Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H26FN3O2S2 |
| Molecular Weight | 423.568 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(C)C1=CC=C(CNC(=S)NCC2=CC=C(NS(C)(=O)=O)C(F)=C2)C=C1
InChI
InChIKey=DUHBVFMCIJLUJX-UHFFFAOYSA-N
InChI=1S/C20H26FN3O2S2/c1-20(2,3)16-8-5-14(6-9-16)12-22-19(27)23-13-15-7-10-18(17(21)11-15)24-28(4,25)26/h5-11,24H,12-13H2,1-4H3,(H2,22,23,27)
| Molecular Formula | C20H26FN3O2S2 |
| Molecular Weight | 423.568 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
JYL1421 is a more selective and in most models a more potent Vanilloid receptor (TRPV1) antagonist than capsazepine, therefore it may promote the assessment of the (patho) physiological roles of the TRPV1 receptor. Vanilloid receptors play a roll in sensory transduction for capsaicin (capsaicin-induced calcium uptake), protons, and heat.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| High affinity antagonists of the vanilloid receptor. | 2002 Oct |
|
| Pharmacological characterization of the TRPV1 receptor antagonist JYL1421 (SC0030) in vitro and in vivo in the rat. | 2005 Jul 4 |
|
| The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation. | 2007 Mar 28 |
Sample Use Guides
To test whether JYL1421 was antagonizing vanilloid action through a competitive mechanism, it was determined the dose response curves for induction of 45Ca uptake by capsaicin and RTX as a function of the concentration of JYL1421. Cells were incubated with fixed concentrations of antagonist together with varied concentrations of capsaicin for 5 min. For JYL1421, it was obtained Ki values of 8.0 ± 0.3 nM (three experiments) as an antagonist of capsaicin and of 9.6 ± 0.1 nM (three experiments) as an antagonist of RTX.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 07:59:47 GMT 2023
by
admin
on
Sat Dec 16 07:59:47 GMT 2023
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| Record UNII |
Y6TH2I6W99
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| Record Status |
Validated (UNII)
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| Record Version |
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Y6TH2I6W99
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10295883
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401907-26-4
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admin on Sat Dec 16 07:59:47 GMT 2023 , Edited by admin on Sat Dec 16 07:59:47 GMT 2023
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