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SB-705498

HY-10633

(SB 705498; SB705498)

SB-705498

SB-705498 Chemical Structure

SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.

Size Price Stock Quantity
10 mM * 1 mL in DMSO $88 In-stock
5 mg $80 In-stock
10 mg $150 In-stock
50 mg $650 In-stock
100 mg $1050 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL in DMSO €86 In-stock
5 mg €78 In-stock
10 mg €147 In-stock
50 mg €637 In-stock
100 mg €1029 In-stock
200 mg Get quote
500 mg Get quote

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Product name: SB-705498
Cat. No.: HY-10633

SB-705498 Data Sheet

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    Purity: 99.73%

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    DataSheet

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    LCMS

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Biological Activity of SB-705498

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.

Chemical Information

M.Wt 429.23 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C17H16BrF3N4O
CAS No 501951-42-4
Solvent & Solubility

DMSO ≥80mg/mL; Water <1mg/mL; Ethanol ≥20mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 2.3298 mL 11.6488 mL 23.2975 mL
5 mM 0.4660 mL 2.3298 mL 4.6595 mL
10 mM 0.2330 mL 1.1649 mL 2.3298 mL

References on SB-705498

Inhibitor Kit

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