AAK1-IN-4 NEW
| Price | $1520 | $1980 | $2500 |
| Package | 25mg | 50mg | 100mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2025-04-30 |
Product Details
| Product Name: AAK1-IN-4 | CAS No.: 1815612-79-3 |
| Supply Ability: 10g | Release date: 2025/04/30 |
Product Introduction
Bioactivity
| Name | AAK1-IN-4 |
| 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 0.5 μM for 0-10 minutes shows significant cell potency with a value of 2.4 in liver microsomes and high metabolic stability, with values of 95, 95, and 93 in human, rat, and mouse microsomes respectively, without detected 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries， 10000+ Noval Small Molecucles，16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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United States- Since: 2011-01-07
- Address: 36 Washington Street, Wellesley Hill, Massachusetts, USA
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