2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. ROR
  4. GSK2981278

GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.

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

GSK2981278 Chemical Structure

GSK2981278 Chemical Structure

CAS No. : 1474110-21-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 80 In-stock
Solution
10 mM * 1 mL in DMSO USD 80 In-stock
Solid
1 mg USD 35 In-stock
5 mg USD 79 In-stock
10 mg USD 121 In-stock
25 mg USD 231 In-stock
50 mg USD 346 In-stock
100 mg USD 520 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

GSK2981278 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding[1].

IC50 & Target

RORγ[1]
In Vitro

GSK2981278 markedly and potently inhibits IL-17A and IL-22 protein secretion in a concentration dependent manner (IC50 = 3.2 nM) during 5 days of culture under Th17 skewing conditions[1].
GSK2981278 (0.3, 1, 3, 10, 30, 100, 300, 1000 pM; 5 day) potently and selectively inhibits IL-17 and IL-22 levels. Culture in the presence of ≥3 nM GSK2981278 led to a near-complete inhibition of IL-17A protein secretion[1].

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

GSK2981278 Related Antibodies
In Vivo

GSK2981278 (1% in ointment; topically; for three days) reduces skin redness and scaling, as well as decreased hyperplasia, as evidenced by a 23% reduction in epidermal thickness. GSK2981278 attenuates inflammation in a mouse model of psoriasis[1].

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

Animal Model: BALB/c JByRj Female Mice (8 week-old at study initiation; imiquimod (IMQ) mouse model) [1]
Dosage: 1%
Administration: In ointment; topically; for three days
Result: Reduced skin redness and scaling, as well as decreased hyperplasia, as evidenced by a 23% reduction in epidermal thickness.
Clinical Trial
Molecular Weight

461.61

Formula

C25H35NO5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)CN(S(=O)(C1=CC=C(OCC2CCOCC2)C(CO)=C1)=O)C3=CC=C(CC)C=C3
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 (216.63 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 2.1663 mL 10.8317 mL 21.6633 mL
5 mM 0.4333 mL 2.1663 mL 4.3327 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 (5.42 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 (5.42 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 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

Purity: 99.51%

SDS (393 KB)

COA (257 KB) LCMS (266 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 2.1663 mL 10.8317 mL 21.6633 mL 54.1583 mL
5 mM 0.4333 mL 2.1663 mL 4.3327 mL 10.8317 mL
10 mM 0.2166 mL 1.0832 mL 2.1663 mL 5.4158 mL
15 mM 0.1444 mL 0.7221 mL 1.4442 mL 3.6106 mL
20 mM 0.1083 mL 0.5416 mL 1.0832 mL 2.7079 mL
25 mM 0.0867 mL 0.4333 mL 0.8665 mL 2.1663 mL
30 mM 0.0722 mL 0.3611 mL 0.7221 mL 1.8053 mL
40 mM 0.0542 mL 0.2708 mL 0.5416 mL 1.3540 mL
50 mM 0.0433 mL 0.2166 mL 0.4333 mL 1.0832 mL
60 mM 0.0361 mL 0.1805 mL 0.3611 mL 0.9026 mL
80 mM 0.0271 mL 0.1354 mL 0.2708 mL 0.6770 mL
100 mM 0.0217 mL 0.1083 mL 0.2166 mL 0.5416 mL
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GSK2981278 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:

GSK29812781474110-21-8GSK 2981278GSK-2981278RORRAR-related orphan receptorinverseil17RORγ-DNAbinding,IL-17AIL-22,ointmenttopicallyinflammationpsoriasisInhibitorinhibitorinhibit

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