SB-705498 NEW
| Price | $41 | $76 | $176 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: SB-705498 | CAS No.: 501951-42-4 |
| Purity: ≥95% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | SB-705498 |
| Description | SB705498 is a TRPV1 antagonist for hTRPV1. SB-705498 has been investigated for the treatment of Rhinitis, Chronic Cough, and Non-allergic Rhinitis. |
| In vitro | SB705498 (0.3 nM-1 μM) effectively blocks capsaicin-induced activation of human TRPV1 channels in 1321N1 and HEK293 cells, with apparent pKi values of 7.5 and 7.6, respectively. A 100 nM SB705498 coapplication rapidly, completely, and reversibly suppresses hTRPV1 in HEK293 cells, without significantly affecting [Ca2+] responses induced by carbachol activation of muscarinic acetylcholine receptors or Ca2+ entry through store-operated channels following thapsigargin-induced Ca2+ store depletion. SB705498 also shows negligible antagonistic effects on TRPV4 activation in HEK293 cells within the 10 pM to 1 μM range and selectively inhibits TRPV1, demonstrating notable potency against rat and guinea pig TRPV1 with pKi values of 7.5 and 7.3, respectively. At 100 nM-10 μM, it rapidly and completely inhibits hTRPV1 in sustained capsaicin responses at -70 mV, with IC50 values of 3 nM and 17 nM at -70 mV and +70 mV, respectively. Furthermore, 1 μM SB705498 fully and reversibly inhibits TRPV1-mediated conductance during the response plateau, uniformly blocking both chemical and physical TRPV1 activation with minimal to no activity against other ion channels, receptors, and enzymes, including inhibition of TRPV1 by heat and altered pH levels. |
| In vivo | SB705498 demonstrates potent and reversible inhibition of TRPV1 receptor activation through various modes, including vanilloid (capsaicin), heat, and acid mediation. It shows remarkable efficacy at 10 and 30 mg/kg orally, effectively reversing allodynia. Additionally, SB705498 achieves an 80% reduction in allodynia within the guinea pig FCA model at a dosage of 10 mg/kg orally [2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : 16 mg/mL (37.3 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 60 mg/mL (139.79 mM) |
| Keywords | inhibit | SB705498 | Inhibitor | SB 705498 | TRP Channel | SB-705498 | Transient receptor potential channels |
| Inhibitors Related | (+)-Camphor | AP 18 | Methyl syringate | Caffeic Acid | Oleoyl Serotonin | (-)-Menthol | Camphor | Pregnenolone | Probenecid | 1,4-Cineole | Methyl salicylate | SKF-96365 hydrochloride |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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