GLPG-0778 Chemical Properties

Density 

1.40±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMF: 2 mg/ml; DMSO: 5 mg/ml; Ethanol: 1 mg/ml

form 

A crystalline solid

pka

7.99±0.20(Predicted)

color 

White to off-white

GLPG-0778 Usage And Synthesis

Description

Solcitinib is a JAK1 inhibitor (IC₅₀ = 9.8 nM). It is greater than 10-fold selective for JAK1 over JAK2, JAK3, and TYK2.

Uses

Solcitinib is an orally active, competitive, potent, selective JAK1 inhibitor, with an IC50 of 9.8 nM, and 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; Solcitinib is used in the research of moderate-to-severe plaque-type psoriasis.

IC 50

JAK1: 9.8 nM (IC₅₀)

References

[1] Ludbrook VJ, et al. Investigation of selective JAK1 inhibitor GSK2586184 for the treatment of psoriasis in a randomized placebo-controlled phase IIa study. Br J Dermatol. 2016 May;174(5):985-95. DOI:10.1111/bjd.14399