[CAS NO. 1474110-21-8] GSK2981278
PRODUCTS SPECIFICATIONS [1474110-21-8]
DESCRIPTION [1474110-21-8]
Overview
| MDL | MFCD29059455 |
|---|---|
| Molecular Weight | 461.61 |
| Molecular Formula | C25H35NO5S |
| SMILES | CC(C)CN(S(=O)(C1=CC=C(OCC2CCOCC2)C(CO)=C1)=O)C3=CC=C(CC)C=C3 |
3 Publications Citing Use of MCE
Summary
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
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
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02548052 | GlaxoSmithKline |
Psoriasis
|
October 22, 2015 | Phase 1 |
| NCT03004846 | GlaxoSmithKline |
Psoriasis
|
February 13, 2017 | Phase 1|Phase 2 |
Appearance
Solid
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
DMSO : ≥ 100 mg/mL ( 216.63 mM )
* "≥" means soluble, but saturation unknown.
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 |