| Size | Price | Stock | Qty |
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| 500mg |
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Purity: ≥98%
Cetilistat (previously known as ATL-962) is a novel inhibitor of pancreatic and gastrointestinal lipases. It has the potential to treat obesity in both diabetic and non-diabetic patients. It is a highly lipophilic benzoxazinone analog with good PK, safety and tolerability profiles in vivo. Cetilistat acts by inhibiting pancreatic lipase which is an enzyme that breaks down triglycerides in the intestine. Triglycerides from the diet can not be hydrolyzed into the absorbable free fatty acids without this lipase enzyme and are excreted undigested.
| ln Vitro |
Rat pancreatic lipase activity is inhibited by cetilistat, with an IC50 of 54.8 nM. Moreover, cetilistat is 9.2 times more powerful than rat pancreatic lipase at inhibiting human pancreatic lipase activity, with an IC50 of 5.95 nM[1].
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| ln Vivo |
In male SD rats, cetilistat (3, 10, 30, or 100 mg/kg) inhibits pancreatic lipase activity, reducing intestinal fat absorption[1]. By decreasing intestinal fat absorption, cetilistat (4.9, 14.9, or 50.7 mg/kg; mixed into powdered high-fat food; thrice a day; for three weeks) has anti-obesity and antihyperlipidemic effects on DIO F344 rats[1].
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| Animal Protocol |
Animal/Disease Models: Fifty male SD rats (eight weeks of age)[1]
Doses: 3, 10 , 30, or 100 mg/kg Route of Administration: Orally administered; prepared in 0.5 % methylcellulose (MC) suspension Experimental Results: Dose-dependently decreased AUC 0-6 h of plasma triglyceride induced by oral loading of Intrafat 20%. The effect was statistically significant at 3 mg/kg, reaching 45% reduction, while an almost 90 % reduction was achieved at 100 mg/kg. Animal/Disease Models: Male diet-induced obesity (DIO) F344 rats (five weeks of age)[1] Doses: 4.9 , 14.9, or 50.7 mg/kg Route of Administration: Administered as food admixture in a high-fat diet; one time/day; for three weeks Experimental Results: Dramatically and dose-dependently decreased body weight gain compared with control. |
| References | |
| Additional Infomation |
Cetilistat is a benzoxazine.
Cetilistat is a novel inhibitor of pancreatic lipase being developed by Alizyme for the treatment of obesity and associated co-morbidities, including type 2 diabetes. Drug Indication Investigated for use/treatment in obesity. Mechanism of Action Cetilistat is a gastrointestinal lipase inhibitor that blocks fat digestion and absorption, leading to reduced energy intake, and thus weight loss. It is distinct from most other anti-obesity agents as it does not act on the brain to reduce appetite, but acts peripherally. The compound remains in the gastrointestinal tract with no significant absorption into the body. |
| Molecular Formula |
C25H39NO3
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|---|---|---|
| Molecular Weight |
401.58
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| Exact Mass |
401.292
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| CAS # |
282526-98-1
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| Related CAS # |
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| PubChem CID |
9952916
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| Appearance |
White to off-white solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
509.7±43.0 °C at 760 mmHg
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| Melting Point |
74°C
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| Flash Point |
158.9±22.6 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.521
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| LogP |
9.93
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
29
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| Complexity |
477
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MVCQKIKWYUURMU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H39NO3/c1-3-4-5-6-7-8-9-10-11-12-13-14-15-16-19-28-25-26-23-18-17-21(2)20-22(23)24(27)29-25/h17-18,20H,3-16,19H2,1-2H3
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| Chemical Name |
2-hexadecoxy-6-methyl-3,1-benzoxazin-4-one
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4902 mL | 12.4508 mL | 24.9016 mL | |
| 5 mM | 0.4980 mL | 2.4902 mL | 4.9803 mL | |
| 10 mM | 0.2490 mL | 1.2451 mL | 2.4902 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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