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SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1. SB705498 potently inhibits capsaicin-induced activation of human TRPV1 expressed in 1321N1 cells or HEK293 cells with apparent pKi of 7.5 or 7.6, respectively. Coapplication of 100 nM SB705498 rapidly, completely and reversibly inhibits hTRPV1 expressed in HEK293 cells. Compared with placebo, SB-705498 reduced the area of capsaicin-evoked flare (P=0.0047). The heat pain threshold on non-sensitised skin was elevated following SB-705498 (estimated difference from placebo [95% confidence intervals]: 1.3 degrees C [0.07,2.53], P=0.019). Following capsaicin sensitisation, the heat pain threshold and tolerance were similar between SB-705498 and placebo. However, SB-705498 increased heat pain tolerance at the site of UVB-evoked inflammation (estimated difference from placebo: 0.93 degrees C [0.25,1.6], P=0.0054). The magnitude of the pharmacodynamic effects of SB-705498 appeared to be related to plasma concentration. These results indicate that SB-705498, at a clinically safe and well-tolerated dose, has target-specific pharmacodynamic activity in humans. These data provide the first clinical evidence that a TRPV1 antagonist may alleviate pain and hyperalgesia associated with inflammation and tissue injury.
PHYTO medicine. 2024 Apr 03.
Alcohol inducing macrophage M2b polarization in colitis by modulating the TRPV1-MAPK/NF-κB pathways
SB-705498 purchased from AbMole
| Molecular Weight | 429.23 |
| Formula | C17H16BrF3N4O |
| CAS Number | 501951-42-4 |
| Solubility (25°C) | DMSO ≥70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related TRP Channel Products |
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| HC-030031
HC-030031 is a selective TRPA1 blocker, antagonizing TRPA1-mediated calcium influx induced by AITC and formalin (IC50 = 6.2 and 5.3 μM, respectively). |
| AMG-517
AMG 517 is a potent and selective TRPV1 antagonist, antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM. |
| Icilin
Icilin is a synthetic super-agonist of the transient receptor potential M8 (TRPM8) ion channel. |
| Phenazopyridine hydrochloride
Phenazopyridine HCl is a competitive SARM1 inhibitor as well as a TRPM8 antagonist with an IC50 for SARM1 inhibition of 145 μM. It has local anesthetic/analgesic activity and can be used in studies related to traumatic brain injury, peripheral neuropathy, and neurodegenerative diseases. |
| Probenecid
Probenecid is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16. |
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Products are for research use only. Not for human use. We do not sell to patients.
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