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MedKoo Cat#: 319672 | Name: Liafensine

Description:

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

Liafensine, also known as BMS-820836, is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI). In vitro, Liafensine exhibits potent inhibition of the human serotonin transporter (SERT, IC₅₀ ≈ 2.9 nM), norepinephrine transporter (NET, IC₅₀ ≈ 8.8 nM), and dopamine transporter (DAT, IC₅₀ ≈ 27 nM), indicating a balanced triple reuptake inhibition profile. In phase II clinical trials, it showed antidepressant activity comparable to escitalopram, but it was discontinued due to insufficient differentiation in efficacy and concerns over its side effect profile, including increased blood pressure and insomnia.

Chemical Structure

Liafensine
Liafensine
CAS#1198790-53-2

Theoretical Analysis

MedKoo Cat#: 319672

Name: Liafensine

CAS#: 1198790-53-2

Chemical Formula: C24H22N4

Exact Mass: 366.1844

Molecular Weight: 366.47

Elemental Analysis: C, 78.66; H, 6.05; N, 15.29

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 #
No Data
Synonym
BMS-820836; BMS 820836; BMS820836; Liafensine
IUPAC/Chemical Name
(S)-6-(2-methyl-4-(naphthalen-2-yl)-1,2,3,4-tetrahydroisoquinolin-7-yl)pyridazin-3-amine
InChi Key
VCIBGDSRPUOBOG-QFIPXVFZSA-N
InChi Code
InChI=1S/C24H22N4/c1-28-14-20-13-19(23-10-11-24(25)27-26-23)8-9-21(20)22(15-28)18-7-6-16-4-2-3-5-17(16)12-18/h2-13,22H,14-15H2,1H3,(H2,25,27)/t22-/m0/s1
SMILES Code
NC1=NN=C(C2=CC3=C(C=C2)[C@H](C4=CC=C5C=CC=CC5=C4)CN(C)C3)C=C1
Appearance
Solid powder
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
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
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 366.47 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: Bhagwagar Z, Torbeyns A, Hennicken D, Zheng M, Dunlop BW, Mathew SJ, Khan A, Weisler R, Nelson C, Shelton R, Thase ME, Lane R. Assessment of the Efficacy and Safety of BMS-820836 in Patients With Treatment-Resistant Major Depression: Results From 2 Randomized, Double-Blind Studies. J Clin Psychopharmacol. 2015 Aug;35(4):454-9. doi: 10.1097/JCP.0000000000000335. PubMed PMID: 25961781. 2: Zheng M, Burt D, Chan W, Hawthorne D, Gasior M, Bhagwagar Z, Keswani S, AbuTarif M, Bertz R. Comparison of different QT interval correction methods for heart rate and QT beat-to-beat method in a thorough QT study of triple monoamine reuptake inhibitor BMS-820836. J Clin Pharmacol. 2015 Oct;55(10):1137-46. doi: 10.1002/jcph.528. Epub 2015 Jun 9. PubMed PMID: 25904041. 3: Zheng M, Appel L, Luo F, Lane R, Burt D, Risinger R, Antoni G, Cahir M, Keswani S, Hayes W, Bhagwagar Z. Safety, pharmacokinetic, and positron emission tomography evaluation of serotonin and dopamine transporter occupancy following multiple-dose administration of the triple monoamine reuptake inhibitor BMS-820836. Psychopharmacology (Berl). 2015 Feb;232(3):529-40. doi: 10.1007/s00213-014-3688-x. Epub 2014 Aug 14. PubMed PMID: 25116481. 4: Risinger R, Bhagwagar Z, Luo F, Cahir M, Miler L, Mendonza AE, Meyer JH, Zheng M, Hayes W. Evaluation of safety and tolerability, pharmacokinetics, and pharmacodynamics of BMS-820836 in healthy subjects: a placebo-controlled, ascending single-dose study. Psychopharmacology (Berl). 2014 Jun;231(11):2299-310. doi: 10.1007/s00213-013-3391-3. Epub 2013 Dec 15. PubMed PMID: 24337079.

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