Orlistat
(Synonyms: 奥利司他; Tetrahydrolipstatin; Ro-18-0647) 目录号 : GC17318
奥利司他是胰脏和胃中脂肪酶的不可逆抑制剂，是治疗肥胖症的药物。
Cas No.:96829-58-2
Sample solution is provided at 25 µL, 10mM.
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Orlistat is an irreversible inhibitor of lipases in the pancreas and stomach. It is a drug for the treatment of obesity. It suppresses the action of gastrointestinal lipases, thereby impairing the metabolism of lipids in the gastrointestinal lumen, which can prevent the absorption of 30% of the lipids in dietary fat[1,2]. Orlistat is very hydrophobic and binds covalently to the active serine residues of pancreatic lipase. Orlistat passes through cell membranes sufficiently and exerts intracellular effects[3].
Orlistat(0-25µM;32h) induced a pronounced antiproliferative effect in the PC-3 cell line[4]. Orlistat inhibits Jurkat cell growth and induces a perturbation of cell cycle along with a decline of FASN activity and protein levels[6]. Orlistat-mediated(0-50µM) FASN inhibition could overcome sorafenib resistance and enhance cell killing in HCC by changing cell metabolism[7].
Orlistat(10 mg/kg/day, p.o.) alleviates colon cancer promotion in WD-driven CAC mice by suppressing inflammation, especially by inhibiting STAT3 and NF-κB activation[5].Orlistat(240 mg/kg/day;3 weeks; i.p.) prevented the growth of PC-3 tumors. Animals exhibited no outward signs of toxicity, experienced no loss of weight, nor were there any effects of Orlistat on hematocrit or WBC levels[4].
References:
[1]. Chandra P, Enespa, et,al. Microbial lipases and their industrial applications: a comprehensive review. Microb Cell Fact. 2020 Aug 26;19(1):169. doi: 10.1186/s12934-020-01428-8. PMID: 32847584; PMCID: PMC7449042.
[2]. Bansal AB, Al Khalili Y. Orlistat. 2022 Nov 2. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2022 Jan-. PMID: 31194359.
[3]. Padwal, et,al. Drug treatments for obesity: Orlistat, sibutramine, and rimonabant. Lancet 2007, 369, 71-77.
[4]. Kridel SJ, Axelrod F, et,al. Orlistat is a novel inhibitor of fatty acid synthase with antitumor activity. Cancer Res. 2004 Mar 15;64(6):2070-5. doi: 10.1158/0008-5472.can-03-3645. PMID: 15026345.
[5]. Jin BR, Kim HJ, et,al. Anti-Obesity Drug Orlistat Alleviates Western-Diet-Driven Colitis-Associated Colon Cancer via Inhibition of STAT3 and NF-κB-Mediated Signaling. Cells. 2021 Aug 11;10(8):2060. doi: 10.3390/cells10082060. PMID: 34440829; PMCID: PMC8394553.
[6]. Cioccoloni G, Aquino A, et,al. Fatty acid synthase inhibitor orlistat impairs cell growth and down-regulates PD-L1 expression of a human T-cell leukemia line. J Chemother. 2020 Feb;32(1):30-40. doi: 10.1080/1120009X.2019.1694761. Epub 2019 Nov 28. PMID: 31775585.
[7]. Shueng PW, Chan HW, et,al. Orlistat Resensitizes Sorafenib-Resistance in Hepatocellular Carcinoma Cells through Modulating Metabolism. Int J Mol Sci. 2022 Jun 10;23(12):6501. doi: 10.3390/ijms23126501. PMID: 35742944; PMCID: PMC9223797.
奥利司他是胰脏和胃中脂肪酶的不可逆抑制剂,是治疗肥胖症的药物。它抑制胃肠道内脂肪酶的作用,从而影响胃肠道脂质的代谢,可以防止膳食脂肪的30%被吸收[1,2]。奥利司他非常疏水,与胰脏脂肪酶的活性丝氨酸残基发生共价结合。奥利司他能够充分通过细胞膜并发挥细胞内作用[3]。
奥利司他(0-25 µM; 32 h) 在 PC-3 细胞系中产生明显的抗增殖效应[4]。奥利司他抑制 Jurkat 细胞的生长并引起细胞周期紊乱,伴随着 FASN 活性和蛋白水平的下降[6]。奥利司他介导的(0-50 µM) FASN 抑制可以克服 HCC 对索拉非尼的耐药性,并通过改变细胞代谢增强细胞杀伤[7]。
奥利司他(10 mg/kg/天,p.o.) 可以通过抑制炎症,特别是通过抑制 STAT3 和 NF-κB 活化,减轻 WD 驱动的 CAC 小鼠结肠癌促进作用[5]。奥利司他(240 mg/kg/天,3 周,i.p.) 可以预防 PC-3 肿瘤的生长。动物没有外观上的毒性表现,没有体重减轻,奥利司他对红细胞压积或白细胞计数没有影响[4]。
| Cell experiment [1]: | |
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Cell lines |
prostate cancer cells(PC3) |
|
Preparation Method |
The effect of Orlistat on proliferation of prostate cancer cells was measured by the incorporation of bromodeoxyuridine (BrdUrd). PC-3 was seeded as subconfluent monolayers into microtiter plates. Cells were exposed to Orlistat for 32 h, then a BrdUrd labeling solution was added to the wells. |
|
Reaction Conditions |
0-25µM;32h |
|
Applications |
Orlistat induced a pronounced antiproliferative effect in the PC-3 cell line. |
| Animal experiment [2]: | |
|
Animal models |
Male athymic nude mice 4-5 weeks of age |
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Preparation Method |
PC-3 cells were injected into the flank of nude mice. Tumors were allowed to grow until they reached a size of 100 mm3, at which time administration of Orlistat or vehicle was initiated in separate sets of 8 mice. Orlistat was administered at 240 mg/kg/day for a period of 3 weeks. |
|
Dosage form |
240 mg/kg/day;3 weeks; i.p. |
|
Applications |
Orlistat prevented the growth of PC-3 tumors. |
|
References: [1]. Kridel SJ, Axelrod F, et,al. Orlistat is a novel inhibitor of fatty acid synthase with antitumor activity. Cancer Res. 2004 Mar 15;64(6):2070-5. doi: 10.1158/0008-5472.can-03-3645. PMID: 15026345. | |
| Cas No. | 96829-58-2 | SDF | |
| 别名 | 奥利司他; Tetrahydrolipstatin; Ro-18-0647 | ||
| 化学名 | [(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-2-formamido-4-methylpentanoate | ||
| Canonical SMILES | CCCCCCCCCCCC(CC1C(C(=O)O1)CCCCCC)OC(=O)C(CC(C)C)NC=O | ||
| 分子式 | C29H53NO5 | 分子量 | 495.73 |
| 溶解度 | ≥ 17.4mg/mL in DMSO | 储存条件 | Store at 2-8°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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0172 mL | 10.0861 mL | 20.1723 mL |
| 5 mM | 0.4034 mL | 2.0172 mL | 4.0345 mL |
| 10 mM | 0.2017 mL | 1.0086 mL | 2.0172 mL |
| 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet