1. Membrane Transporter/Ion Channel
  2. TRP Channel

SAR7334 hydrochloride 

Cat. No.: HY-15699A Purity: 95.30%
Handling Instructions

SAR7334 hydrochloride is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.

For research use only. We do not sell to patients.
SAR7334 hydrochloride Chemical Structure

SAR7334 hydrochloride Chemical Structure

CAS No. : 1333207-63-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 370 In-stock
5 mg USD 336 In-stock
10 mg USD 420 In-stock
50 mg USD 780 In-stock
100 mg USD 960 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of SAR7334 hydrochloride:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

SAR7334 hydrochloride is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.

IC50 & Target

IC50: 7.9 nM (TRPC6 currents)[3]

In Vitro

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].

In Vivo

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].

References
Preparing Stock Solutions
Concentration Volume Mass 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
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[3]

SAR7334 is formulated in saline.

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

440.79

Formula

C₂₁H₂₄Cl₃N₃O

CAS No.

1333207-63-8

SMILES

N[[email protected]@H](C1)CCCN1[[email protected]@H]2CC3=CC=CC=C3[[email protected]]2OC4=CC=C(C#N)C=C4Cl.Cl.Cl

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
SAR7334 hydrochloride
Cat. No.:
HY-15699A
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