| Identification | Back Directory | [Name]
2-Pyridinemethanol, α-[cis-3-hydroxy-3-methyl-1-[4-(trifluoromethyl)-2-pyridinyl]cyclobutyl]-, (αS)- | [CAS]
1432051-63-2 | [Synonyms]
TRPV3 74a
TRPV3 antagonist 74a
TRPV3 antagonist 74a,TRPV-3 antagonist 74a
(αS)-α-[cis-3-Hydroxy-3-methyl-1-[4-(trifluoromethyl)-2-pyridinyl]cyclobutyl]-2-pyridinemethanol
2-Pyridinemethanol, α-[cis-3-hydroxy-3-methyl-1-[4-(trifluoromethyl)-2-pyridinyl]cyclobutyl]-, (αS)- | [Molecular Formula]
C17H17F3N2O2 | [MDL Number]
MFCD32633449 | [MOL File]
1432051-63-2.mol | [Molecular Weight]
338.33 |
| Chemical Properties | Back Directory | [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| | [form ]
Solid | [pka]
13.36±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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 |
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