRPC6 channels that opens new opportunities for the investigation of TRPC channel function in vivo. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected.
| ln Vitro |
SAR7334 prevents Ca2+ influx into cells mediated by TRPC6, TRPC3, and TRPC7, with IC50 values of 9.5, 282, and 226 nM, respectively[1][2][3]. It has no effect on Ca2+ influx mediated by TRPC4 and TRPC5. In podocytes, Ang II-induced calcium influx is significantly blocked by SAR7334 (1 μM) [1]. The impact of SAR7334 (1 μM) on SOCE is minimal [2]. TRPC6 current is dose-dependently reduced by SAR7334, with an IC50 of 7.9 nM. The current of TRPC6 is significantly reduced by SAR7334 (100 nM) [3].
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| ln Vivo |
In isolated perfused mouse lungs, SAR7334 (10 mg/kg, orally) suppresses TRPC6-dependent acute HPV. Its appropriateness for long-term oral administration is demonstrated by SAR7334. SAR7334 did not change the mean arterial pressure in spontaneously hypertensive rats (SHR) in an initial short-term trial [3].
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| 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.
[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 |
| Molecular Formula |
C21H24CL3N3O
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|---|---|
| Molecular Weight |
440.794
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| CAS # |
1333207-63-8
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| Related CAS # |
SAR7334;1333210-07-3
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| SMILES |
N#CC1=CC=C(O[C@H]2[C@H](N3C[C@H](N)CCC3)CC4=C2C=CC=C4)C(Cl)=C1.[H]Cl.[H]Cl
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| InChi Key |
LFMYIKNZNTZSJX-IQJQELQDSA-N
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| InChi Code |
InChI=1S/C21H22ClN3O.2ClH/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,3,5,9,11,13,24H22*1H/t16-,19-,21-/m1../s1
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| Chemical Name |
4-[[(1R,2R)-2-[(3R)-3-Amino-1-piperidinyl]-2,3-dihydro-1H-inden-1-yl]oxy]-3-chlorobenzonitrile dihydrochloride
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| Synonyms |
SAR-7334 SAR 7334 SAR7334. SAR-7334 HCl, SAR-7334 hydrochloride
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~226.87 mM)
H2O : ~50 mg/mL (~113.43 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.67 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 25.0 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: ≥ 2.5 mg/mL (5.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 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: ≥ 2.5 mg/mL (5.67 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 | 2.2687 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 |
*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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