SB-366791
Based on 8 publication(s) in Google Scholar
SB-366791 is a potent and selective vanilloid receptor (VR1/TRPV1) antagonist (IC50=5.7 nM). SB-366791 can be used for the research of inflammation.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.29%
- No. CAS: 472981-92-3
- Fòrmula: C16H14ClNO2
- Peso molecular:287.74
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SB-366791
More- Neuron. 2024 Jun 5;112(11):1815-1831.e4. [Abstract]
- Adv Sci (Weinh). 2025 Sep 15:e10102. [Abstract]
- Cell Rep Med. 2025 Aug 19;6(8):102276. [Abstract]
- Dev Cell. 2024 Jun 3;59(11):1396-1409.e5. [Abstract]
- Sci Signal. 2020 Nov 24;13(659):eaax0273. [Abstract]
- J Ethnopharmacol. 2025 Sep 16;355(Pt A):120618. [Abstract]
- FASEB J. 2025 Jul 31;39(14):e70817. [Abstract]
- FASEB J. 2025 May 31;39(10):e70657. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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IHC
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
Actividad biológica
Descripciòn
IC50 & Target
[2]|
hTRPV1 5.7 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
0.27 μM
Compound: SB-366791
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Antagonist activity at recombinant human TRPV1 channel expressed in CHO cells assessed as inhibition of capsiacin-induced Ca2+ flux by Fluo-3 dye based FLIPR assay
Antagonist activity at recombinant human TRPV1 channel expressed in CHO cells assessed as inhibition of capsiacin-induced Ca2+ flux by Fluo-3 dye based FLIPR assay
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[PMID: 26850005] |
| HEK293 | IC50 |
0.19 μM
Compound: SB-366791
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Antagonist activity at recombinant human TRPV1 channel expressed in HEK293 cells assessed as inhibition of capsiacin-induced Ca2+ flux preincubated for 5 mins followed by capsiacin challenge by Fluo-4-AM dye based spectrofluorimetry
Antagonist activity at recombinant human TRPV1 channel expressed in HEK293 cells assessed as inhibition of capsiacin-induced Ca2+ flux preincubated for 5 mins followed by capsiacin challenge by Fluo-4-AM dye based spectrofluorimetry
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[PMID: 26850005] |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 472981-92-3
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Appearance Solid
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Peso molecular 287.74
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Fòrmula C16H14ClNO2
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Color White to off-white
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SMILES
O=C(NC1=CC=CC(OC)=C1)/C=C/C2=CC=C(Cl)C=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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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
SB-366791 purchased from MedChemExpress. Usage Cited in: Neuron. 2024 Jun 5;112(11):1815-1831.e4. [Abstract]
Finally, SB366791 (3 μM) showed reduced inhibition of 2-APB-evoked currents of mTRPV1Y512W, mTRPV1S513A, mTRPV1S513T, mTRPV1L516F, mTRPV1T551S, mTRPV1T551C, and mTRPV1L670I, and the reduced potencies were confirmed using 9 μM SB366791 under conditions of channel activation by thermal stimulation.
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Adv Sci (Weinh)
Thermosensory TRPV Heterotetramers Drive Seasonal Polyphenism: Molecular Basis of CcIav/CcNan-PKCα-AKH/AKHR Signaling in Pear Psyllid Morph Transition. [Abstract]2025 Sep 15:e10102. PMID: 40953294
SB-366791 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Sep 15:e10102. [Abstract]
The 2:2 heterotetramer exhibited greatest capsaicin sensitivity (EC50 value of 2.24 × 10−5 mm\), reversibly inhibited by TRPV antagonist SB-366791 (0-100 μM).
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Cell Rep Med
Computational framework for prioritizing candidate compounds overcoming the resistance of pancancer immunotherapy. [Abstract]2025 Aug 19;6(8):102276. PMID: 40769146 -
Dev Cell
Using an ER-specific optogenetic mechanostimulator to understand the mechanosensitivity of the endoplasmic reticulum. [Abstract]2024 Jun 3;59(11):1396-1409.e5. PMID: 38569547
SB-366791 purchased from MedChemExpress. Usage Cited in: Dev Cell. 2024 Jun 3;59(11):1396-1409.e5. [Abstract]
Dual inhibition of TRPV1 and PKD2 with SB-366791 (3 μM, 1h) and PKD2 knockdown further reduced force-induced Ca2+ release than inhibiting either alone. This result was corroborated by dual inhibition through TRPV1 knockdown and PKD2 knockdown, showing that TRPV1 and PKD2 contributed to the force-induced ER Ca2+ release in a cumulative manner.
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Sci Signal
Airway relaxation mechanisms and structural basis of osthole for improving lung function in asthma. [Abstract]2020 Nov 24;13(659):eaax0273. PMID: 33234690 -
J Ethnopharmacol
2025 Sep 16;355(Pt A):120618. PMID: 40967489
SB-366791 purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2025 Sep 16;355(Pt A):120618. [Abstract]
The treatment with YPFND-H or SB-366791 (1 μM) mitigated the upregulation of TRPV1 by inhibiting p38 MAPK phosphorylation.
SB-366791 purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2025 Sep 16;355(Pt A):120618. [Abstract]
The treatment with YPFND-H or SB-366791 (1 μM) mitigated the upregulation of TRPV1 by inhibiting p38 MAPK phosphorylation.
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FASEB J
Nitric Oxide Scavenging Alleviates Scar Pruritus by Inhibiting S-Nitrosylation of Transient Receptor Potential Channels and Limiting Calcium Influx. [Abstract]2025 Jul 31;39(14):e70817. PMID: 40637249 -
FASEB J
Capsazepine Inhibits Astrocyte Activation and Attenuates Neuroinflammation by Targeting Syntaxin 7. [Abstract]2025 May 31;39(10):e70657. PMID: 40386937
Solvente y solubilidad
In Vitro:
DMSO : ≥ 100 mg/mL (347.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
In Vivo:
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 (8.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (8.69 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureza y Documentación
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Ficha de datos (272 KB)
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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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Lappin SC, et al. TRPV1 antagonist, SB-366791, inhibits glutamatergic synaptic transmission in rat spinal dorsal horn following peripheral inflammation. Eur J Pharmacol. 2006;540(1-3):73-81. [Content Brief]
[2]. Gunthorpe MJ, et al. Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist [published correction appears in Neuropharmacology. 2004 May;46(6):905]. Neuropharmacology. 2004;46(1):133-149. [Content Brief]
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 | 3.4754 mL | 17.3768 mL | 34.7536 mL | 86.8840 mL |
| 5 mM | 0.6951 mL | 3.4754 mL | 6.9507 mL | 17.3768 mL | |
| 10 mM | 0.3475 mL | 1.7377 mL | 3.4754 mL | 8.6884 mL | |
| 15 mM | 0.2317 mL | 1.1585 mL | 2.3169 mL | 5.7923 mL | |
| 20 mM | 0.1738 mL | 0.8688 mL | 1.7377 mL | 4.3442 mL | |
| 25 mM | 0.1390 mL | 0.6951 mL | 1.3901 mL | 3.4754 mL | |
| 30 mM | 0.1158 mL | 0.5792 mL | 1.1585 mL | 2.8961 mL | |
| 40 mM | 0.0869 mL | 0.4344 mL | 0.8688 mL | 2.1721 mL | |
| 50 mM | 0.0695 mL | 0.3475 mL | 0.6951 mL | 1.7377 mL | |
| 60 mM | 0.0579 mL | 0.2896 mL | 0.5792 mL | 1.4481 mL | |
| 80 mM | 0.0434 mL | 0.2172 mL | 0.4344 mL | 1.0860 mL | |
| 100 mM | 0.0348 mL | 0.1738 mL | 0.3475 mL | 0.8688 mL |
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