Description
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 . 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 . Clinical trial: Up to now, 6-Iodonordihydrocapsaicin is still in the preclinical development stage.
Product information
CAS Number: 859171-97-4
Molecular Weight: 419.30
Formula: C17H26INO3
Chemical Name: N-[(4-hydroxy-2-iodo-5-methoxyphenyl)methyl]nonanamide
Smiles: CCCCCCCCC(=O)NCC1=CC(OC)=C(O)C=C1I
InChiKey: AAORACFZMYMFCG-UHFFFAOYSA-N
InChi: InChI=1S/C17H26INO3/c1-3-4-5-6-7-8-9-17(21)19-12-13-10-16(22-2)15(20)11-14(13)18/h10-11,20H,3-9,12H2,1-2H3,(H,19,21)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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