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2-Pyridinemethanol, α-[cis-3-hydroxy-3-methyl-1-[4-(trifluoromethyl)-2-pyridinyl]cyclobutyl]-, (αS)- manufacturers
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| | 2-Pyridinemethanol, α-[cis-3-hydroxy-3-methyl-1-[4-(trifluoromethyl)-2-pyridinyl]cyclobutyl]-, (αS)- Basic information |
| | 2-Pyridinemethanol, α-[cis-3-hydroxy-3-methyl-1-[4-(trifluoromethyl)-2-pyridinyl]cyclobutyl]-, (αS)- Chemical Properties |
| Boiling point | 447.8±45.0 °C(Predicted) | | density | 1.377±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO|33.83|100| | | pka | 13.36±0.20(Predicted) | | form | Solid | | color | White to off-white |
| | 2-Pyridinemethanol, α-[cis-3-hydroxy-3-methyl-1-[4-(trifluoromethyl)-2-pyridinyl]cyclobutyl]-, (αS)- Usage And Synthesis |
| Uses | TRPV3 antagonist 74a is a potent and selective TRPV3 antagonist. TRPV3 antagonist 74a displays no significant activity against a panel of other ion channels. TRPV3 antagonist 74a can be used for the research of neuropathic pain[1][2]. | | in vivo | TRPV3 antagonist 74a (150 μg; intradermal injection; 30 minutes) decreases the number of scratches significantly[2]. .
TRPV3 antagonist 74a (10~100 mg/kg; p.o.) dose-dependently attenuates mechanical allodynia induced by von Frey hair stimulation to the ipsilateral (injured) hind paw. TRPV3 antagonist 74a exhibits anti-nociceptive activity in the reserpine model of central pain by increasing muscle pressure threshold[1]. | Animal Model: | WT mice | | Dosage: | 150 μg | | Administration: | Intradermal injection; 30 minutes | | Result: | The number of scratches decreased significantly.
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| | IC 50 | TRPV3 | | storage | Store at -20°C | | References | [1] Gomtsyan A, et al. Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists. J Med Chem. 2016;59(10):4926-4947. DOI:10.1021/acs.jmedchem.6b00287 [2] Zhao J, et al. PAR2 Mediates Itch via TRPV3 Signaling in Keratinocytes. J Invest Dermatol. 2020;140(8):1524-1532. DOI:10.1016/j.jid.2020.01.012 |
| | 2-Pyridinemethanol, α-[cis-3-hydroxy-3-methyl-1-[4-(trifluoromethyl)-2-pyridinyl]cyclobutyl]-, (αS)- Preparation Products And Raw materials |
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