| Identification | Back Directory | [Name]
Autotaxin inhibitor compound 1
(Autotaxin-IN-1) | [CAS]
1619971-30-0 | [Synonyms]
Autotaxin-IN-1
Autotaxin inhibitor compound 1
Autotaxin inhibitor compound 1
(Autotaxin-IN-1)
Ethanone, 1-[2-[(2,3-dihydro-1H-inden-2-yl)amino]-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidin-6-yl]-2-[2-(1H-1,2,3-triazol-5-yl)ethoxy]- | [Molecular Formula]
C21H23N7O2 | [MDL Number]
MFCD32201059 | [MOL File]
1619971-30-0.mol | [Molecular Weight]
405.45 |
| Hazard Information | Back Directory | [Description]
Autotaxin-IN-1 is a potent inhibitor of autotaxin. | [Uses]
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]. | [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).
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| [IC 50]
Autotaxin: 2 nM (IC50) | [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. DOI:10.1021/acsmedchemlett.6b00207 |
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