[CAS NO. 282526-98-1] Cetilistat
PRODUCTS SPECIFICATIONS [282526-98-1]
DESCRIPTION [282526-98-1]
Overview
| MDL | MFCD09839697 |
|---|---|
| Molecular Weight | 401.58 |
| Molecular Formula | C25H39NO3 |
| SMILES | CC1=CC=C(N=C(OCCCCCCCCCCCCCCCC)OC2=O)C2=C1 |
Summary
Cetilistat (ATL-962), an inhibitor of pancreatic lipase , acts as an effective anti-obesity agent. Cetilistat inhibits rat and human pancreatic lipase activity with IC 50 s of 54.8 nM, and 5.95 nM, respectively [1] .
IC50 & Target
IC50: 54.8 nM (rat pancreatic lipase), 5.95 nM (human pancreatic lipase) [1]
In Vitro
Cetilistat inhibits rat pancreatic lipase activity with an IC 50 of 54.8 nM. Also, Cetilistat inhibits human pancreatic lipase activity with an IC 50 of 5.95 nM, which is 9.2 times more potent than for rat pancreatic lipase [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Cetilistat (3, 10, 30, or 100 mg/kg) reduces intestinal fat absorption by inhibiting pancreatic lipase activity in male SD rats
[1]
.
Cetilistat (4.9, 14.9, or 50.7 mg/kg; mixed into powdered high-fat diet; once a day; for three weeks) shows anti-obesity and antihyperlipidemic effects on DIO F344 rats by reducing intestinal fat absorption
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Fifty male SD rats (eight weeks of age) [1] |
| Dosage: | 3, 10, 30, or 100 mg/kg |
| Administration: | Orally administered; prepared in 0.5 % methylcellulose (MC) suspension |
| Result: | Dose-dependently reduced 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 Model: | Male diet-induced obesity (DIO) F344 rats (five weeks of age) [1] |
| Dosage: | 4.9, 14.9, or 50.7 mg/kg |
| Administration: | Administered as food admixture in a high-fat diet; once a day; for three weeks |
| Result: | Significantly and dose-dependently reduced body weight gain compared with control. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00148382 | Alizyme |
Obesity
|
April 2005 | Phase 1 |
| NCT00156897 | Alizyme |
Non-Insulin-Dependent Diabetes Mellitus|Obesity
|
December 2004 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : < 1 mg/mL (insoluble or slightly soluble)
H 2 O : < 0.1 mg/mL (insoluble)
* Cetilistat is usually formulated as a suspension.
Synonyms