AF40431 is the first reported small molecule ligand of sortilin with IC50 of 4.4 µM and Kd of 0.7 µM. AF40431 binds to the neurotensin binding site of sortilin.
| Molecular Weight | 319.35 |
| Formula | C17H21NO5 |
| CAS Number | 181125-92-8 |
| Solubility (25°C) | DMSO ≥ 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Neurotensin Receptor Products |
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| Kinetensin
Kinetensin is a neurotensin-like peptide isolated from pepsin-treated human plasma. |
| [Lys8, Lys9]-Neurotensin (8-13)
[Lys8, Lys9]-Neurotensin (8-13) (JMV438), a Neurotensin analog, exerts its analgesic effects through activation of the G protein-coupled receptors NTS1 and NTS2. |
| [D-Trp11]-Neurotensin
[D-Trp11]-Neurotensin, an analogue of Neurotensin (NT), is a selective antagonist of NT in perfused rat hearts but behaves as a full agonist in guinea pig atria and rat stomach strips. |
| Contulakin G
Contulakin G is an O-glycosylated invertebrate neurotensin. |
| Acetyl neurotensin (8-13)
Acetyl neurotensin (8-13) is the shortest analog of neurotensin with full binding and pharmacological activities. |
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