GSK 2981278

SKU: orb1226206

Description

GSK 2981278 (GSK2981278) is a potent, highly selective RORγ/RORγt inhibitor that potently inhibits IL-17A and IL-22 protein secretion in human peripheral T cell with IC50 of 3.2 nM; shows no effects on RORα-dependent activation; robustly inhibits RORγ-mediated cytokine production at both the mRNA and protein level, inhibits RORγt-mediated transactivation; attenuates inflammation in mouse model of psoriasis.Psoriasis Phase 2 Clinical(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.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.(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.

Key Properties

• CAS Number: 1474110-21-8
• MW: 461.617
• Purity: >98% (HPLC)
• Formula: C₂₅H₃₅NO₅S
• SMILES: O=S(C1=CC=C(OCC2CCOCC2)C(CO)=C1)(N(C3=CC=C(CC)C=C3)CC(C)C)=O
• Target: ROR
• Solubility: DMSO: 10 mM （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  Animal model: BALB/c JByRj Female Mice (8 week-old at study initiation; imiquimod (IMQ) mouse model). 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK2981278 | GSK-2981278

Quick Database Links

Gene Symbol

ROR