Sibutramine hydrochloride monohydrateCAS# 125494-59-9 |
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| 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. |
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| 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. |
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| 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. | ||
Sibutramine hydrochloride monohydrate Dilution Calculator
Sibutramine hydrochloride monohydrate Molarity Calculator
| 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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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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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).
