1. Neuronal Signaling
    Membrane Transporter/Ion Channel
  2. Serotonin Transporter
    Potassium Channel
  3. Sibutramine hydrochloride monohydrate

Sibutramine hydrochloride monohydrate (Synonyms: BTS 54-524 hydrochloride monohydrate)

Cat. No.: HY-14470
Handling Instructions

Sibutramine hydrochloride monohydrate is a novel 5-HT (serotonin) and noradrenaline reuptake inhibitor (SNRI). The IC50 for Sibutramine block of voltage-gated K+ channel (KV)4.3 is 17.3 μM.

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Sibutramine hydrochloride monohydrate Chemical Structure

Sibutramine hydrochloride monohydrate Chemical Structure

CAS No. : 125494-59-9

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Sibutramine hydrochloride monohydrate is a novel 5-HT (serotonin) and noradrenaline reuptake inhibitor (SNRI). The IC50 for Sibutramine block of voltage-gated K+ channel (KV)4.3 is 17.3 μM.

IC50 & Target

5-HT (serotonin) reuptake[1]
IC50: 17.3 μM (KV4.3) [2]

In Vitro

Sibutramine is a novel 5-HT (serotonin) and noradrenaline reuptake inhibitor (SNRI). Sibutramine reduces the food intake of rodents and this effect is partially or completely reversed by pretreating with 5-HT or noradrenaline antagonists, indicating that both neurotransmitters are involved in sibutramine's hypophagic effect[1]. Sibutramine causes the concentration-dependent block of the KV1.3 and KV3.1 currents with IC50s of 3.7 and 32.7 μM, respectively. The steady-state currents of KV1.3 and KV3.1 are decreased by Sibutramine in a concentration-dependent manner with IC50s of 3.7±0.7 (n=6) and 32.7±5.0 μM (n=5), respectively[2].

In Vivo

Sibutramine (SIB) (5 mg/kg ip), which blocks the reuptake of both 5-hydroxytryptamine (5-HT) and noradrenaline (NA), also requires ARC pro-opiomelanocortin (POMC) neurons to achieve its appetitive effects in male and female mice. Sibutramine (5 mg/kg) suppresses 3-hour dark cycle food intake to a comparable extent in young adult and middle-aged male and female POMC-EGFP mice[3]. In normal Wistar rats, 3 mg/kg Sibutramine produces a marked (~30%) inhibition of food intake on the first day of dosing. Consistent with published data, the effects of Sibutramine on food intake diminished with time, although cumulative food intake over the 9-day study is significantly (P<0.001) lower in Sibutramine-treated (213.3±5.7 g) than in vehicle-treated (260.2±3.0 g) rats. Sibutramine also significantly reduces overall body weight gain (vehicle 30±2 g, Sibutramine 14±3 g; P<0.001)[4].

Molecular Weight









Room temperature in continental US; may vary elsewhere.


Please store the product under the recommended conditions in the Certificate of Analysis.

Kinase Assay

Sibutramine is dissolved in the bath solution to give a 30 mM stock solution[2].
The KV4.3, KV1.3, and KV3.1 cDNA are stably transfected into CHO cells using the Lipofectamine reagent. CHO cells are maintained in Iscove's modified Dulbecco's medium supplemented with 10% fetal bovine serum, 0.1 mM hypoxanthine, and 0.01 mM thymidine in a humidified 5% CO2 incubator at 37°C. The transfected cells are exchanged with fresh Iscove's modified Dulbecco's medium containing 0.3 mg/mL Geneticin (G-418), and they are passed at 2- to 3-day intervals using a brief trypsin-EDTA treatment. The cells are dissociated and seeded onto glass coverslips (diameter 12 mm) in a 35 mm dish 1 day before use. For electrophysiological experiments, coverslips with attached cells are transferred to a recording chamber (RC-13). The chamber is superfused at a rate of 0.5 mL/min with normal external solution at room temperature (22-24°C). The Origin 7.0 software program is used for the analysis. The concentration-response data are fit to the following Hill equation: y=1/(1+([D]/IC50)n), where IC50 is the concentration of Sibutramine required to produce a 50% block, [D] is the concentration of Sibutramine, and n the Hill coefficient[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

POMCfneo/fneo and wild-type littermates and POMC-EGFP young adult, and middle-aged adult mice are individually housed for 1 week before experimentation and received a habituation ip injection of vehicle 1 day before experimentation. Mice are then treated with vehicle, Lorcaserin (8 mg/kg), D-fenfluramine (3 mg/kg), or Sibutramine (5 mg/kg) 45 minutes before the onset of the dark cycle (lights on at 7:00 AM and off at 7:00 PM) and food is removed. At the onset of the dark cycle, chow pellets are replaced and 3- to 4-hour food intake measured. These studies are performed using a within subjects experimental design, with a minimum of a 3-day treatment-free period.
Male Wistar and obese (fa/fa) Zucker rats (ZuckerfLIS/Alpkh) are used. Sprague-Dawley rats are used. NPY5RA-972 (10 mg/kg, n=7) or vehicle (n=6) is dosed (p.o.) twice daily (at 06:00 h and 16:00 h). For 3 days before commencement of dosing with compound, rats are accustomed to handling and dosing with vehicle only. Food intake and body weight are measured daily. A positive control group (n=7) receiving Sibutramine is included in the chronic studies. Sibutramine is a marketed appetite-suppressant drug that acts principally by inhibiting the reuptake of serotonin and norepinephrine. Sibutramine is dosed at 3 mg/kg once daily (at 16:00 h). Sibutramine-treated rats also receive a dose of vehicle (at 06:00 h) to maintain consistency of procedures across all groups.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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Sibutramine hydrochlorideBTS 54-524 hydrochlorideSerotonin TransporterPotassium Channel5-HTTSERTSLC6A4KcsAInhibitorinhibitorinhibit

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