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Submit ReviewTRPV3 74a is a selective TRPV3 antagonist (KB = 0.56 μM). Displays no significant activity against a panel of other ion channels. Exhibits efficacy in animal models of neuropathic pain. Brain penetrant.
M. Wt | 338.32 |
Formula | C17H17F3N2O2 |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 1432051-63-2 |
PubChem ID | 71554840 |
InChI Key | MTJXDHFAWXGXIN-OAGGEKHMSA-N |
Smiles | C[C@]1(C[C@@]([C@@H](C2=CC=CC=N2)O)(C3=CC(C(F)(F)F)=CC=N3)C1)O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 33.83 | 100 |
The following data is based on the product molecular weight 338.32. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.96 mL | 14.78 mL | 29.56 mL |
5 mM | 0.59 mL | 2.96 mL | 5.91 mL |
10 mM | 0.3 mL | 1.48 mL | 2.96 mL |
50 mM | 0.06 mL | 0.3 mL | 0.59 mL |
References are publications that support the biological activity of the product.
Gomtsyan et al (2016) Synthesis and pharmacology of (pyridin-2-yl)methanol derivatives as novel and selective transient receptor potential vanilloid 3 antagonists. J.Med.Chem. 59 4926 PMID: 27077528
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.