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Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastric lipases. Orlistat is also an inhibitor of fatty acid synthase (FASN). Orlistat is a compound that promotes loss of weight by preventing the digestion and absorption of fat in food. It is intended for use in conjunction with a physician-supervised reduced-calorie diet. Orlistat is the saturated derivative of lipstatin, a potent natural inhibitor of pancreatic lipases isolated from the bacterium Streptomyces toxytricini. In vitro experiments demonstrate that orlistat has an IC50 of 122 ng/ml for PL from human duodenal juice, but an IC50 of about 300 ng/ml for LPL.
| Molecular Weight | 495.73 |
| Formula | C29H53NO5 |
| CAS Number | 96829-58-2 |
| Solubility (25°C) | DMSO 89 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related FAS Products |
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| IPI-9119
IPI-9119 is an orally active, selective and irreversible Fatty Acid Synthase (FASN) inhibitor, with an IC50 of 0.3 nM. |
| Anti-Mouse Fas Ligand Antibody
Anti-Mouse Fas Ligand Antibody is an anti-mouse Fas Ligand IgG antibody inhibitor derived from host Armenian Hamster. |
| Eicosapentaenoic acid ethyl ester
Eicosapentaenoic acid ethyl ester (AMR101, EPA ethyl ester, Ethyl eicosapentaenoate) is an omega-3 fatty acid agent that significantly reduces the triglyceride (TG) levels and improves other lipid parameters without significantly increasing the low-density lipoprotein (LDL) cholesterol levels. |
| FT113
FT113 is a potent inhibitor of fatty acid synthase(FASN) with ic50 of 213 nM. |
| PF429242 dihydrochloride
PF429242 dihydrochloride is a reversible and competitive SREBP site 1 protease (S1P) inhibitor with an IC50 of 175 nM. |
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