Upadacitinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Upadacitinib (ABT-494) 是一种有效的选择性 JAK1 抑制剂，细胞 IC50 为 8 nM，生化 IC50 为 40 nM。

Upadacitinib (ABT-494) is a potent and selective JAK1 inhibitor with celluar IC50 of 8 nM, biochemical IC50 of 40 nM; displays 74-fold and 50-fold selectivity over JAK2 and JAK3, respectively; a second-generation JAK inhibitor in development for rheumatoid arthritis.Rheumatoid Arthritis Phase 3 Clinical(In Vitro):In biochemical assays, Upadacitinib is 74-fold more selective for JAK-1 than for JAK-2 (which is involved in erythropoiesis) and 58-fold more selective for JAK-1 than for JAK-3 (which is involved in immunosurveillance). The enhanced selectivity of Upadacitinib for JAK-1 over JAK-2 and JAK-3 may offer an improved benefit–risk profile in patients with RA range.(In Vivo):Upadacitinib (0.1-10 mg/kg; oral gavage; twice a day for 10 days) demonstrates efficacy in rat arthritis models.

In biochemical assays, Upadacitinibis 74-fold more selective for JAK-1 than for JAK-2 (which is involved in erythropoiesis) and 58-fold more selective for JAK-1 than for JAK-3 (which is involved in immunosurveillance). The enhanced selectivity of Upadacitinibfor JAK-1 over JAK-2 and JAK-3 may offer an improved benefit–risk profile in patients with RA range.

Upadacitinib (0.1-10 mg/kg; oral gavage; twice a day for 10 days) demonstrates efficacy in rat arthritis models. Animal Model:Female Lewis rats (Rat adjuvant-induced arthritis model)Dosage:0.1, 0.3, 1, 3, 10 mg/kg Administration:Oral gavage; twice a day for 10 days Result:Inhibited disease pathology in rat adjuvant induced arthritis.

ABT-494 | ABT494 | ABT 494

Angiogenesis

JAK

JAK1|JAK2

Inflammation/Immunology

Rheumatoid Arthritis

1310726-60-3

380.3676

C17H19F3N6O

>98% (HPLC)

DMSO: ≥ 22 mg/mL

CCC1CN(CC1C2=CN=C3N2C4=C(NC=C4)N=C3)C(=O)NCC(F)(F)F

1-Pyrrolidinecarboxamide, 3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)-, (3S,4R)-

(-20℃)

With Ice Pack

≥ 2 years