| Identification | Back Directory | [Name]
2-Thiophenecarboxamide, N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-4-(6-chloropyrazolo[1,5-a]pyrimidin-3-yl)-5-methyl- | [CAS]
1314893-26-9 | [Synonyms]
MARK-IN-2
MARK IN 2,MARKIN2
2-Thiophenecarboxamide, N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-4-(6-chloropyrazolo[1,5-a]pyrimidin-3-yl)-5-methyl- | [Molecular Formula]
C18H18ClF2N5OS | [MDL Number]
MFCD31692329 | [MOL File]
1314893-26-9.mol | [Molecular Weight]
425.88 |
| Hazard Information | Back Directory | [Description]
MARK-IN-2 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of 5 nM. MARK-IN-2 (Compound 27) is a potent MARK inhibitor. Inhibition of MARK represents a potentially attractive means of arresting neurofibrillary tangle pathology in Alzheimer's disease. MARK-IN-2 inhibits MARK3 with an IC50 of 5 nM. MARK-IN-2 also inhibits MARK3 in primary cell culture of rat cortical neurons with an IC50 of 280 nM[1]. Characterization of the i.v. pharmacokinetic properties of MARK-IN-2 in rat and dog reveals reasonable volumes of distribution but moderate to high clearance and short half-lives. MARK-IN-2 (Compound 27) has moderate terminal elimination half-life (t1/2=0.7 h, and 1 h for rat and dog) [1]. | [Uses]
MARK-IN-2 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of 5 nM. | [in vivo]
Characterization of the i.v. pharmacokinetic properties of MARK-IN-2 in rat and dog reveals reasonable volumes of distribution but moderate to high clearance and short half-lives. MARK-IN-2 (Compound 27) has moderate terminal elimination half-life (t1/2=0.7 h, and 1 h for rat and dog) [1]. | [References]
[1]. Sloman DL, et al. Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4362-6. |
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