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Solcitinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Solcitinib图片
CAS NO:1206163-45-2
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 389.45
Formula C22H23N5O2
CAS No. 1206163-45-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 20 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo) O=C(C1CC1)NC2=NN3C(C4=CC=C(C(N5CC(C)(C)C5)=O)C=C4)=CC=CC3=N2
Synonyms GLPG-0778; GSK-2586184; GSK2586184A; GLPG 0778; GLPG0778; GSK 2586184; GSK-2586184A; G154578; GSK2586184; GSK 2586184A; Solcitinib
实验参考方法
In Vitro

In vitro activity: Solcitinib (formerly GSK2586184 or GLPG0778) is a potent, selective, and orally available Janus kinase (JAK)1 inhibitor being evaluated as a treatment for moderate-to-severe plaque-type psoriasis. It has an IC50 of 9.8 nM for JAK1 and is 11-, 55- and 23-fold more selective over JAK2, JAK3 and TYK2, respectively. 12 weeks of treatment with GSK2586184 resulted in clinical improvement and was generally well tolerated in patients with moderate-to-severe plaque-type psoriasis. Overall, the incidence of adverse events (AEs) was similar across treatment groups, and no relationship between frequency of AE and GSK2586184 dose was identified. Differential gene expression was observed in involved and uninvolved skin at baseline and in involved skin after 2 weeks of treatment with GSK2586184.


Kinase Assay: Solcitinib (formerly GSK2586184 or GLPG0778) is a potent, selective, and orally available Janus kinase (JAK)1 inhibitor being evaluated as a treatment for moderate-to-severe plaque-type psoriasis. It has an IC50 of 9.8 nM for JAK1 and is 11-, 55- and 23-fold more selective over JAK2, JAK3 and TYK2, respectively.

In Vivo12 weeks of treatment with GSK2586184 resulted in clinical improvement and was generally well tolerated in patients with moderate-to-severe plaque-type psoriasis. Overall, the incidence of adverse events (AEs) was similar across treatment groups, and no relationship between frequency of AE and GSK2586184 dose was identified. Differential gene expression was observed in involved and uninvolved skin at baseline and in involved skin after 2 weeks of treatment with GSK2586184.
Animal model Clinical trials
Formulation & Dosage Oral; 100 mg, 200 mg and 400 mg GSK2586184 twice-daily groups
References Br J Dermatol. 2016 May;174(5):985-95.