Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM).
| Molecular Weight | 328.28 |
| Formula | C17H23Cl2NO |
| CAS Number | 195875-84-4 |
| Form | Solid |
| Solubility (25°C) | DMSO 2 mg/mL (ultrasonic and warming) |
| Storage | 4°C, protect from light |
| 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.
[4] Agnès Sommet, et al. Lancet. Tesofensine and weight loss
| Related Dopamine Transporter Products |
|---|
| Z1078601926
Z1078601926 is an allosterical inhibitor of human dopamine transporter (hDAT). |
| RTI 336
RTI 336 is a phenyltropane analog, as well as a potent and selective dopamine transporter (DAT) inhibitor. |
| Dasotraline
Dasotraline is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively. |
| Bupropion morpholinol
Bupropion morpholinol (Hydroxy Bupropion) is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities. |
| (R)-Phenylpiracetam
(R)-Phenylpiracetam (MRZ 9547) is a dopamine transporter (DAT) inhibitor (Ki: 14.8 μM; IC50: 65.5 μM). (R)-Phenylpiracetam can be used for the research of the neurological or neuropsychiatric disorders. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
