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Home   »   Product Pathways  »  TRP Channel  »  SB-705498

Products are for research use only. Not for human use. We do not sell to patients.

CS-0757 SB-705498

(SB 705498;SB705498)
Structure Price and Availability of    SB-705498
United States
Size Price Stock
5mg $80 In-stock Inquiry
10mg $150 In-stock
50mg $650 In-stock
100mg $1050 In-stock
200 mg Get quote
500 mg Get quote
 Distributor In Japan:  フナコシ株式会社    電話番号:81-3-5684-1620   
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SB-705498  M.Wt:  429.23
SB-705498  Formula: C17H16BrF3N4O
SB-705498  Solubility: DMSO ≥80mg/mL; Water <1mg/mL; Ethanol ≥20mg/mL
SB-705498  Purity: >98%
SB-705498  Storage:  Please store the product under the recommended conditions in the Certificate of Analysis.
CAS: 501951-42-4

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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. IC50 value: 7.1 (pIC50) Target: TRPV1 SB-705498 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 SB-705498 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.

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