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MedKoo Cat#: 125995 | Name: Tesofensine citrate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Tesofensine, also known as NS-2330, is a serotonin–noradrenaline–dopamine reuptake inhibitor potentially for the treatment of obesity.

Chemical Structure

Tesofensine citrate
CAS#861205-83-6 (citrate)

Theoretical Analysis

MedKoo Cat#: 125995

Name: Tesofensine citrate

CAS#: 861205-83-6 (citrate)

Chemical Formula: C23H31Cl2NO8

Exact Mass: 519.1427

Molecular Weight: 520.40

Elemental Analysis: C, 53.08; H, 6.00; Cl, 13.62; N, 2.69; O, 24.59

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
195875-84-4 (free base) Tesofensine Tartrate 861205-83-6 (citrate)
Synonym
Tesofensine citrate; NS-2330; NS2330; NS 2330; Tesofensine;
IUPAC/Chemical Name
(1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane 2-hydroxypropane-1,2,3-tricarboxylate
InChi Key
ZIVJUFNVDKADJT-BEDQTAKTSA-N
InChi Code
InChI=1S/C17H23Cl2NO.C6H8O7/c1-3-21-10-14-13(9-12-5-7-17(14)20(12)2)11-4-6-15(18)16(19)8-11;7-3(8)1-6(13,5(11)12)2-4(9)10/h4,6,8,12-14,17H,3,5,7,9-10H2,1-2H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/t12-,13+,14+,17+;/m0./s1
SMILES Code
OC(=O)CC(O)(CC(O)=O)C(O)=O.CCOC[C@H]1[C@H]2CC[C@@H](C[C@@H]1C3=CC(Cl)=C(Cl)C=C3)N2C
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 -4 C for short term (days to weeks) or -20 C for long term(months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 520.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Hansen HH, Jensen MM, Overgaard A, Weikop P, Mikkelsen JD. Tesofensine induces appetite suppression and weight loss with reversal of low forebrain dopamine levels in the diet-induced obese rat. Pharmacol Biochem Behav. 2013 Sep;110:265-71. doi: 10.1016/j.pbb.2013.07.018. PubMed PMID: 23932919. 2: Bentzen BH, Grunnet M, Hyveled-Nielsen L, Sundgreen C, Lassen JB, Hansen HH. Anti-hypertensive treatment preserves appetite suppression while preventing cardiovascular adverse effects of tesofensine in rats. Obesity (Silver Spring). 2013 May;21(5):985-92. doi: 10.1002/oby.20122. PubMed PMID: 23784901. 3: van de Giessen E, de Bruin K, la Fleur SE, van den Brink W, Booij J. Triple monoamine inhibitor tesofensine decreases food intake, body weight, and striatal dopamine D2/D3 receptor availability in diet-induced obese rats. Eur Neuropsychopharmacol. 2012 Apr;22(4):290-9. doi: 10.1016/j.euroneuro.2011.07.015. PubMed PMID: 21889317. 4: Schoedel KA, Meier D, Chakraborty B, Manniche PM, Sellers EM. Subjective and objective effects of the novel triple reuptake inhibitor tesofensine in recreational stimulant users. Clin Pharmacol Ther. 2010 Jul;88(1):69-78. doi: 10.1038/clpt.2010.67. PubMed PMID: 20520602. 5: Hansen HH, Hansen G, Tang-Christensen M, Larsen PJ, Axel AM, Raben A, Mikkelsen JD. The novel triple monoamine reuptake inhibitor tesofensine induces sustained weight loss and improves glycemic control in the diet-induced obese rat: comparison to sibutramine and rimonabant. Eur J Pharmacol. 2010 Jun 25;636(1-3):88-95. doi: 10.1016/j.ejphar.2010.03.026. PubMed PMID: 20385125. 6: Axel AM, Mikkelsen JD, Hansen HH. Tesofensine, a novel triple monoamine reuptake inhibitor, induces appetite suppression by indirect stimulation of alpha1 adrenoceptor and dopamine D1 receptor pathways in the diet-induced obese rat. Neuropsychopharmacology. 2010 Jun;35(7):1464-76. doi: 10.1038/npp.2010.16. PubMed PMID: 20200509; PubMed Central PMCID: PMC3055463. 7: Bello NT, Zahner MR. Tesofensine, a monoamine reuptake inhibitor for the treatment of obesity. Curr Opin Investig Drugs. 2009 Oct;10(10):1105-16. Review. PubMed PMID: 19777399. 8: Astrup A, Madsbad S, Breum L, Jensen TJ, Kroustrup JP, Larsen TM. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. Lancet. 2008 Nov 29;372(9653):1906-13. doi: 10.1016/S0140-6736(08)61525-1. PubMed PMID: 18950853. 9: Doggrell SA. Tesofensine--a novel potent weight loss medicine. Evaluation of: Astrup A, Breum L, Jensen TJ, Kroustrup JP, Larsen TM. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. Lancet 2008;372:1906-13. Expert Opin Investig Drugs. 2009 Jul;18(7):1043-6. doi: 10.1517/13543780902967632. PubMed PMID: 19548858. 10: Lehr T, Staab A, Tillmann C, Trommeshauser D, Schaefer HG, Kloft C. A quantitative enterohepatic circulation model: development and evaluation with tesofensine and meloxicam. Clin Pharmacokinet. 2009;48(8):529-42. doi: 10.2165/11313370-000000000-00000. PubMed PMID: 19705923. 11: Nielsen AL, Larsen TM, Madsbad S, Breum L, Jensen TJ, Kroustrup JP, Astrup A. [The effect of tesofensine on body weight and body composition in obese subjects--secondary publication]. Ugeskr Laeger. 2009 Oct 5;171(41):2974-7. Danish. PubMed PMID: 19824222. 12: Lehr T, Staab A, Trommeshauser D, Schaefer HG, Kloft C. Quantitative pharmacology approach in Alzheimer's disease: efficacy modeling of early clinical data to predict clinical outcome of tesofensine. AAPS J. 2010 Jun;12(2):117-29. doi: 10.1208/s12248-009-9164-6. PubMed PMID: 20077053; PubMed Central PMCID: PMC2844519. 13: Lehr T, Staab A, Tillmann C, Nielsen EØ, Trommeshauser D, Schaefer HG, Kloft C. Contribution of the active metabolite M1 to the pharmacological activity of tesofensine in vivo: a pharmacokinetic-pharmacodynamic modelling approach. Br J Pharmacol. 2008 Jan;153(1):164-74. PubMed PMID: 17982477; PubMed Central PMCID: PMC2199391. 14: Rascol O, Poewe W, Lees A, Aristin M, Salin L, Juhel N, Waldhauser L, Schindler T; ADVANS Study Group.. Tesofensine (NS 2330), a monoamine reuptake inhibitor, in patients with advanced Parkinson disease and motor fluctuations: the ADVANS Study. Arch Neurol. 2008 May;65(5):577-83. doi: 10.1001/archneur.65.5.577. PubMed PMID: 18474731. 15: Appel L, Bergström M, Buus Lassen J, Långström B. Tesofensine, a novel triple monoamine re-uptake inhibitor with anti-obesity effects: dopamine transporter occupancy as measured by PET. Eur Neuropsychopharmacol. 2014 Feb;24(2):251-61. doi: 10.1016/j.euroneuro.2013.10.007. PubMed PMID: 24239329. 16: Gilbert JA, Gasteyger C, Raben A, Meier DH, Astrup A, Sjödin A. The effect of tesofensine on appetite sensations. Obesity (Silver Spring). 2012 Mar;20(3):553-61. doi: 10.1038/oby.2011.197. PubMed PMID: 21720440. 17: Larsen MH, Rosenbrock H, Sams-Dodd F, Mikkelsen JD. Expression of brain derived neurotrophic factor, activity-regulated cytoskeleton protein mRNA, and enhancement of adult hippocampal neurogenesis in rats after sub-chronic and chronic treatment with the triple monoamine re-uptake inhibitor tesofensine. Eur J Pharmacol. 2007 Jan 26;555(2-3):115-21. PubMed PMID: 17112503. 18: Sjödin A, Gasteyger C, Nielsen AL, Raben A, Mikkelsen JD, Jensen JK, Meier D, Astrup A. The effect of the triple monoamine reuptake inhibitor tesofensine on energy metabolism and appetite in overweight and moderately obese men. Int J Obes (Lond). 2010 Nov;34(11):1634-43. doi: 10.1038/ijo.2010.87. PubMed PMID: 20479765. 19: Astrup A, Meier DH, Mikkelsen BO, Villumsen JS, Larsen TM. Weight loss produced by tesofensine in patients with Parkinson's or Alzheimer's disease. Obesity (Silver Spring). 2008 Jun;16(6):1363-9. doi: 10.1038/oby.2008.56. PubMed PMID: 18356831. 20: Expression of concern--effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. Lancet. 2013 Apr 6;381(9873):1167. doi: 10.1016/S0140-6736(13)60778-3. PubMed PMID: 23561987.

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