Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
Products are for research use only. Not for human use. We do not sell to patients.
(SB 705498; SB705498)
SB-705498 Chemical Structure
|Product name: SB-705498|
|Cat. No.: HY-10633|
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)
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.
|M.Wt||429.23||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|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|
. Martin J. Gunthorpe, Sara Luis Hannan, Darren Smart et al. Characterization of SB-705498, a Potent and Selective Vanilloid Receptor-1 (VR1/TRPV1) Antagonist That Inhibits the Capsaicin-, Acid-, and Heat-Mediated Activation of the Receptor. JPET June 2007 vol. 321 no. 3 1183-1192.
. Chizh BA, O'Donnell MB, Napolitano A et al. The effects of the TRPV1 antagonist SB-705498 on TRPV1 receptor-mediated activity and inflammatory hyperalgesia in humans. Pain. 2007 Nov;132(1-2):132-41.
. Rami HK, Thompson M, Stemp G et al. Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3287-91.
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.
BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.
Capsaicin, the active component of chili peppers, is a member of the vanilloid family, binds to a receptor called the vanilloid receptor subtype 1 (VR1). Capsaicin is able to kill prostate cancer and lung cancer cells by causing them to undergo apoptosis.
Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, capsaicin; potent TRPV1 receptor antagonist with IC50 of 562 nM.
Chembridge-5861528 is a TRPA1 channel blocker that antagonizes AITC- and 4-HNE-evoked calcium influx (IC50 values are 14.3 and 18.7(mu)M respectively).
GSK101 (GSK1016790A) is a novel TRPV4 activator.
HC-030031 is a selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx with IC50 of 6.2 (mu)M and 5.3 (mu)M respectively.
HC-067047 is a potent and selective TRPV4 antagonist with IC50 values of 48 (plusmn) 6 nM, 133 (plusmn) 25 nM, and 17 (plusmn) 3 nM, respectively in human, rat, and mouse. Also inhibits the endogenous TRPV4-mediated response to 4(alpha)-PDH (IC50 = 22 nM).
Icilin(AG 3-5) is a synthetic super-agonist of TRPM8 ion channel.
Imperatorin is an effective of NO synthesis inhibitor (IC50=9.2 (mu)mol), which also is a BChE inhibitor (IC50=31.4 (mu)mol). Imperatorin is a weak agonist of TRPV1 with EC50 of 12.6(plusmn)3.2 (mu)M.