1815613-44-5

1815613-44-5 structure
1815613-44-5 structure
  • Name: AAK1-IN-5
  • Chemical Name: AAK1-IN-5
  • CAS Number: 1815613-44-5
  • Molecular Formula: C19H23F4N3O
  • Molecular Weight: 385.40
  • Create Date: 2022-05-24 23:56:52
  • Modify Date: 2024-01-10 09:23:31
  • AAK1-IN-5 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC50 of 1.2 nM, Filt Ki of 0.05 nM, and cell IC50 of 0.5 nM). AAK1-IN-4 has the potential for the research for neuropathic pain[1].

Name AAK1-IN-5
Description AAK1-IN-5 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC50 of 1.2 nM, Filt Ki of 0.05 nM, and cell IC50 of 0.5 nM). AAK1-IN-4 has the potential for the research for neuropathic pain[1].
Related Catalog
Target

IC50: 1.2 nM (AAK1)[1]. Ki: 0.05 nM (AAK1)[1]

In Vitro AAK1-IN-5 (compound 58) (0.5 μM, 0-10 min) has a good metabolic stability, with half-life values of over 120 min in human and mouse liver microsomes, and 76.0, 17.6, 26.0 min in rat, cynomolgus monkey, and dog, respectively[1].
In Vivo AAK1-IN-5 (compound 58) can reduce hyperalgesia in SD rats (chronic constriction injury) efficiently with good efficacy observed at doses of 1 and 3 mg/kg[1]. Animal Model: Male Sprague-Dawley rats (chronic constriction injury, CCI)[1] Dosage: 1-3 mg/kg Administration: p.o., 0-5.5 hours Result: Reduced hyperalgesia in CCI rats efficiently with good efficacy observed at doses of 1 and 3 mg/kg.
References

[1]. Luo G, et al. Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain. J Med Chem. 2022;65(6):4534-4564.

Molecular Formula C19H23F4N3O
Molecular Weight 385.40
The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.