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MedKoo Cat#: 526931 | Name: GSK2981278
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GSK2981278 is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma). GSK2981278 is a strong RORγ-selective inverse agonist that inhibits activation of the il17 promoter. GSK2981278 robustly inhibits RORγ-mediated cytokine production at both the mRNA and protein level. GSK2981278 attenuates inflammation in a mouse model of psoriasis. Topical treatment with GSK2981278 will significantly limit Th17-type cytokine expression and should therefore lead to improved clinical outcomes for patients.

Chemical Structure

GSK2981278
GSK2981278
CAS#1474110-21-8

Theoretical Analysis

MedKoo Cat#: 526931

Name: GSK2981278

CAS#: 1474110-21-8

Chemical Formula: C25H35NO5S

Exact Mass: 461.2236

Molecular Weight: 461.62

Elemental Analysis: C, 65.05; H, 7.64; N, 3.03; O, 17.33; S, 6.95

Price and Availability

Size Price Availability Quantity
10mg USD 90.00 Ready to ship
25mg USD 190.00 Ready to ship
50mg USD 350.00 Ready to ship
100mg USD 550.00 Ready to ship
200mg USD 950.00 Ready to ship
500mg USD 1,850.00 Ready to ship
1g USD 2,950.00 Ready to ship
2g USD 4,850.00 Ready to ship
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Related CAS #
No Data
Synonym
GSK2981278; GSK-2981278; GSK 2981278.
IUPAC/Chemical Name
N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamide
InChi Key
LZLBRISQTJVZNP-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H35NO5S/c1-4-20-5-7-23(8-6-20)26(16-19(2)3)32(28,29)24-9-10-25(22(15-24)17-27)31-18-21-11-13-30-14-12-21/h5-10,15,19,21,27H,4,11-14,16-18H2,1-3H3
SMILES Code
O=S(C1=CC=C(OCC2CCOCC2)C(CO)=C1)(N(C3=CC=C(CC)C=C3)CC(C)C)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
GSK2981278 is a highly potent and selective inverse agonist for RORγ.
In vitro activity:
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. Reference: PLoS One. 2016 Feb 12;11(2):e0147979. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/26870941/
In vivo activity:
The imiquimod (IMQ) mouse model was employed to demonstrate efficacy of GSK2981278 in a psoriaform-like mouse model. Topical application of IMQ can induce and exacerbate psoriasis-like chronic skin inflammation in mice, including epidermal thickening, a dependence on T cell immunity, and a mechanism dependent on the IL-23/IL-17 pathway. It was first confirmed that GSK2981278 can inhibit IL-17A protein secretion by mouse CD4+ T cells, confirming cross-reactivity of our compound for both mouse and human RORγ (data not shown). Next, mice were treated topically with GSK2981278 (1% ointment or placebo) for three days (day -3 to day 0), after which mice continued to receive compound for the duration of the study. Starting on day 0, mice were challenged topically with IMQ (5%) cream or petrolatum (non-inflammatory inert cream) for up to ten days (day 0 to day +9). On the last day of treatment, the skin was imaged and clinically assessed. GSK2981278 was undetectable (<5 ng/ml) in serum at harvest, indicating that systemic exposure was minimal. Mice exposed to GSK2981278 exhibited reduced skin redness and scaling, as well as decreased hyperplasia, as evidenced by a 23% reduction in epidermal thickness when compared to the placebo + IMQ-treated group (Fig 2A and 2B). Reference: PLoS One. 2016 Feb 12;11(2):e0147979. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/26870941/
Solvent mg/mL mM
Solubility
DMSO 92.0 199.30
Ethanol 92.0 199.30
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 461.62 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
1. Smith SH, Peredo CE, Takeda Y, Bui T, Neil J, Rickard D, Millerman E, Therrien JP, Nicodeme E, Brusq JM, Birault V, Viviani F, Hofland H, Jetten AM, Cote-Sierra J. Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin. PLoS One. 2016 Feb 12;11(2):e0147979. doi: 10.1371/journal.pone.0147979. PMID: 26870941; PMCID: PMC4752338.
In vivo protocol:
1. Smith SH, Peredo CE, Takeda Y, Bui T, Neil J, Rickard D, Millerman E, Therrien JP, Nicodeme E, Brusq JM, Birault V, Viviani F, Hofland H, Jetten AM, Cote-Sierra J. Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin. PLoS One. 2016 Feb 12;11(2):e0147979. doi: 10.1371/journal.pone.0147979. PMID: 26870941; PMCID: PMC4752338.
1: Smith SH, Peredo CE, Takeda Y, Bui T, Neil J, Rickard D, Millerman E, Therrien JP, Nicodeme E, Brusq JM, Birault V, Viviani F, Hofland H, Jetten AM, Cote-Sierra J. Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin. PLoS One. 2016 Feb 12;11(2):e0147979. doi: 10.1371/journal.pone.0147979. PubMed PMID: 26870941; PubMed Central PMCID: PMC4752338.