SB-705498
Based on 8 publication(s) in Google Scholar
SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.
For research use only. We do not sell to patients.
- Purity: 99.72%
- CAS No.: 501951-42-4
- Formula: C17H16BrF3N4O
- Molecular Weight:429.23
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Membrane Transporter/Ion Channel Compound Library
HY-L011
-
Neuronal Signaling Compound Library
HY-L013
-
Clinical Compound Library
HY-L026
-
Drug Repurposing Compound Library
HY-L035
-
Anti-COVID-19 Compound Library
HY-L052
-
Orally Active Compound Library
HY-L061
-
Mechanoreceptors Compound Library
HY-L095
-
Heterocyclic Compound Library
HY-L138
-
Pain-Related Compound Library
HY-L139
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Inhibitors Library
HY-L158
-
Ion Channel Compound Library
HY-L166
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) SB-705498
More- Nat Biomed Eng. 2025 Jun;9(6):905-916. [Abstract]
- Neuron. 2024 Jun 5;112(11):1815-1831.e4. [Abstract]
- J Exp Clin Cancer Res. 2020 Oct 2;39(1):206. [Abstract]
- Int Immunopharmacol. 2025 May 13:158:114807. [Abstract]
- J Biol Chem. 2022 May;298(5):101847. [Abstract]
- Sci Rep. 2016 Jul 20;6:30168. [Abstract]
- Mol Med Rep. 2024 Jul;30(1):110. [Abstract]
- Research Square Print. 2023 Feb 21.
Biological Activity
pIC50: 7.1
SB705498 (0.3 nM-1 μM) 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 SB705498 rapidly, completely and reversibly inhibits hTRPV1 expressed in HEK293 cells. SB705498 has no significant effect on endogenous [Ca2+] responses in HEK293 cells produced by muscarinic acetylcholine receptor activation with carbachol or store-operated channel-mediated Ca2+ entry after depletion of intracellular stores with the Ca2+ pump inhibitor thapsigargin. SB705498 (10 pM-1 μM) also has no significant antagonist effect versus the close TRPV1 receptor paralog TRPV4 transiently expressed in HEK293 cells and activated using the synthetic ligand 4α-phorbol-12,13-didecanoate (10 μM). SB705498 reveals good antagonist potency against both the rat and guinea pig TRPV1. SB705498 antagonizes rat and guinea pig TRPV1 with pKi of 7.5 and 7.3, respectively. Coapplication of 100 nM to 10 μM SB705498 to the steady state of a maintained capsaicin response leads to rapid and complete inhibition of hTRPV1 at -70 mV. SB705498 inhibits capsaicin-mediated activation of hTRPV1 with IC50 of 3 nM and 17 nM at positive and negative holding potentials (-70 mV and + 70 mV), respectively. Coapplication of 1 μM SB705498 to the plateau period of the response produces complete and reversible inhibition of the TRPV1-mediated conductance[1]. SB705498 shows approximately equal activity versus multiple and diverse chemical and physical modes of TRPV1 receptor activation. SB705498 shows little or no activity versus a wide range of ion channels, receptors and enzymes. SB705498 produces full blockade of heat as well as pH activation of hTRPV1[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 501951-42-4
-
Appearance Solid
-
Molecular Weight 429.23
-
Formula C17H16BrF3N4O
-
Color White to off-white
-
SMILES
BrC1=CC=CC=C1NC(N[C@@H]2CCN(C3=NC=C(C(F)(F)F)C=C3)C2)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
-
Journal Impact Factor
-
Most Recent
-
Nat Biomed Eng
Solvent-mediated analgesia via the suppression of water permeation through TRPV1 ion channels. [Abstract]2025 Jun;9(6):905-916. PMID: 39572786 -
Neuron
TRPV1 analgesics disturb core body temperature via a biased allosteric mechanism involving conformations distinct from that for nociception. [Abstract]2024 Jun 5;112(11):1815-1831.e4. PMID: 38492574 -
J Exp Clin Cancer Res
2020 Oct 2;39(1):206. PMID: 33008449 -
Int Immunopharmacol
Inhibition of TRPV1 attenuates innate nasal epithelial responses via NF-κB signaling pathway in allergic rhinitis. [Abstract]2025 May 13:158:114807. PMID: 40367690 -
J Biol Chem
Capsaicin inhibits intestinal Cl- secretion and promotes Na+ absorption by blocking TRPV4 channels in healthy and colitic mice. [Abstract]2022 May;298(5):101847. PMID: 35314195 -
Sci Rep
Suppression of TRPV4 channels ameliorates anti-dipsogenic effects under hypoxia in the subfornical organ of rats. [Abstract]2016 Jul 20;6:30168. PMID: 27436489 -
Mol Med Rep
Calcitonin gene‑related peptide alleviates hyperoxia‑induced human alveolar cell injury via the CGRPR/TRPV1/Ca2+ axis. [Abstract]2024 Jul;30(1):110. PMID: 38695251 -
Solvent & Solubility
DMSO : 100 mg/mL (232.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.82 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (274 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3298 mL | 11.6488 mL | 23.2975 mL | 58.2438 mL |
| 5 mM | 0.4660 mL | 2.3298 mL | 4.6595 mL | 11.6488 mL | |
| 10 mM | 0.2330 mL | 1.1649 mL | 2.3298 mL | 5.8244 mL | |
| 15 mM | 0.1553 mL | 0.7766 mL | 1.5532 mL | 3.8829 mL | |
| 20 mM | 0.1165 mL | 0.5824 mL | 1.1649 mL | 2.9122 mL | |
| 25 mM | 0.0932 mL | 0.4660 mL | 0.9319 mL | 2.3298 mL | |
| 30 mM | 0.0777 mL | 0.3883 mL | 0.7766 mL | 1.9415 mL | |
| 40 mM | 0.0582 mL | 0.2912 mL | 0.5824 mL | 1.4561 mL | |
| 50 mM | 0.0466 mL | 0.2330 mL | 0.4660 mL | 1.1649 mL | |
| 60 mM | 0.0388 mL | 0.1941 mL | 0.3883 mL | 0.9707 mL | |
| 80 mM | 0.0291 mL | 0.1456 mL | 0.2912 mL | 0.7280 mL | |
| 100 mM | 0.0233 mL | 0.1165 mL | 0.2330 mL | 0.5824 mL |
Powered by Bioz