Lipase Inhibitor, THL CAS: 96829-58-2
MF: C29H53NO5
MW: 495.7
An inhibitor of pancreatic and gastric lipase, and an activator of caspase-3..

Lipase Inhibitor, THL (CAS 96829-58-2)

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別名: (-)-Tetrahydrolipstatin; Orlistat
アプリケーション: Lipase Inhibitor, THL is an inhibitor of pancreatic and gastric lipase, and an activator of caspase-3.
CAS 番号: 96829-58-2
Purity: ≥98%
Molecular Weight: 495.7
Molecular Formula: C29H53NO5
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* Refer to Certificate of Analysis for lot specific data (including water content).

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.


参考文献

1. Lookene, A., et al. 1994. Eur. J. Biochem. 222: 395-403. PMID: 8020477
2. Sternby, B., et al. 2002. Clin Nutr. 21: 395-402. PMID: 12381337
3. Kridel, S.J., et al. 2004. Cancer Res. 64: 2070-2075. PMID: 15026345
4. Knowles, L.M., et al. 2004. J. Biol. Chem. 279: 30540-30545. PMID: 15138278

Physical State :
Solid
Solubility :
Soluble in DMSO (19 mg/mL), ethanol (20 mg/mL), and DMF (20 mg/mL).
保存方法 :
Store at -20° C
Melting Point :
<50° C
Boiling Point :
615.88° C at 760 mmHg (Predicted)
Refractive Index :
n20D 1.47
Optical Activity :
α20/D -35°, c = 1 in chloroform; α20/D°
IC50 :
LDL-associated phospholipase A2: IC50 = 50 nM (human); Sn1-specific diacylglycerol lipase beta: IC50 = 60 nM (human); Cannabinoid CB1 receptor: IC50 = 100 nM (rat); Pancreatic triacylglycerol lipase: IC50 = 600 nM (Sus scrofa); Protein BAT5: IC50 = 30 nM (human); Monoacylglycerol lipase ABHD12: IC50 = 80 nM (human)
Ki Data :
Cannabinoid CB1 receptor: Ki= 2500 nM (human); Cannabinoid CB2 receptor: Ki= >10000 nM (human)
試験・研究用以外には使用しないでください。 臨床及び体外診断には使用できません。
WGK Germany :
3
RTECS :
OH3167600
PubChem CID :
Merck Index :
14: 6869
MDL Number :
MFCD05662360
Beilstein Registry :
3658031
SMILES :
CCCCCCCCCCC[[email protected]@H](C[[email protected]]1[[email protected]@H](C(=O)O1)CCCCCC)OC(=O)[[email protected]](CC(C)C)NC=O

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Lipase Inhibitor, THL (CAS 96829-58-2)  参考文献

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引用 1 to 3 of 3 合計

PMID: # 1544468  Lüthi-Peng, Q. et al. 1992. FEBS Lett. 299: 111-115.

PMID: # 29208697  J. Lipid Res. 59: 283-297.

PMID: # 29281779  Mol. Cells. 935-944.

引用 1 to 3 of 3 合計
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