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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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| Moringin
Moringin is a potent and selective TRPA1 ion channel natural agonist with an EC50 of 3.14 μM. Moringin does not activate or activates very weakly the vanilloids somatosensory channels TRPV1, TRPV2, TRPV3 and TRPV4, and the melastatin cooling receptor TRPM8. |
| (S)-ABT-102
(S)-ABT-102 is a potent TRPV1 antagonist, with an IC50 of 123 nM. (S)-ABT-102 can block the activation of TRPV1 by capsaicin. |
| Oleoyl Serotonin
Oleoyl Serotonin is a TRPV1 antagonist with IC50 value of 2.57 μM for human TRPV1. |
| ABT-102
ABT-102 (CHEMBL398338) is a potent and highly selective transient receptor potential vanilloid 1 (TRPV1) receptor antagonist. |
| MK-2295
MK-2295 (TRPV1 antagonist 5) is a potent TRPV1 antagonist. MK-2295 can be used for the research of chronic pain. |
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Products are for research use only. Not for human use. We do not sell to patients.
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