5'-Iodoresiniferatoxin
5'-Iodoresiniferatoxin is a very potent and strong competitive antagonist of the transient receptor potential vanilloid 1 (TRPV1) receptor. It is derived from resiniferatoxin (RTX), which is produced by the Moroccan succulent Euphorbia resinifera. It is iodinated at the 5-position and can be prepared from RTX by electrophilic aromatic substitution. It binds to TRPV1 (VR1) receptors expressed in HEK293 cells with Kd value of 4.3 nM and Ki value of 5.8 nM. It binds to the VR1 receptor with high affinity but does not induce RTX- or capsaicin-like effects in Xenopus laevis oocytes expressing VR1. It is 40-fold more potent than capsazepine.
Supplier | BOC Sciences |
---|---|
Product # | 535974-91-5 |
Pricing | Inquire |
Cas | 535974-91-5 |
Molecular Weight | 754.60 |
Molecular Formula | C37H39IO9 |
Canonical SMILES | CC1CC2(C3C4C1(C5C=C(C(=O)C5(CC(=C4)COC(=O)CC6=CC(=C(C(=C6)I)O)OC)O)C)OC(O3)(O2)CC7=CC=CC=C7)C(=C)C |