| 6-IodonordihydrocapsaicinVanilloid receptor antagonist |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
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- MSDS (Material Safety Data Sheet)
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Chemical structure
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| Cas No. | 859171-97-4 | SDF | Download SDF |
| Chemical Name | N-(4-hydroxy-2-iodo-5-methoxybenzyl)nonanamide | ||
| Canonical SMILES | IC(C=C1O)=C(C=C1OC)CNC(CCCCCCCC)=O | ||
| Formula | C17H26INO3 | M.Wt | 419.3 |
| Solubility | <20.96mg l="" in="" ethanol;=""><41.93mg l="" in="" dmso=""> | Storage | Store at RT |
| Physical Appearance | White solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 10 nm against 100 nm capsaicin
The vanilloid TRPV1 receptor, also known as VR1 receptor, belongs to the large family of ‘transient receptor potential’ (TRP). TRPV1 functions as a molecular integrator of nociceptive stimuli, including heat, protons and plant toxins, and is most abundant in peripheral sensory fibers of the C and Ad type. 6-iodo-nordihydrocapsaicin is a potent TRPV1 antagonist.
In vitro: Using human recombinant TRPV1, 6-Iodonordihydrocapsaicin (IC50=10 nm against 100 nm capsaicin) was about four times more potent than the prototypical TRPV1 antagonist, capsazepine [1].
In vivo: 6-Iodonordihydrocapsaicin was tested against capsaicin also on native TRPV1 in: (i) rat dorsal root ganglion neurons in culture; (ii) guinea-pig urinary bladder; and (iii) guinea-pig bronchi. In all cases, except for the guineapig bronchi, the compound was significantly more potent than capsazepine as a TRPV1 antagonist [1].
Clinical trial: Up to now, 6-Iodonordihydrocapsaicin is still in the preclinical development stage.
Reference:[1] Appendino G, Harrison S, De Petrocellis L, Daddario N, Bianchi F, Schiano Moriello A, Trevisani M, Benvenuti F, Geppetti P, Di Marzo V. Halogenation of a capsaicin analogue leads to novel vanilloid TRPV1 receptor antagonists. Br J Pharmacol. 2003 Aug;139(8):1417-24.
