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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 PMC7072683
rat podocytes 1 µM 10 minutes SAR7334 significantly blocked the Ang II–evoked calcium transient PMC5428415
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. PMC8104955
HK-2 cells 20–100 nM 12 hours SAR7334 promotes autophagic flux by inhibiting TRPC6 and mitigates oxidative stress-induced apoptosis of PTC. PMC6170481
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. PMC9382118
TRPC6-HEK-FITR cells 9.5 nM 未指定 To evaluate the inhibitory effect of SAR7334 on TRPC6-mediated Ca2+ influx, results showed that SAR7334 effectively inhibited TRPC6 channels. PMC4507166
TRPC3-CHO cells 282 nM 未指定 To evaluate the inhibitory effect of SAR7334 on TRPC3-mediated Ca2+ influx, results showed that SAR7334 had a weaker inhibitory effect on TRPC3 channels. PMC4507166
TRPC7-HEK-FITR cells 226 nM 未指定 To evaluate the inhibitory effect of SAR7334 on TRPC7-mediated Ca2+ influx, results showed that SAR7334 had a weaker inhibitory effect on TRPC7 channels. PMC4507166
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. PMC7367496
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. PMC7367496
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. PMC11592500
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. PMC7378956
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. PMC9953629
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. PMC9953629

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. PMC7367496
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. PMC4507166

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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