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Pyr3 {[allProObj[0].p_purity_real_show]}

货号:A1176630

Pyr3是选择性的 TRPC3 通道抑制剂,IC50 为 700 nM,能有效抑制 TRPC3 介导的钙离子流入,适用于研究细胞内钙信号传导通路。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Pyr3 化学结构 CAS号:1160514-60-2
Pyr3 化学结构
CAS号:1160514-60-2
Pyr3 3D分子结构
CAS号:1160514-60-2
Pyr3 化学结构 CAS号:1160514-60-2
Pyr3 3D分子结构 CAS号:1160514-60-2
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Pyr3 纯度/质量文件 产品仅供科研

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Pyr3 生物活性

描述 Pyr3 selectively and directly inhibits TRPC3 channels as follows: Pyr3 inhibits TRPC3-mediated Ca2+ influx in a dose-dependent manner with an IC50 value of 700 nM. The effect of Pyr3 becomes evident at 0.3 μM, while TRPC3 is almost completely inhibited at 3 μM. Interestingly, Pyr3 inhibited Ca2+ influx in cells expressing both TRPC3 and TRPC6, but not in cells expressing both TRPC1 and TRPC5. Pyr3 inhibited Ang II-induced NFAT translocation in a concentration-dependent manner with an IC50 value of 0.05 μM[1].

Pyr3 细胞实验

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.

Pyr3 动物实验

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

Pyr3 参考文献

[1]Kiyonaka S, et al. Selective and direct inhibition of TRPC3 channels underlies biological activities of a pyrazole compound. Proc Natl Acad Sci U S A. 2009 Mar 31;106(13):5400-5.

Pyr3 实验方案

计算器
存储液制备 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

Pyr3 技术信息

CAS号1160514-60-2
分子式C16H11Cl3F3N3O3
分子量 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
别名
运输蓝冰
InChI Key RZHGONNSASQOAY-UHFFFAOYSA-N
Pubchem ID 56964346
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 120 mg/mL(262.79 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
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