Pyr3 - CAS 1160514-60-2
Category: Inhibitor
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TRP Channel
Pyr3, a pyrazole derivative, is a selective antagonist of the TRP canonical 3 channel (TRPC3) which can function as a receptor-operated channel. It inhibits TRPC3-mediated Ca2+ influx with an IC50 value of 0.7 μM without effect on other TRPC members and suppresses activation of nuclear factor of activated T cells with an IC50 value of 0.05 μM.
≥98% by HPLC
Off-White to Pale Yellow Solid
Pyr3; Pyr-3; Pyr 3; 1-[4-[(2,3,3-Trichloro-1-oxo-2-propen-1-yl)amino]phenyl]-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid
Store in a cool and dry place (or refer to the Certificate of Analysis).
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1.Excitation and modulation of TRPA1, TRPV1, and TRPM8 channel-expressing sensory neurons by the pruritogen chloroquine.
Than JY;Li L;Hasan R;Zhang X J Biol Chem. 2013 May 3;288(18):12818-27. doi: 10.1074/jbc.M113.450072. Epub 2013 Mar 18.
The sensations of pain, itch, and cold often interact with each other. Pain inhibits itch, whereas cold inhibits both pain and itch. TRPV1 and TRPA1 channels transduce pain and itch, whereas TRPM8 transduces cold. The pruritogen chloroquine (CQ) was reported to excite TRPA1, leading to the sensation of itch. It is unclear how CQ excites and modulates TRPA1(+), TRPV1(+), and TRPM8(+) neurons and thus affects the sensations of pain, itch, and cold. Here, we show that only 43% of CQ-excited dorsal root ganglion neurons expressed TRPA1; as expected, the responses of these neurons were completely prevented by the TRPA1 antagonist HC-030031. The remaining 57% of CQ-excited neurons did not express TRPA1, and excitation was not prevented by either a TRPA1 or TRPV1 antagonist but was prevented by the general transient receptor potential canonical (TRPC) channel blocker BTP2 and the selective TRPC3 inhibitor Pyr3. Furthermore, CQ caused potent sensitization of TRPV1 in 51.9% of TRPV1(+) neurons and concomitant inhibition of TRPM8 in 48.8% of TRPM8(+) dorsal root ganglion neurons. Sensitization of TRPV1 is caused mainly by activation of the phospholipase C-PKC pathway following activation of the CQ receptor MrgprA3.
2.Mechanistic insights into the detection of free fatty and bile acids by ileal glucagon-like peptide-1 secreting cells.
Goldspink DA;Lu VB;Billing LJ;Larraufie P;Tolhurst G;Gribble FM;Reimann F Mol Metab. 2018 Jan;7:90-101. doi: 10.1016/j.molmet.2017.11.005. Epub 2017 Nov 11.
OBJECTIVES: ;The aim of this study was to investigate the electrical properties of ileal Glucagon-like peptide 1 (GLP-1) secreting L-cells using murine organoid cultures and the electrophysiological and intracellular signaling pathways recruited following activation of the G;αq;-coupled free fatty acid receptors FFA1 and G;αs;-coupled bile acid receptors GPBAR1.;METHODS: ;Experiments were performed using ileal organoids generated from mice transgenically expressing fluorescent reporters (Epac2-camps and GCaMP3) under control of the proglucagon promoter. Electrophysiology and single cell imaging were performed on identified L-cells in organoids, and GLP-1 secretion from cultured organoids was measured by immunoassay.;RESULTS: ;The FFA1 ligand TAK-875 triggered L-cell electrical activity, increased intracellular calcium, and activated a depolarizing current that was blocked by the TRPC3 inhibitor Pyr3. TAK-875 triggered GLP-1 secretion was Pyr3 sensitive, suggesting that the TRPC3 channel links FFA1 activation to calcium elevation and GLP-1 release in L-cells. GPBAR1 agonist triggered PKA-dependent L-type Ca;2+; current activation and action potential firing in L-cells. The combination of TAK-875 and a GPBAR1 agonist triggered synergistic calcium elevation and GLP-1 secretory responses.
3.Transient receptor potential cation 3 channel regulates melanoma proliferation and migration.
Oda K;Umemura M;Nakakaji R;Tanaka R;Sato I;Nagasako A;Oyamada C;Baljinnyam E;Katsumata M;Xie LH;Narikawa M;Yamaguchi Y;Akimoto T;Ohtake M;Fujita T;Yokoyama U;Iwatsubo K;Aihara M;Ishikawa Y J Physiol Sci. 2017 Jul;67(4):497-505. doi: 10.1007/s12576-016-0480-1. Epub 2016 Sep 9.
Melanoma has an extremely poor prognosis due to its rapidly progressive and highly metastatic nature. Several therapeutic drugs have recently become available, but are effective only against melanoma with specific BRAF gene mutation. Thus, there is a need to identify other target molecules. We show here that Transient receptor potential, canonical 3 (TRPC3) is widely expressed in human melanoma. We found that pharmacological inhibition of TRPC3 with a pyrazole compound, Pyr3, decreased melanoma cell proliferation and migration. Similar inhibition was observed when the TRPC3 gene was silenced with short-hairpin RNA (shRNA). Pyr3 induced dephosphorylation of signal transducer and activator of transcription (STAT) 5 and Akt. Administration of Pyr3 (0.05 mg/kg) to mice implanted with human melanoma cells (C8161) significantly inhibited tumor growth. Our findings indicate that TRPC3 plays an important role in melanoma growth, and may be a novel target for treating melanoma in patients.
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