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Sibutramine hydrochloride monohydrate

CAS# 125494-59-9

Sibutramine hydrochloride monohydrate

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Chemical structure

Sibutramine hydrochloride monohydrate

3D structure

Chemical Properties of Sibutramine hydrochloride monohydrate

Cas No. 125494-59-9 SDF Download SDF
PubChem ID 64765 Appearance Powder
Formula C17H29Cl2NO M.Wt 334.32
Type of Compound N/A Storage Desiccate at -20°C
Synonyms BTS 54-524 hydrochloride monohydrate
Solubility Soluble in DMSO
Chemical Name 1-[1-(4-chlorophenyl)cyclobutyl]-N,N,3-trimethylbutan-1-amine;hydrate;hydrochloride
SMILES CC(C)CC(C1(CCC1)C2=CC=C(C=C2)Cl)N(C)C.O.Cl
Standard InChIKey KFNNPQDSPLWLCX-UHFFFAOYSA-N
Standard InChI InChI=1S/C17H26ClN.ClH.H2O/c1-13(2)12-16(19(3)4)17(10-5-11-17)14-6-8-15(18)9-7-14;;/h6-9,13,16H,5,10-12H2,1-4H3;1H;1H2
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Protocol

Kinase Assay [2]
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].

Animal Administration [3][4]
Mice[3] 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. Rats[4] 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.

References:
[1]. Heal DJ, et al. Sibutramine: a novel anti-obesity drug. A review of the pharmacological evidence to differentiate it from d-amphetamine and d-fenfluramine. Int J Obes Relat Metab Disord. 1998 Aug;22 Suppl 1:S18-28; discussion S29. [2]. Kim SE, et al. Open channel block of A-type, kv4.3, and delayed rectifier K+ channels, KV1.3 and KV3.1, bySibutramine. J Pharmacol Exp Ther. 2007 May;321(2):753-62. [3]. Burke LK, et al. 5-HT obesity medication efficacy via POMC activation is maintained during aging. Endocrinology. 2014 Oct;155(10):3732-8. [4]. Turnbull AV, et al. Selective antagonism of the NPY Y5 receptor does not have a major effect on feeding in rats. Diabetes. 2002 Aug;51(8):2441-9.

Sibutramine hydrochloride monohydrate Dilution Calculator

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Sibutramine hydrochloride monohydrate Molarity Calculator

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Preparing Stock Solutions of Sibutramine hydrochloride monohydrate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.9911 mL 14.9557 mL 29.9115 mL 59.8229 mL 74.7787 mL
5 mM 0.5982 mL 2.9911 mL 5.9823 mL 11.9646 mL 14.9557 mL
10 mM 0.2991 mL 1.4956 mL 2.9911 mL 5.9823 mL 7.4779 mL
50 mM 0.0598 mL 0.2991 mL 0.5982 mL 1.1965 mL 1.4956 mL
100 mM 0.0299 mL 0.1496 mL 0.2991 mL 0.5982 mL 0.7478 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Sibutramine hydrochloride monohydrate

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.

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].

References:
[1]. Heal DJ, et al. Sibutramine: a novel anti-obesity drug. A review of the pharmacological evidence to differentiate it from d-amphetamine and d-fenfluramine. Int J Obes Relat Metab Disord. 1998 Aug;22 Suppl 1:S18-28; discussion S29. [2]. Kim SE, et al. Open channel block of A-type, kv4.3, and delayed rectifier K+ channels, KV1.3 and KV3.1, bySibutramine. J Pharmacol Exp Ther. 2007 May;321(2):753-62. [3]. Burke LK, et al. 5-HT obesity medication efficacy via POMC activation is maintained during aging. Endocrinology. 2014 Oct;155(10):3732-8. [4]. Turnbull AV, et al. Selective antagonism of the NPY Y5 receptor does not have a major effect on feeding in rats. Diabetes. 2002 Aug;51(8):2441-9.

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References on Sibutramine hydrochloride monohydrate

Development and validation of sensitive methods for determination of sibutramine hydrochloride monohydrate and direct enantiomeric separation on a protein-based chiral stationary phase.[Pubmed:18567303]

J AOAC Int. 2008 May-Jun;91(3):572-9.

Sibutramine hydrochloride monohydrate, chemically 1-(4-chlorophenyl)-N,N-dimethyl-alpha-(2-methylpropyl) hydrochloride monohydrate (SB.HCI.H20), was approved by the U.S. Food and Drug Administration for the treatment of obesity. The objective of this study was to develop, validate, and compare methods using UV-derivative spectrophotometry (UVDS) and reversed-phase high-performance liquid chromatography (HPLC) for the determination of SB.HCI.H20 in pharmaceutical drug products. The UVDS and HPLC methods were found to be rapid, precise, and accurate. Statistically, there was no significant difference between the proposed UVDS and HPLC methods. The enantiomeric separation of SB was obtained on an alpha-1-acid glycoprotein column. The R- and S-sibutramine were eluted in < 5 min with baseline separation of the chromatographic peaks (alpha = 1.9 and resolution = 1.9).

Description

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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