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Autotaxin inhibitor compound 1

Names

[ CAS No. ]:
1619971-30-0

[ Name ]:
Autotaxin inhibitor compound 1

Biological Activity

[Description]:

Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK/PD relationship. Autotaxin-IN-1 is used in treatment of osteoarthritis pain[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)
Research Areas >> Inflammation/Immunology

[Target]

Autotaxin:2 nM (IC50)


[In Vivo]

Autotaxin-IN-1 (i.v.; 1.0mg/kg) has T1/2 of 1.14 hours[1]. Autotaxin-IN-1 (p.o.; 10 mg/kg) has Cmax of 660 nM and AUC of 3440 nM•h[1]. Animal Model: Normal rat[1] Dosage: 1.0 mg/kg, 10 mg/kg (Pharmacokinetic Study) Administration: I.v. (1.0 mg/kg); p.o. (10 mg/kg) Result: Has T1/2 of 1.14 hours (i.v.; 1.0mg/kg). Has Cmax of 660 nM and AUC of 3440 nM▪h (p.o.; 10 mg/kg).

[References]

[1]. Jones SB, et al. Novel Autotaxin Inhibitors for the Treatment of Osteoarthritis Pain: Lead Optimization via Structure-Based Drug Design. ACS Med Chem Lett. 2016 Aug 2;7(9):857-61.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H23N7O2

[ Molecular Weight ]:
405.45

[ Storage condition ]:
-20°C

Related Compounds