Shopping Cart
- Remove All
Your shopping cart is currently empty
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | 8-10 weeks | |
50 mg | $1,980 | 8-10 weeks | |
100 mg | $2,500 | 8-10 weeks |
Description | AAK1-IN-4 is a potent and specific inhibitor of adaptor protein-2-associated kinase 1 (AAK1), capable of efficiently penetrating the central nervous system and exhibiting oral bioactivity. It has demonstrated a high degree of selectivity with an AAK1 inhibitory concentration (IC50) of 4.6 nM, a Filt dissociation constant (Ki) of 0.9 nM, and a cellular IC50 of 8.6 nM. AAK1-IN-4 holds promise as a valuable tool in the investigation of neuropathic pain [1]. |
In vitro | AAK1-IN-4 (compound 43) at a concentration of 0.5 μM for a duration of 0-10 minutes, demonstrates significant cell potency with a value of 2.4 in liver microsomes and exhibits high metabolic stability, evidenced by values of 95, 95, and 93 in human, rat, and mouse microsomes respectively, without any detected issues related to CYP inhibition [1]. |
In vivo | AAK1-IN-4, administered orally at a dosage of 3 mg/kg, substantially mitigates tactile allodynia, achieving nearly 80% pain response inhibition in a rat model of chronic constriction injury (CCI)-induced pain, alongside demonstrating considerable spinal cord penetration and an 8.8 spinal-cord-to-plasma concentration ratio. When dosage ranged from 1-10 mg/kg, AAK1-IN-4 significantly attenuated mechanical allodynia in a rat model of streptozotocin (STZ)-induced diabetic peripheral neuropathic pain (DPNP), with peak pain response inhibition exceeding 80% at 10 mg/kg and over 60% at 3 mg/kg. These findings underscore AAK1-IN-4's potent analgesic effects across different doses and neuropathic pain models, affirming its therapeutic potential. |
Molecular Weight | 372.46 |
Formula | C20H28N4O3 |
Cas No. | 1815612-79-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.