Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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O159936-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $64.90 | |
O159936-250mg | 250mg | In stock | $146.90 | |
O159936-1g | 1g | In stock | $526.90 | |
O159936-5g | 5g | In stock | $2,369.90 | |
O159936-25g | 25g | In stock | $10,661.90 | |
O159936-100g | 100g | In stock | $38,381.90 |
Selective, competitive lipase inhibitor
Synonyms | CCG-100851 | DTXCID40820067 | ORLISTAT [MART.] | Orlistat, United States Pharmacopeia (USP) Reference Standard | Q424163 | [(2S)-1-[(2R,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2R)-2-formamido-4-methylpentanoate | BDBM24567 | HSDB 7556 | L-Leucine, N- |
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Specifications & Purity | Moligand™, ≥97%(HPLC) |
Biochemical and Physiological Mechanisms | Orlistat, used in obesity research, is a pancreatic lipase inhibitor that acts locally in the gastrointestinal tract to inhibit lipase.Selective, competitive lipase inhibitor (IC 50 = 0.15 µM). Displays antiproliferative and antitumor activity. Active in |
Storage Temp | Store at -20°C,Argon charged |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Pancreatic lipase inhibitor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | Lipase Inhibitor, THL (Tetrahydrolipstatin), is a compound that has been shown to rapidly inactivate lipoprotein lipase (LPL). This agent has been found to bind both subunits of LPL, induce tetramerisation, and cause local conformational changes. The exception to lipase inhibition capacities of THL is phospholipase A2, which is not affected by THL. Mechanistic studies suggest that THL inhibits the thioesterase domain of fatty acid synthase (FAS) and as a result halts cell proliferation and causes cell apoptosis. More detailed experiments show that gradually THL affects the retinoblastoma protein pathway and leads to cell-cycle arrest at G1/S boundary. Lipase Inhibitor, THL is an inhibitor of pancreatic and gastric lipase, as well as carboxyl ester lipase (CEL) and diacylglycerol lipase-α (DAGLα). Lipase Inhibitor, THL also activates caspase-3. |
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IUPAC Name | [(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-2-formamido-4-methylpentanoate |
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INCHI | InChI=1S/C29H53NO5/c1-5-7-9-11-12-13-14-15-16-18-24(34-29(33)26(30-22-31)20-23(3)4)21-27-25(28(32)35-27)19-17-10-8-6-2/h22-27H,5-21H2,1-4H3,(H,30,31)/t24-,25-,26-,27-/m0/s1 |
InChi Key | AHLBNYSZXLDEJQ-FWEHEUNISA-N |
Canonical SMILES | CCCCCCCCCCCC(CC1C(C(=O)O1)CCCCCC)OC(=O)C(CC(C)C)NC=O |
Isomeric SMILES | CCCCCCCCCCC[C@@H](C[C@H]1[C@@H](C(=O)O1)CCCCCC)OC(=O)[C@H](CC(C)C)NC=O |
WGK Germany | 3 |
RTECS | OH3167600 |
PubChem CID | 3034010 |
Molecular Weight | 495.75 |
Reaxy-Rn | 3658031 |
CAS Registry No. | 96829-58-2 |
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DrugBank Ligand | DB01083 |
Wikipedia | Tetrahydrolipstatin |
PubChem CID | 3034010 |
ChEMBL Ligand | CHEMBL175247 |
PEP | orlistat |
DrugCentral Ligand | 1996 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
I2205038 | Certificate of Analysis | Jul 15, 2022 | O159936 |
I2205039 | Certificate of Analysis | Jul 15, 2022 | O159936 |
I2205040 | Certificate of Analysis | Jul 15, 2022 | O159936 |
I2205041 | Certificate of Analysis | Jul 15, 2022 | O159936 |
I2205042 | Certificate of Analysis | Jul 15, 2022 | O159936 |
G2106197 | Certificate of Analysis | Mar 11, 2021 | O159936 |
Solubility | Soluble in DMSO (19 mg/mL), ethanol (20 mg/mL), and DMF (20 mg/mL). |
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Sensitivity | heat sensitive |
Specific Rotation[α] | -35° (C=1,CHCl3) |
Melt Point(°C) | 43-47°C |
Pictogram(s) | GHS09 |
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Hazard Statements | H411:Toxic to aquatic life with long lasting effects H412:Harmful to aquatic life with long lasting effects |
Precautionary Statements | P273:Avoid release to the environment. P501:Dispose of contents/container to ... P391:Collect spillage. |
WGK Germany | 3 |
RTECS | OH3167600 |
Reaxy-Rn | 3658031 |
Merck Index | 6869 |
1. Wenjing Jiang, Qun Huang, Xiangxing Meng, Rizwan-ur Rehman, Kun Qian, Xu Yang, Xiaozhi Liu, Jingnan Chen, Ye Zhang, Jing Li, Jilite Wang, Qingbin Guo, Suwen Liu, Hao Wang. (2023) Ursolic Acid Inhibited Cholesterol Esterase and Pancreatic Lipase Activities and Decreased Micellar Cholesterol Solubility In Vitro. JOURNAL OF FOOD BIOCHEMISTRY, 2023 (6637700). [PMID:] |
2. Sihua Quan, Mengyi Wen, Ping Xu, Chu Chu, Hui Zhang, Kai Yang, Shengqiang Tong. (2023) Efficient screening of pancreatic lipase inhibitors from Rheum palmatum by affinity ultrafiltration–high-performance liquid chromatography combined with high-resolution inhibition profiling. PHYTOCHEMICAL ANALYSIS, [PMID:38053479] |
3. Mei Dong, Cheng Zhao, Yongfang Huang, Ke Zheng, Guanhu Bao, Fenglin Hu, Fan Peng, Mingjun Chen, Zengzhi Li, Ruili Lu. (2023) Metabolites analysis and new bioactive compounds from the medicine food homology product of Cordyceps chanhua on artificial media. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, (115749). [PMID:37801798] |
4. Dan Yang, Xin-yu-yao Ding, Hai-Xia Xu, Yu-Xian Guo, Qing-Feng Zhang. (2023) Chemical profile of Roselle extract and its inhibitory activities on three digestive enzymes in vitro and in vivo. INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES, 253 (2): (126902). [PMID:37714233] |
5. Wen Li, Xinyue Cui, Zilin Chen. (2023) The screening of lipase inhibitors based on the metal-organic framework Zeolitic Imidazolate Framework-8-immobilized enzyme microreactor. JOURNAL OF CHROMATOGRAPHY A, 1706 (464257). [PMID:37531848] |
6. Suwen Liu, Wenhong Jiang, Chang Liu, Shuo Guo, Hao Wang, Xuedong Chang. (2023) Chinese chestnut shell polyphenol extract regulates the JAK2/STAT3 pathway to alleviate high-fat diet-induced, leptin-resistant obesity in mice. Food & Function, 14 (10): (4807-4823). [PMID:37128963] |
7. Xiang Li, Rongxia Li, Xueyu Wang, Xinying Zhang, Zhiyi Xiao, Haibo Wang, Wenhui Sun, Hao Yang, Peng Yu, Qing Hu, Qinghui Guo, Hua Sun. (2023) Effects and mechanism of action of Chrysanthemum morifolium (Jinsi Huangju) on hyperlipidemia and non-alcoholic fatty liver disease. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 255 (115391). [PMID:37099836] |
8. Xinyue Zhang, Dan Li, Kexin Wang, Jiao Xie, Yaojie Liu, Tianxin Wang, Suwen Liu, Qun Huang, Qingbin Guo, Hao Wang. (2023) Hyperoside inhibits pancreatic lipase activity in vitro and reduces fat accumulation in vivo. Food & Function, 14 (10): (4763-4776). [PMID:37128768] |
9. Jinpeng Liu, Mashooq Khan, Yong Wei, Anna Liu, Tao Wang, Qiongzheng Hu, Li Yu. (2023) High-throughput screening of lipase inhibitors as anti-obesity drugs on liquid crystal-infused porous surfaces. SENSORS AND ACTUATORS B-CHEMICAL, 387 (133837). [PMID:] |
10. Tao Gao, Shuang Liu, Huang-yang Luo, Ren Wu, Rui Yan, Ling-zhi He, Qing-yu Nie, Hua-li Tang, Guiju Sun. (2023) Purification, structural identification, antioxidant activity, and inhibitory effects on digestive enzymes of α-glucan from Chuanminshen violaceum. Journal of Functional Foods, 104 (105536). [PMID:] |
11. Olaoye Solomon Balogun, Anthonia Olufunke Oluduro, Zhiqiang Liu. (2023) Chemical composition and in vitro biological studies of volatile oils from Nigerian bee propolis. JOURNAL OF APICULTURAL RESEARCH, [PMID:] |
12. Liyuan Ran, Jinhui Yu, Rui Ma, Qing Yao, Mingjie Wang, Yuping Bi, Zichao Yu, Yingjie Wu. (2022) Microalgae oil from Schizochytrium sp. alleviates obesity and modulates gut microbiota in high-fat diet-fed mice. Food & Function, 13 (24): (12799-12813). [PMID:36421064] |
13. Lan Wei, Jingjing Li, Yun Yang, Mei Zhu, Mengke Zhao, Jianhua Yang, Zhiyun Yang, Luyao Zhou, Shenyue Zhou, Jiajia Gong, Xiaogang Jiang, Jiangyun Liu, Yali Li, Jian Zhang. (2022) Characterization and potential bioactivity of polyphenols of Rosa rugosa. Food Bioscience, 50 (102108). [PMID:] |
14. Fu-Qin He, Guang-Zhen Wan, Juan Chen. (2022) Pancreatic lipase and alpha-glucosidase inhibitors screening from Schisandra chinensis based on spectrum-effect relationship and ultra-high-performance liquid chromatography-tandem mass spectrometry. JOURNAL OF SEPARATION SCIENCE, 45 (23): (4198-4208). [PMID:36189874] |
15. Qing Zhang, Yue Zhou, Xingyu Feng, Yuan Gao, Chengzhi Huang, Xueqing Yao. (2022) Low-dose orlistat promotes the therapeutic effect of oxaliplatin in colorectal cancer. BIOMEDICINE & PHARMACOTHERAPY, 153 (113426). [PMID:36017794] |
1. Wenjing Jiang, Qun Huang, Xiangxing Meng, Rizwan-ur Rehman, Kun Qian, Xu Yang, Xiaozhi Liu, Jingnan Chen, Ye Zhang, Jing Li, Jilite Wang, Qingbin Guo, Suwen Liu, Hao Wang. (2023) Ursolic Acid Inhibited Cholesterol Esterase and Pancreatic Lipase Activities and Decreased Micellar Cholesterol Solubility In Vitro. JOURNAL OF FOOD BIOCHEMISTRY, 2023 (6637700). [PMID:] |
2. Sihua Quan, Mengyi Wen, Ping Xu, Chu Chu, Hui Zhang, Kai Yang, Shengqiang Tong. (2023) Efficient screening of pancreatic lipase inhibitors from Rheum palmatum by affinity ultrafiltration–high-performance liquid chromatography combined with high-resolution inhibition profiling. PHYTOCHEMICAL ANALYSIS, [PMID:38053479] |
3. Mei Dong, Cheng Zhao, Yongfang Huang, Ke Zheng, Guanhu Bao, Fenglin Hu, Fan Peng, Mingjun Chen, Zengzhi Li, Ruili Lu. (2023) Metabolites analysis and new bioactive compounds from the medicine food homology product of Cordyceps chanhua on artificial media. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, (115749). [PMID:37801798] |
4. Dan Yang, Xin-yu-yao Ding, Hai-Xia Xu, Yu-Xian Guo, Qing-Feng Zhang. (2023) Chemical profile of Roselle extract and its inhibitory activities on three digestive enzymes in vitro and in vivo. INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES, 253 (2): (126902). [PMID:37714233] |
5. Wen Li, Xinyue Cui, Zilin Chen. (2023) The screening of lipase inhibitors based on the metal-organic framework Zeolitic Imidazolate Framework-8-immobilized enzyme microreactor. JOURNAL OF CHROMATOGRAPHY A, 1706 (464257). [PMID:37531848] |
6. Suwen Liu, Wenhong Jiang, Chang Liu, Shuo Guo, Hao Wang, Xuedong Chang. (2023) Chinese chestnut shell polyphenol extract regulates the JAK2/STAT3 pathway to alleviate high-fat diet-induced, leptin-resistant obesity in mice. Food & Function, 14 (10): (4807-4823). [PMID:37128963] |
7. Xiang Li, Rongxia Li, Xueyu Wang, Xinying Zhang, Zhiyi Xiao, Haibo Wang, Wenhui Sun, Hao Yang, Peng Yu, Qing Hu, Qinghui Guo, Hua Sun. (2023) Effects and mechanism of action of Chrysanthemum morifolium (Jinsi Huangju) on hyperlipidemia and non-alcoholic fatty liver disease. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 255 (115391). [PMID:37099836] |
8. Xinyue Zhang, Dan Li, Kexin Wang, Jiao Xie, Yaojie Liu, Tianxin Wang, Suwen Liu, Qun Huang, Qingbin Guo, Hao Wang. (2023) Hyperoside inhibits pancreatic lipase activity in vitro and reduces fat accumulation in vivo. Food & Function, 14 (10): (4763-4776). [PMID:37128768] |
9. Jinpeng Liu, Mashooq Khan, Yong Wei, Anna Liu, Tao Wang, Qiongzheng Hu, Li Yu. (2023) High-throughput screening of lipase inhibitors as anti-obesity drugs on liquid crystal-infused porous surfaces. SENSORS AND ACTUATORS B-CHEMICAL, 387 (133837). [PMID:] |
10. Tao Gao, Shuang Liu, Huang-yang Luo, Ren Wu, Rui Yan, Ling-zhi He, Qing-yu Nie, Hua-li Tang, Guiju Sun. (2023) Purification, structural identification, antioxidant activity, and inhibitory effects on digestive enzymes of α-glucan from Chuanminshen violaceum. Journal of Functional Foods, 104 (105536). [PMID:] |
11. Olaoye Solomon Balogun, Anthonia Olufunke Oluduro, Zhiqiang Liu. (2023) Chemical composition and in vitro biological studies of volatile oils from Nigerian bee propolis. JOURNAL OF APICULTURAL RESEARCH, [PMID:] |
12. Liyuan Ran, Jinhui Yu, Rui Ma, Qing Yao, Mingjie Wang, Yuping Bi, Zichao Yu, Yingjie Wu. (2022) Microalgae oil from Schizochytrium sp. alleviates obesity and modulates gut microbiota in high-fat diet-fed mice. Food & Function, 13 (24): (12799-12813). [PMID:36421064] |
13. Lan Wei, Jingjing Li, Yun Yang, Mei Zhu, Mengke Zhao, Jianhua Yang, Zhiyun Yang, Luyao Zhou, Shenyue Zhou, Jiajia Gong, Xiaogang Jiang, Jiangyun Liu, Yali Li, Jian Zhang. (2022) Characterization and potential bioactivity of polyphenols of Rosa rugosa. Food Bioscience, 50 (102108). [PMID:] |
14. Fu-Qin He, Guang-Zhen Wan, Juan Chen. (2022) Pancreatic lipase and alpha-glucosidase inhibitors screening from Schisandra chinensis based on spectrum-effect relationship and ultra-high-performance liquid chromatography-tandem mass spectrometry. JOURNAL OF SEPARATION SCIENCE, 45 (23): (4198-4208). [PMID:36189874] |
15. Qing Zhang, Yue Zhou, Xingyu Feng, Yuan Gao, Chengzhi Huang, Xueqing Yao. (2022) Low-dose orlistat promotes the therapeutic effect of oxaliplatin in colorectal cancer. BIOMEDICINE & PHARMACOTHERAPY, 153 (113426). [PMID:36017794] |