2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. SB-366791

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.

For research use only. We do not sell to patients.

SB-366791 Chemical Structure

SB-366791 Chemical Structure

CAS No. : 472981-92-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 92 In-stock
25 mg USD 198 In-stock
50 mg USD 317 In-stock
100 mg USD 528 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

SB-366791 Related Antibodies

Top Publications Citing Use of Products

View All TRP Channel Isoform Specific Products:

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TRPC TRPM TRPV TRPA TRPML

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target[2]

hTRPV1

5.7 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.27 μM
Compound: SB-366791
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
[PMID: 26850005]
HEK293 IC50
0.19 μM
Compound: SB-366791
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
[PMID: 26850005]
In Vivo

SB-366791 (30 μM) inhibits the frequency of miniature excitatory postsynaptic currents (EPSCs). SB-366791 (30 μM) reduces the frequency of spontaneous EPSCs in the spinal cord slices from FCA-treated rats. SB-366791(30 μM) inhibits the amplitude of C-fibre evoked EPSCs. SB-366791 has also been used in vivo to assess the potential analgesic action of the inhibition of TRPV1, and significantly inhibits capsaicin-induced hypothermia, eye wiping movements and vasodilatation in the knee joint. SB-366791 inhibits glutamatergic transmission via an apparently pre-synaptic mechanism(s)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

287.74

Formula

C16H14ClNO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=CC(OC)=C1)/C=C/C2=CC=C(Cl)C=C2
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
Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4754 mL 17.3768 mL 34.7536 mL
5 mM 0.6951 mL 3.4754 mL 6.9507 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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 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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SB-366791 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SB-366791472981-92-3SB366791SB 366791TRP ChannelTransient receptor potential channelspotentselectivetransientreceptorpotentialvanilloidinflammationInhibitorinhibitorinhibit

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