1. Metabolic Enzyme/Protease
  2. ROR
  3. GSK2981278

GSK2981278 

Cat. No.: HY-19770 Purity: 99.70%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 112 In-stock
Estimated Time of Arrival: December 31
1 mg USD 70 In-stock
Estimated Time of Arrival: December 31
5 mg USD 110 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
50 mg USD 490 In-stock
Estimated Time of Arrival: December 31
100 mg USD 790 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

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].

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.

1474110-21-8

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (216.63 mM)

*"≥" 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
10 mM 0.2166 mL 1.0832 mL 2.1663 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.70%

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Keywords:

GSK2981278GSK 2981278GSK-2981278RORRAR-related orphan receptorinverseil17RORγ-DNAbinding,IL-17AIL-22,ointmenttopicallyinflammationpsoriasisInhibitorinhibitorinhibit

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Product Name:
GSK2981278
Cat. No.:
HY-19770
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