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tesofensine

Product Name
tesofensine
CAS No.
195875-84-4
Chemical Name
tesofensine
Synonyms
Tesofensine-13C-d3;Tesofensine 0.5mg Tablets;Tesofensine 500mcg Tablets;(1R,2R,3S,5S)-3-(3,4-Dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane;(1S,3S,4R,5R)-3-(3,4-dichlorophenyl)-4-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane;8-Azabicyclo[3.2.1]octane, 3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-, (1R,2R,3S,5S)-
CBNumber
CB12498844
Molecular Formula
C17H23Cl2NO
Formula Weight
328.28
MOL File
195875-84-4.mol
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tesofensine Property

Boiling point:
396.6±42.0 °C(Predicted)
Density 
1.161±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMF: 2 mg/mL,DMSO: 1 mg/mL,Ethanol: Slightly soluble,PBS (pH 7.2): 0.14 mg/mL
form 
A solid
pka
10.46±0.60(Predicted)
color 
White to off-white
Stability:
Hygroscopic
InChI
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
InChIKey
VCVWXKKWDOJNIT-ZOMKSWQUSA-N
SMILES
[C@@]12([H])N(C)[C@@]([H])(CC1)C[C@H](C1=CC=C(Cl)C(Cl)=C1)[C@H]2COCC
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

TRC
Product number
T136500
Product name
Tesofensine
Packaging
1mg
Price
$305
Updated
2021/12/16
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tesofensine Chemical Properties,Usage,Production

Description

Tesofensine ((1R, 2R, 3S, 5S)-3-(3, 4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane)) is an inhibitor of neuronal reuptake of dopamine, noradrenaline, and serotonin. Tesofensine was developed for the treatment of Alzheimer's and Parkinson's disease but lacked efficacy. Meta-analysis revealed that tesofensine (0.125–1.0 mg, once daily; oral) produced dose-dependent weight loss, and 32% of obese patients had ≥ 5% weight loss following 14 wk of treatment. Weight loss was accompanied by hypophagia, suggesting an appetite suppressant action[2].

History

Tesofensine is a dopamine, serotonin, and noradrenaline (triple) reuptake inhibitor originally developed by NeuroSearch for the treatment of Alzheimer's disease and Parkinson's disease. Development of the compound for these neurological indications was unsuccessful but significant weight loss was reported during the clinical trials in Parkinson's disease. Hence, tesofensine is now being developed by NeuroSearch for the treatment of obesity and type 2 diabetes[1].

Uses

Tesofensine, is a serotonin–noradrenaline–dopamine reuptake inhibitor from the phenyltropane family of drugs, which is currently in clinical development for the treatment of obesity.

in vivo

Tesofensine (a single dose of 0.1-3? mg/kg, s.c.) induces hypophagia in the DIO rat. A single dose of Tesofensine (0. 1-3?mg/kg, s.c.) robustly and dose dependently inhibits food intake in DIO rats over the 12?h nocturnal observation period. Daily administration of a moderate dose of Tesofensine (2.0?mg/kg, s.c.) over 16 days triggers a significant reduction in body weight after 4 days of administration relative to vehicle-treated controls[3].

Animal Model:Diet-induced obesity (DIO) rat[3]
Dosage:0.1-3?mg/kg
Administration:Administered subcutaneously (s.c.); a single dose (acute treatment)
Result:The threshold dose for inhibition of total food intake was 1.0?mg/kg.
The ED50 for inhibition of total food intake in DIO rats was estimated to be 1.3?mg/kg.
Animal Model:Diet-induced obesity (DIO) rat[3]
Dosage:2.0?mg/kg
Administration:Administered subcutaneously (s.c.) daily for over 16 days (chronic treatment)
Result:The average relative decrease in the body weight of tesofensine-treated DIO rats over the entire treatment period was 8.6±1.4%.
When comparing to vehicle controls, the relative weight loss with tesofensine was 13.8±1.4%.

References

[1] Dourish, C. J. Wilding and J. Halford. “Anti-obesity Drugs: From Animal Models to Clinical Efficacy.”Animal and Translational Models for CNS Drug Discovery 2008: 271-315.
[2] Vidya Narayanaswami, Linda P. Dwoskin. “Obesity: Current and potential pharmacotherapeutics and targets.” Pharmacology Therapeutics 170 (2017): Pages 116-147.

tesofensine Preparation Products And Raw materials

Raw materials

Preparation Products

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tesofensine Suppliers

J & K SCIENTIFIC LTD.
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View Lastest Price from tesofensine manufacturers

Shaanxi Dideu Medichem Co. Ltd
Product
Tesofensine 195875-84-4
Price
US $1.00/KG
Min. Order
1KG
Purity
99%+
Supply Ability
200 kgs
Release date
2025-09-13
Shaanxi Dideu Medichem Co. Ltd
Product
tesofensine 195875-84-4
Price
US $0.10/KG
Min. Order
1KG
Purity
99.0%
Supply Ability
1000 tons
Release date
2025-08-26
Ningbo Qingteng Plastic Cost.,Ltd.
Product
Tesofensine 195875-84-4
Price
US $10.00/box
Min. Order
1box
Purity
99%
Supply Ability
100000box
Release date
2025-08-25

195875-84-4, tesofensineRelated Search:


  • (1S,3S,4R,5R)-3-(3,4-dichlorophenyl)-4-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane
  • (1R,2R,3S,5S)-3-(3,4-Dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane
  • Tesofensine-13C-d3
  • 8-Azabicyclo[3.2.1]octane, 3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-, (1R,2R,3S,5S)-
  • Tesofensine 500mcg Tablets
  • Tesofensine 0.5mg Tablets
  • 195875-84-4