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Chemical Structure| 1160514-60-2 Chemical Structure| 1160514-60-2

Structure of Pyr3
CAS No.: 1160514-60-2

Chemical Structure| 1160514-60-2

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Pyr3 is a selective TRPC3 channel inhibitor with an IC50 of 700 nM, effectively blocking TRPC3-mediated calcium influx, suitable for studying intracellular calcium signaling pathways.

4.5 *For Research Use Only! Not for Human Use. We Do Not Sell to Patients.

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Product Details of Pyr3

CAS No. :1160514-60-2
Formula : C16H11Cl3F3N3O3
M.W : 456.63
SMILES Code : O=C(C(Cl)=C(Cl)Cl)NC1=CC=C(C=C1)N2N=CC(C(OCC)=O)=C2C(F)(F)F
English Name :Ethyl 1-(4-(2,3,3-trichloroacrylamido)phenyl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylate
MDL No. :MFCD00178741
InChI Key :RZHGONNSASQOAY-UHFFFAOYSA-N
Pubchem ID :56964346

Safety of Pyr3

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MDA-MB-231 1.0 µM 120 hours Blocking TRPC3 attenuated the proliferation of MDA-MB-231 cells and increased the percentage of cells in the sub-G1 phase. Cancers (Basel). 2019 Apr 18;11(4):558
Submandibular gland acini 3 µM 30 min Pyr3 inhibited carbachol-induced autophagy and mistargeting of secretory granules. Gastroenterology. 2011 Jun;140(7):2107-15, 2115. e1-4
NT2/D1 cells 3 µM 72 hours TRPC3 inhibition induced a dose-dependent reduction in cell proliferation, while cell adhesion remained unaffected. Front Cell Dev Biol. 2024 Feb 15;12:1337714
MDA-MB-231 0.5-1.0 µM 72 hours Blocking TRPC3 decreased the percentage of viable MDA-MB-231 cells in a concentration-dependent manner. Cancers (Basel). 2019 Apr 18;11(4):558
Mouse mesenteric artery endothelial cells 1 μM To validate the effect of Pyr3 on mouse mesenteric artery endothelial cells. Pyr3 significantly reduced the ACh-induced hyperpolarization amplitude. Cardiovasc Res. 2012 Sep 1;95(4):439-47.
Rat mesenteric artery endothelial cells 1 μM To investigate the role of TRPC3 channels in rat mesenteric artery endothelial cells. Pyr3 significantly reduced the ACh-induced hyperpolarization amplitude. Cardiovasc Res. 2012 Sep 1;95(4):439-47.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Acute pancreatitis model Intraperitoneal injection 0.1 μg/g Hourly for 4 times Pyr3 reduced plasma amylase content by about 50% and alleviated pancreatic edema and pathological changes. Gastroenterology. 2011 Jun;140(7):2107-15, 2115. e1-4
Mice TRPC3 knockout mice Intraluminal 1 μM Single dose To evaluate the effect of Pyr3 on endothelium-dependent hyperpolarization-mediated vasodilation in TRPC3 knockout mice. Results showed Pyr3 significantly attenuated ATP-stimulated endothelium-dependent hyperpolarization-mediated vasodilation. J Am Heart Assoc. 2014 Aug 20;3(4):e000913
Mice Hypertensive model (BPH mice) and normotensive control (BPN mice) Bath application 10 μM Not specified To investigate the vasodilatory effects of Pyr3 and Pyr10 on mesenteric arteries from BPN and BPH mice, finding that BPN arteries showed a larger vasodilatory response to Pyr3 and Pyr10. J Physiol. 2017 Mar 1;595(5):1497-1513
Mice XY mouse gonads Ex vivo culture 3 µM 24-hour treatment followed by 24 and 48 hours of culture in fresh media Pyr3-treated XY gonads exhibited a substantial reduction in germ cell numbers (2.9-fold) when compared to control XY gonads, caused by reduced germ cell proliferation. Additionally, Pyr3-treated XY gonads showed a loss of the coelomic blood vessel due to increased apoptosis of endothelial cells after 72 hours of culture. Front Cell Dev Biol. 2024 Feb 15;12:1337714
Mice Pilocarpine-induced Status Epilepticus model Intraperitoneal injection 3 mg/kg Single dose Pyr3 selectively inhibits TRPC3 channels, significantly reducing the overall RMS power of pilocarpine-induced SE and selectively attenuating theta activity during SE. Epilepsia. 2017 Feb;58(2):247-254

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.19mL

0.44mL

0.22mL

10.95mL

2.19mL

1.09mL

21.90mL

4.38mL

2.19mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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