| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Tesofensine (NS-2330) is an investigational drug acting as a pre-synaptic serotonin–noradrenaline–dopamine reuptake inhibitor and has the potential for the treatment of obesity. Tesofensine was originally developed by a Danish biotechnology company, NeuroSearch, who transferred the rights to Saniona in 2014.
| ln Vivo |
In DIO rats, tesofensine (subcutaneous injection, single dose, 0.1-3 mg/kg) can cause hypophagia. Over the course of a 12-hour nocturnal observation period, DIO rats' food intake was significantly and dose-dependently decreased by a single dose of Tesofensine (0.1-3 mg/kg, sc). When tesofensine (2.0 mg/kg, subcutaneous injection) was administered daily for 16 days, there was a notable reduction in weight after 4 days when compared to the vehicle-treated controls [3].
|
|---|---|
| Animal Protocol |
Animal/Disease Models: Diet-induced obesity (DIO) rats [3]
Doses: 0.1-3 mg/kg Route of Administration: subcutaneousadministration (sc); single dose (acute treatment) Experimental Results: The threshold dose for inhibiting total food intake is 1.0 mg/kg. The ED50 for inhibition of total food intake in DIO rats is estimated to be 1.3 mg/kg. Animal/Disease Models: Diet-induced obesity (DIO) rats [3] Doses: 2.0 mg/kg Route of Administration: Daily subcutaneousadministration for more than 16 days (long-term treatment) Experimental Results: Average body weight after tisofensin treatment The relative decrease in DIO rats during the entire treatment period was 8.6±1.4%. The relative weight loss for tisofensin was 13.8 ± 1.4% compared to vehicle control. |
| References |
|
| Additional Infomation |
Drug Indication
Investigated for use/treatment in alzheimer's disease, parkinson's disease, and obesity. Mechanism of Action Tesofensine is a Serotonin-norepinephrine-dopamine-reuptake-inhibitor (SNDRI). SNDRIs are a class of psychoactive antidepressants. They act upon neurotransmitters in the brain, namely, serotonin, norepinephrine and dopamine. These three biogenic monoamines are associated with depression and increasing the availability in the brain is one method used to treat the condition. |
| Molecular Formula |
C17H23CL2NO
|
|---|---|
| Molecular Weight |
328.27662
|
| Exact Mass |
327.116
|
| CAS # |
195875-84-4
|
| Related CAS # |
Related CAS#:402856-42-2
|
| PubChem CID |
11370864
|
| Appearance |
White to off-white solid powder
|
| Density |
1.161 g/cm3
|
| Boiling Point |
396.6ºC at 760 mmHg
|
| Flash Point |
193.7ºC
|
| LogP |
4.534
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
21
|
| Complexity |
354
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
CCOC[C@H]1[C@H]2CC[C@H](N2C)C[C@@H]1C3=CC(=C(C=C3)Cl)Cl
|
| InChi Key |
VCVWXKKWDOJNIT-ZOMKSWQUSA-N
|
| InChi Code |
InChI=1S/C17H23Cl2NO/c1-3-21-10-14-13(9-12-5-7-17(14)20(12)2)11-4-6-15(18)16(19)8-11/h4,6,8,12-14,17H,3,5,7,9-10H2,1-2H3/t12-,13+,14+,17+/m0/s1
|
| Chemical Name |
(1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane
|
| Synonyms |
Tesofensine NS-2330 NS2330 NS 2330
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~2 mg/mL (~6.09 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0462 mL | 15.2309 mL | 30.4618 mL | |
| 5 mM | 0.6092 mL | 3.0462 mL | 6.0924 mL | |
| 10 mM | 0.3046 mL | 1.5231 mL | 3.0462 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
A multi-centre, double-blind, parallel-group, randomised, placebo-controlled study to investigate the safety and tolerability of 0.25, 0.5 and 1.0 mg NS 2330 orally and once daily during a 14-week treatment period as add-on to 10 mg donepezil once daily in patients with mild to moderate dementia of the Alzheimer's type.
CTID: null
Phase: Phase 2 Status: Completed
Date: 2004-08-09
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA