Colestyramine (Cholestyramine resin)
(Synonyms: 考来烯胺; Cholestyramine resin; Colestyramine) 目录号 : GC32441
考来烯胺（Cholestyramine resin）（考来烯胺）是一种胆汁酸结合树脂，可抑制肠道对胆汁酸的吸收，从而导致胆固醇合成胆汁酸的增加。
Cas No.:11041-12-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Mice are purchased at 7 weeks of age and allowed to acclimate for one week. At 8-weeks of age the mice are given either a control or a 2% Cholestyramine-supplementing diet for 4 weeks (n=18 per group). Body weight for each mouse is recorded weekly. After 4 weeks, the mice in each group are randomly assigned to one of two treatment groups and orally gavaged with either vehicle (water) or GSPE (250 mg/kg) and terminated 14 hours later (n=9 per experimental group). The four treatment groups are as follows: 1. CON: Control diet for 4 weeks following by oral gavage with vehicle (water) for 14 hrs; 2. GSPE: Control diet for 4 weeks following by oral gavage with 250 mg/kg GSPE for 14 hrs; 3.Cholestyramine 2% Cholestyramine-supplementing diet for 4 weeks following by oral gavage with vehicle for 14 hrs; and 4. Cholestyramine+GSPE: 2% cholestyramine-supplementing diet for 4 weeks following by oral gavage with 250 mg/kg GSPE for 14 hrs. Blood is collected from the orbital plexus under isoflurane anesthesia, and intestines and livers are snap-frozen in liquid nitrogen and stored at -80°C until use. At the start of the 14 hr experiment mice are placed into clean cages, and feces are manually collected at the end of the study[2]. |
References: [1]. Maugeais C, et al. rHDL administration increases reverse cholesterol transport in mice, but is not additive on top of ezetimibe or cholestyramine treatment. Atherosclerosis. 2013 Jul;229(1):94-101. | |
Colestyramine (Cholestyramine) is a bile acid binding resin and can inhibit intestinal bile acid absorption which results in the increasing bile acid synthesis from cholesterol.
Colestyramine (Cholestyramine) is a bile acid binding resin and can inhibit intestinal bile acid absorption which results in the increasing bile acid synthesis from cholesterol[1]. Results reveal that GSPE treatment alone, and co-administration with Colestyramine (CHY), regulate BA, cholesterol and TG metabolism differently compare to Colestyramine (CHY) administration alone. Notably, GSPE decreases intestinal apical sodium-dependent bile acid transporter (Asbt) gene expression, while Colestyramine (CHY) significantly induces expression. Administration with GSPE or Colestyramine (CHY) robustly induces hepatic BA biosynthetic gene expression, especially cholesterol 7α-hydroxylase (Cyp7a1), compare to control, while co-administration further enhances expression. Treatment with Colestyramine (CHY) induces both intestinal and hepatic cholesterologenic gene expression, while co-administration with GSPE attenuates the Colestyramine (CHY)-inducing increase in the liver but not in the intestine. Colestyramine (CHY) also induces hepatic lipogenic gene expression, which is attenuated by co-administration with GSPE[2].
[1]. Maugeais C, et al. rHDL administration increases reverse cholesterol transport in mice, but is not additive on top of ezetimibe or cholestyramine treatment. Atherosclerosis. 2013 Jul;229(1):94-101. [2]. Rebecca M. Heidker, et al. Grape Seed Procyanidins and Cholestyramine Differentially Alter Bile Acid and Cholesterol Homeostatic Gene Expression in Mouse Intestine and Liver. PLoS One. 2016; 11(4): e0154305.
| Cas No. | 11041-12-6 | SDF | |
| 别名 | 考来烯胺; Cholestyramine resin; Colestyramine | ||
| Canonical SMILES | C[N+](C)(C)CC1=CC=C(C(CC(C)C2=CC=CC=C2)CC)C=C1.CC(CC)C.[Cl-].[n] | ||
| 分子式 | 分子量 | ||
| 溶解度 | DMSO : < 1 mg/mL (insoluble or slightly soluble);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Colestyramine slows gastric emptying of liquids and reduces appetite in healthy subjects
Neurogastroenterol Motil 2012 Dec;24(12):1095-101.PMID:22863058DOI:10.1111/j.1365-2982.2012.01988.x.
Background: There is evidence to suggest that the particulate resin Colestyramine, a bile acid sequestrant formerly used as a cholesterol-lowering agent, enhances secretion of the gut hormone cholecystokinin (CCK). Established physiological actions of CCK include inhibition of gastric emptying and induction of satiation. This study evaluated the hypothesis that Colestyramine, which is luminally retained, would slow gastric emptying of liquids and suppress appetite in humans. Methods: Nine healthy volunteers consumed 500 mL liquid test meals containing 4 g Colestyramine, 12 g Colestyramine, or control (water alone), on three occasions, in a randomized order. The effect of Colestyramine on gastric emptying was determined non-invasively using the (13) C-acetate breath test, and appetite and other gut-centered sensations were rated using visual analog scale questionnaires. Key results: Colestyramine dose dependently slowed liquid gastric emptying compared with control (water) (4 g vs control, 鈭?0% reduction, P < 0.05; 12 g vs control, 鈭?5% reduction, P < 0.01). Colestyramine also significantly reduced hunger (4 g vs control, 鈭?0% reduction, P < 0.01), and the amount of food participants felt able to eat (12 g vs control, 鈭?2% reduction, P < 0.001), but increased bloating (both doses, P < 0.05), with no effect on ratings of nausea. Conclusions & inferences: This study provides the first evidence that Colestyramine significantly slows liquid gastric emptying and reduces appetite in healthy humans. Colestyramine therefore presents an attractive gut-brain signaling research tool in that it is not absorbed and thus lacks potentially confounding postabsorptive effects. Furthermore, with clear effects on gastric emptying and appetite, Colestyramine now merits consideration as a trial therapeutic strategy for appetite suppression and weight loss.
Postcholecystectomy diarrhea
JAMA 1979 Feb 23;241(8):823-4.PMID:762849doi
Diarrhea developed in three patients following cholecystectomy. Fecal bile-acid excretion was elevated in the two patients for whom it was measured. All three patients' diarrhea resolved with Cholestyramine resin therapy. This experience suggests that gallbladder removal may lead to a bile-acid-mediated diarrhea in some patients, and that this condition appears to respond to cholestyramine therapy.
Cholestyramine as a promising, strong anion exchange resin for direct capture of genetic biomarkers from raw pancreatic fluids
Biotechnol Bioeng 2017 Apr;114(4):934-938.PMID:27800600DOI:10.1002/bit.26207.
The ability to capture cell-free DNA from the gastrointestinal tract, in a minimally invasive manner, could enhance our ability to diagnose gastrointestinal disease, or gain a better understanding of the spatial mapping of the intestinal microbiota. We, therefore, sought to identify a class of capture agents that could directly and efficiently sequester genetic material from intestinal fluids. As a particular case study, we examined the ability to capture DNA from pancreatic secretions, for potential application in enabling the sequestration of early, genetic biomarkers of pancreatic disease. We hypothesized that the cholestyramine series of strong cation exchange resins, which are FDA approved for the treatment of high cholesterol, may be capable of capturing DNA from pancreatic secretions. We identified a particular Cholestyramine resin, DOWEX 1 脳 2 100-200 mesh, which is able to efficiently capture and purify DNA from pancreatic fluid. Using only 200 渭L of pancreatic secretions, we are able to recover 247 卤 182 ng of amplifiable human DNA, giving an estimated pancreatic fluid DNA content of 1.23 卤 0.91 ng/渭L. To our knowledge, this is the first demonstration of a material that can effectively capture and purify DNA directly from untreated pancreatic fluids. Thus, our approach could hold high utility for the in vivo capture of DNA and disease biomarkers if incorporated into an appropriate sampling device. Biotechnol. Bioeng. 2017;114: 934-938. 漏 2016 Wiley Periodicals, Inc.
In vitro characterization of sodium glycocholate binding to Cholestyramine resin
J Pharm Sci 1995 Jan;84(1):55-61.PMID:7714745DOI:10.1002/jps.2600840114.
Cholestyramine resin in a bile acid sequestrant which binds with bile salts in the intestinal lumen to increase the fecal excretion of bile salts and, thus, lower blood serum cholesterol. In order to gain a better understanding of the low in vivo potency of cholestyramine, in vitro equilibrium binding studies, water sorption studies, and resin capacity measurements were performed using cholestyramine and the bile salt sodium glycocholate. Equilibrium binding and water sorption studies entailed equilibrating cholestyramine (1.0-20 mg/mL) with solutions which varied in glycocholate anion concentration (0.20-16.5 mM) and chloride anion concentration (15-150 mM). The resin's practical specific capacity for glycocholate was lower than the practical specific capacity for chloride. This difference suggests that the rigid, bulky bile salt was pore excluded from 10% of the resin's ionogentic sites. A fundamental parameter called the capacity-corrected molar selectivity coefficient, KGC-Cl-, was postulated to describe the underlying binding phenomena and was determined by measuring the free glycocholate and chloride anion concentrations; KGC-Cl- ranged from 9.8 (+/- 0.7) to 18.6 (+/- 0.2) and depended on the square of the free chloride concentration. The capacity-corrected molar selectivity coefficient was larger than the molar selectivity coefficient due to pore exclusion of glycocholate. A more simple method to calculate the capacity-corrected molar selectivity coefficient which required less data gave similar values to the more rigorous method (r2 = 0.955).
[Acceleration of amiodarone elimination by cholestyramine]
Dtsch Med Wochenschr 1986 Aug 15;111(33):1241-4.PMID:3743429DOI:10.1055/s-2008-1068613.
In eleven patients serum levels of amiodarone and its desethyl metabolite were determined after a single dose of 400 mg amiodarone given with and without subsequent administration of Colestyramine. In addition, the elimination half-life was measured in three patients after discontinuation of long-term amiodarone therapy. Mean serum levels of amiodarone at 7 1/2 hours after dosing (n = 11) were 0.42 +/- 0.11 micrograms/ml without Colestyramine and 0.21 +/- 0.14 micrograms/ml with Colestyramine (P less than 0.01). Elimination half-life after discontinuing long-term amiodarone therapy (n = 3) was 23 1/2, 29 and 32 days, respectively (half-life in eight controls: 35-58 days). The results indicate that Colestyramine significantly reduces the enterohepatic circulation of amiodarone. Therefore, Colestyramine should be capable of accelerating the regression of dose-dependent side-effects of amiodarone by enhancing its elimination.