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Chemical Structure| 1333210-07-3 Chemical Structure| 1333210-07-3

Structure of SAR7334
CAS No.: 1333210-07-3

Chemical Structure| 1333210-07-3

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

Synonyms: CPA-1588

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Product Details of SAR7334

CAS No. :1333210-07-3
Formula : C21H22ClN3O
M.W : 367.87
SMILES Code : N#CC1=CC=C(O[C@H]2[C@H](N3C[C@H](N)CCC3)CC4=C2C=CC=C4)C(Cl)=C1
Synonyms :
CPA-1588
MDL No. :MFCD27992059
InChI Key :RLKRLNQEXBPQGQ-OZOXKJRCSA-N
Pubchem ID :53378752

Safety of SAR7334

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Cardiac fibroblasts 1 µM 10 minutes To evaluate the effect of SAR7334 on AngII-induced Ca2+ release and Ca2+ entry, results showed that SAR7334 had no significant effect on AngII-induced Ca2+ signaling Cells. 2020 Jan 29;9(2):322.
Rat podocytes 1 µM 10 minutes SAR7334 significantly blocked the Ang II–evoked calcium transient Sci Rep. 2017 Mar 22;7(1):299.
Human aortic smooth muscle cells 100 nM 12 hours To evaluate the effect of SAR7334 on the migration of human aortic smooth muscle cells, results showed that SAR7334 significantly reduced cell migration. Eur Heart J. 2021 May 7;42(18):1773-1785.
HK-2 cells 20–100 nM 12 hours SAR7334 promotes autophagic flux by inhibiting TRPC6 and mitigates oxidative stress-induced apoptosis of PTC. Cell Death Dis. 2018 Oct 3;9(10):1015.
MPC5 podocytes 1 µM 30 minutes To investigate the regulatory effect of SAR7334 on the Ang Ⅱ-TRPC6 signaling axis, results showed that SAR7334 could block the overexpression of TRPC6, AT1R, and Caspase-3, attenuate the degradation of podocyte structural proteins, and inhibit intracellular calcium fluorescence intensity and cell apoptosis. Front Pharmacol. 2022 Aug 3;13:915153.
TRPC6-HEK-FITR cells 9.5 nM To evaluate the inhibitory effect of SAR7334 on TRPC6-mediated Ca2+ influx, results showed that SAR7334 effectively inhibited TRPC6 channels. Br J Pharmacol. 2015 Jul;172(14):3650-60.
TRPC3-CHO cells 282 nM To evaluate the inhibitory effect of SAR7334 on TRPC3-mediated Ca2+ influx, results showed that SAR7334 had a weaker inhibitory effect on TRPC3 channels. Br J Pharmacol. 2015 Jul;172(14):3650-60.
TRPC7-HEK-FITR cells 226 nM To evaluate the inhibitory effect of SAR7334 on TRPC7-mediated Ca2+ influx, results showed that SAR7334 had a weaker inhibitory effect on TRPC7 channels. Br J Pharmacol. 2015 Jul;172(14):3650-60.
Wild type, RYR1-p.G2435R heterozygous, and RYR1-p.G2435R homozygous flexor digitorum brevis muscle fibers 1 µM SAR7334 significantly reduced the resting intracellular calcium concentration in wildtype, RYR1-p.G2435R heterozygous, and RYR1-p.G2435R homozygous muscle fibers and prevented the elevation of intracellular calcium concentration induced by 1-oleoyl-2-acetyl-sn-glycerol. Anesthesiology. 2020 Aug;133(2):364-376.
Wild type, RYR1-p.G2435R heterozygous, and RYR1-p.G2435R homozygous myotubes 250 nM SAR7334 significantly decreased the median manganese quench rate in heterozygous and homozygous RYR1-p.G2435R myotubes, indicating that SAR7334 can block TRPC3/6-mediated cation influx. Anesthesiology. 2020 Aug;133(2):364-376.
Hippocampal neurons 1 µM SAR7334 significantly reduced the [Ca2+]i in MH-R163C neurons and increased their glucose uptake, while it had no significant effect on the glucose uptake in WT neurons. Cells. 2024 Nov 15;13(22):1888.
Hippocampal pyramidal neurons 0.1 or 1 µM SAR7334 reduced [Ca2+]r in all age groups in a dose-dependent manner; however, the effect of SAR7334 was greater with increasing age. Front Aging Neurosci. 2020 Jul 16;12:224.
WT VSMCs 1 µM SAR7334 significantly reduced [Ca2+]i in WT VSMCs from 123 ± 3 nM to 100 ± 6 nM and decreased the hypoxia-induced elevation of [Ca2+]i. Biomedicines. 2023 Feb 19;11(2):623.
Mdx VSMCs 1 µM SAR7334 significantly reduced [Ca2+]i in mdx VSMCs from 285 ± 31 nM to 154 ± 15 nM and decreased the hypoxia-induced elevation of [Ca2+]i. Biomedicines. 2023 Feb 19;11(2):623.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice RYR1-p.G2435R homozygous mice Local administration 1 μM Single dose, 10 minutes SAR7334 significantly reduced the resting intracellular calcium concentration in RYR1-p.G2435R homozygous mice and partially inhibited the elevation of intracellular calcium concentration induced by halothane inhalation. Anesthesiology. 2020 Aug;133(2):364-376.
C57/BL6N mice Acute hypoxic pulmonary vasoconstriction model Lung perfusion 100 nM Single administration To evaluate the inhibitory effect of SAR7334 on acute hypoxic pulmonary vasoconstriction, results showed that SAR7334 effectively inhibited hypoxic pulmonary vasoconstriction. Br J Pharmacol. 2015 Jul;172(14):3650-60.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.72mL

0.54mL

0.27mL

13.59mL

2.72mL

1.36mL

27.18mL

5.44mL

2.72mL

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