Pyr3 |
Catalog No.GC14649
One-Click Copy Product Info
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Pyr3 is a potent and selective inhibitor of transient receptor potential canonical channel 3 (TRPC3), with an IC50 of 700nM for TRPC3-mediated Ca2+ influx.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1160514-60-2
Sample solution is provided at 25 µL, 10mM.
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Pyr3 is a potent and selective inhibitor of transient receptor potential canonical channel 3 (TRPC3), with an IC50 of 700nM for TRPC3-mediated Ca2+ influx [1]. Pyr3 can reduce the secretion level of MMP9 in cells and inhibit the phosphorylation of signal transducer and activator of transcription (STAT) 5[2]. Pyr3 has been widely used to inhibit the proliferation and migration of melanoma, as well as to regulate tumor growth and metastasis[3].
In vitro, Pyr3 treatment for 48 hours significantly inhibited the proliferation of A549 cells, HCT-116 cells, and PC3 cells, with IC50 values of 15.4, 7.9, and 2.3μg/ml, respectively[4]. Treatment with 10μM Pyr3 for 24 hours significantly inhibited the viability of T24 cells, induced cell cycle arrest, and decreased the expression levels of p-PKCα, PKCα and PP2A[5]. Treatment with 1.0μM Pyr3 for 8 hours significantly induced apoptosis in MDA-MB-231 cells, accompanied by cell contraction, cell membrane blebbing, mitochondrial fragmentation and nuclear condensation[6].
In vivo, Pyr3 treatment via intraperitoneal injection at a dose of 20mg/kg/day for seven consecutive days significantly inhibited the growth of glioma tumors in the xenograft mouse model[7]. Five minutes before reperfusion, 10mg/kg of Pyr3 was administered via the right jugular vein to the mice, which significantly reduced the infarcted area of the left ventricle in the mice, and decreased the rate of myocardial cell apoptosis and inflammatory response[8].
References:
[1] Kiyonaka S, Kato K, Nishida M, et al. Selective and direct inhibition of TRPC3 channels underlies biological activities of a pyrazole compound[J]. Proceedings of the National Academy of Sciences, 2009, 106(13): 5400-5405.
[2] Oda K, Umemura M, Katsumata M, et al. Transient receptor potential cation channel 3 (TRPC3) regulates tumor proliferation and migration of BRAF wild type human malignant melanoma[J]. Cancer Research, 2015, 75(15_Supplement): 4371-4371.
[3] Umemura M, Baljinnyam E, De Lorenzo M S, et al. Role of store-operated Ca2+ entry in proliferation and cell cycle in melanoma[J]. Cancer Research, 2012, 72(8_Supplement): 1864-1864.
[4] Kıyan H T, Üvez A, Erkisa M, et al. A Comparative Study on In vitro Anti-cancer and In vivo Anti-angiogenic Effects of TRPC Blockers Pyr-3 and SKF-96365[J]. Letters in Drug Design & Discovery, 2023, 20(7): 957-964.
[5] Ting H K, Dou Y C, Lin Y H, et al. Pyr3 inhibits cell viability and PKCα activity to suppress migration in human bladder cancer cells[J]. European Journal of Pharmacology, 2025, 988: 177235.
[6] Wang Y, Qi Y X, Qi Z, et al. TRPC3 regulates the proliferation and apoptosis resistance of triple negative breast cancer cells through the TRPC3/RASA4/MAPK pathway[J]. Cancers, 2019, 11(4): 558.
[7] Chang H H, Cheng Y C, Tsai W C, et al. Pyr3 induces apoptosis and inhibits migration in human glioblastoma cells[J]. Cellular Physiology and Biochemistry, 2018, 48(4): 1694-1702.
[8] Lu M, Fang X, Shi D, et al. A selective TRPC3 inhibitor Pyr3 attenuates myocardial ischemia/reperfusion injury in mice[J]. Current Medical Science, 2020, 40(6): 1107-1113.
| Cell experiment [1]: | |
Cell lines | A549 cells |
Preparation Method | A549 cells were grown in RPMI 1640 medium supplemented with penicillin G (100U/ml), streptomycin (100μg/ml), L-glutamine, and 10% fetal bovine serum in a humidified incubator at 37°C and 5% CO2. Cells were seeded at a density of 5×103 cells/well in 96 well plates and treated with different concentrations of Pyr3 (0.62, 1.25, 2.5, 5, 10, 20, and 40µg/ml) for 48h. Then, cells were in situ fixed with 50μl of 50% (w/v) trichloroacetic acid at 4°C for 1h. At the end of fixation, wells were washed 5 times with deionized water and allowed air dry at room temperature for 50μl of 0.4% SRB solution was added into each well and incubated at room temperature for 30min. Then, plates were washed with 1% acetic acid to eliminate non-specific bindings and un bounded dye. The bounded SRB dye was dissolved by adding 150μl 10mM Tris base per each well. Measurements were carried out at 564nm. |
Reaction Conditions | 0.62, 1.25, 2.5, 5, 10, 20, and 40µg/ml; 48h |
Applications | Pyr3 treatment notably decreased the cell viability of A549 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | BALB/cAnN.Cg-Foxn1nu/CrlNarl nude mice |
Preparation Method | BALB/cAnN.Cg-Foxn1nu/CrlNarl nude mice (20-25g) were anesthetized with an oxygen/isoflurane mixture gas. Subsequently, 1×105 LN229-Luc2 cells were implanted into the right cerebral hemisphere of the mice. Four days after implantation, the mice were randomly divided into four groups and received treatment with a vector control, or Pyr3. Pyr3 was dissolved in 10% Tween 80 and administered intraperitoneally at a dose of 20mg/kg/day for 7 days. Twelve days later, the mice were euthanized with carbon dioxide; the brain tissues were removed, fixed with formalin, embedded in paraffin, and cut into consecutive sections. The bioluminescence intensity of the implanted tumors was monitored using the non-invasive in vivo imaging system (IVIS) three times a week. The weight of the mice was measured three times a week. |
Dosage form | 20mg/kg/day for 7 days; i.p. |
Applications | Pyr3 treatment inhibited glioma tumor growth in the xenograft orthotopic model without affecting body weight. |
References: | |
| Cas No. | 1160514-60-2 | SDF | |
| Chemical Name | ethyl 1-(4-(2,3,3-trichloroacrylamido)phenyl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylate | ||
| Canonical SMILES | Cl/C(C(NC1=CC=C(C=C1)N2N=CC(C(OCC)=O)=C2C(F)(F)F)=O)=C(Cl)\Cl | ||
| Formula | C16H11Cl3F3N3O3 | M.Wt | 456.63 |
| Solubility | DMF: 50 mg/ml,DMSO: 20 mg/ml,Ethanol: 10 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.19 mL | 10.9498 mL | 21.8996 mL |
| 5 mM | 438 μL | 2.19 mL | 4.3799 mL |
| 10 mM | 219 μL | 1.095 mL | 2.19 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)