| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
GSK2981278 (GSK-2981278; GSK 2981278) is a novel, potent and selective inverse agonist of RORγ (retinoid-related orphan receptor gamma) with potential anti-inflammatory and immumomodulatory activity (e.g. treatment of Psoriasis). As a strong RORγ-selective inverse agonist and modulator, GSK2981278 inhibits IL-17A and IL-22 protein secretion in human peripheral T cell with an IC50 of 3.2 nM.
| ln Vitro |
GSK2981278 significantly and effectively inhibited IL-17A and IL-22 proteins in a concentration-dependent manner (IC50=3.2 nM) during 5 days of culture under Th17 tilt conditions [1]. GSK2981278 (0.3, 1, 3, 10, 30). effectively and locally suppresses IL-17 and IL-22 levels (at doses of 100, 300, and 1000 pM for five days). IL-17A polypeptide is nearly completely inhibited when incubated with ≥ 3 nM GSK2981278 [1].
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| ln Vivo |
GSK2981278 (1% soft; topical; 3 days) decreases skin repair and redness, as shown by a 23% decrease in skin thickness. GSK2981278 reliance in a model of raccoons [1].
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| Animal Protocol |
Animal/Disease Models: BALB/c JByRj female mice (8 weeks old at study entry; imiquimod (IMQ) mouse model) [1]
Doses: 1% Route of Administration: Ointment; Topical; Three Day Experimental Results: Skin Redness and scales are diminished, hyperplasia is diminished, and epidermal thickness is diminished by 23%. |
| References |
[1]. Smith SH, et al. Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin. PLoS One. 2016 Feb 12;11(2):e0147979.
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| Molecular Formula |
C25H35NO5S
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| Molecular Weight |
461.61
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| CAS # |
1474110-21-8
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| Related CAS # |
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| SMILES |
O=S(C1=CC=C(OCC2CCOCC2)C(CO)=C1)(N(C3=CC=C(CC)C=C3)CC(C)C)=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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