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Purity: ≥98%
SB-705498 (SB705498; SB 705498) is an orally bioavailable and competitive antagonist of the capsaicin-mediated activation of TRPV1 (transient receptor potential vanilloid 1) receptors with important biological activity. It inhibits TRPV1 with pKis of 7.6, 7.5, and 7.3 for human, rat, and guinea pig, respectively.
| ln Vitro |
SB705498 (0.3 nM-1 μM) potently suppresses capsaicin-induced activation of human TRPV1 produced in 1321N1 cells or HEK293 cells with an apparent pKi of 7.5 or 7.6, respectively. Co-application of 100 nM SB705498 immediately, fully, and reversibly suppresses hTRPV1 expression in HEK293 cells. SB705498 had no significant influence on endogenous [Ca2+] responses in HEK293 cells depleting intracellular reserves with the Ca2+ pump inhibitor thapsigargin. SB705498 (10 pM-1 μM) and the tight TRPV1 receptor paralog TRPV4 transiently expressed in HEK293 cells and activated with the synthetic ligand 4α-phorbol-12,13-didecanoate (10 μM) There is no clear antagonistic effect. SB705498 demonstrated good antagonist efficacy against rat and guinea pig TRPV1. SB705498 antagonizes rat and guinea pig TRPV1 with pKi of 7.5 and 7.3, respectively. Coadministration of 100 nM to 10 μM SB705498, along with a maintained steady-state capsaicin response, resulted in quick and full suppression of hTRPV1 at -70 mV. SB705498 inhibits capsaicin-mediated activation of hTRPV1 with IC50 of 3 nM and 17 nM at positive and negative potentials (-70 mV and + 70 mV), respectively. Co-application of 1 μM SB705498 with the plateau phase of the reaction leads in full and reversible suppression of TRPV1-mediated conductance [1]. SB705498 displays activity that is broadly consistent with a wide array of chemical and physical modalities of TRPV1 receptor activation. SB705498 has limited activity against a number of ion channels, receptors, and enzymes. SB705498 provides complete heat blocking and pH activation of hTRPV1 [2].
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| ln Vivo |
The TRPV1 activation pathways mediated by heat, acid, and vanillin (capsaicin) are all potently and reversibly blocked by SB705498. SB705498 reversed allodynia well and shown excellent action at 10 and 30 mg/kg po. In the guinea pig FCA model, SB705498 (10 mg/kg po) reversed 80% of the allodynia [2].
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| References |
[1]. Martin J. Gunthorpe, 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.
[2]. Rami HK, 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. |
| Molecular Formula |
C17H16BRF3N4O
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| Molecular Weight |
429.23
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| CAS # |
501951-42-4
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| SMILES |
BrC1=C([H])C([H])=C([H])C([H])=C1N([H])C(N([H])[C@@]1([H])C([H])([H])N(C2C([H])=C([H])C(C(F)(F)F)=C([H])N=2)C([H])([H])C1([H])[H])=O
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| Chemical Name |
N-(2-bromophenyl)-N-[(3R)-1-[5-(trifluoromethyl)-2-pyridinyl]-3-pyrrolidinyl]-urea
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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