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MedKoo Cat#: 319937 | Name: Cetilistat
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Cetilistat, also known as ATL-962, is a drug designed to treat obesity. It acts in the same way as the older drug orlistat (Xenical) by inhibiting pancreatic lipase, an enzyme that breaks down triglycerides in the intestine. Without this enzyme, triglycerides from the diet are prevented from being hydrolyzed into absorbable free fatty acids and are excreted undigested.

Chemical Structure

Cetilistat
Cetilistat
CAS#282526-98-1

Theoretical Analysis

MedKoo Cat#: 319937

Name: Cetilistat

CAS#: 282526-98-1

Chemical Formula: C25H39NO3

Exact Mass: 401.2930

Molecular Weight: 401.59

Elemental Analysis: C, 74.77; H, 9.79; N, 3.49; O, 11.95

Price and Availability

Size Price Availability Quantity
1g USD 150.00 2 Weeks
2g USD 250.00 2 Weeks
5g USD 450.00 2 Weeks
10g USD 750.00 2 Weeks
25g USD 1,250.00 2 Weeks
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Related CAS #
No Data
Synonym
ATL-962; ATL962; ATL 962; Cetilistat
IUPAC/Chemical Name
2-(hexadecyloxy)-6-methyl-4H-benzo[d][1,3]oxazin-4-one
InChi Key
MVCQKIKWYUURMU-UHFFFAOYSA-N
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
SMILES Code
O=C1C2=CC(C)=CC=C2N=C(OCCCCCCCCCCCCCCCC)O1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
In human trials, cetilistat was shown to produce similar weight loss to orlistat, but also produced similar side effects such as oily, loose stools, fecal incontinence, frequent bowel movements, and flatulence. It is likely that the same precautions would apply in that absorption of fat-soluble vitamins and other fat-soluble nutrients may be inhibited, requiring vitamin supplements to be used to avoid deficiencies. Cetilistat has completed Phase 1 and 2 trials in the West and is currently in Phase 3 trials in Japan where it is partnered with Takeda. Norgina BV has now acquired the full global rights to cetilistat from Alizyme after the latter went into administration.
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Cetilistat (ATL-962), an inhibitor of pancreatic lipase, acts as an effective anti-obesity agent. Cetilistat inhibits rat and human pancreatic lipase activity with IC50s of 54.8 nM, and 5.95 nM, respectively.
In vitro activity:
Cetilistat was identified as a most potent anti-SARS-CoV-2 drug compound using the cut-off of 90 % effective concentrations (EC90) <10 μM after treating VeroE6 cells with 0.01 MOI of SARS-CoV-2 for 48 h. Using plaque reduction assay, the EC50 of the drug compounds were determined to be 1.13 μM (cetilistat) (Fig. 3 A–D). At 48 hpi, the 50 % cytotoxic concentrations (CC50) of cetilistat was >100 μM (Table 2 ). The selectivity index of these four drug compounds were >88.50 (cetilistat). Reference: Pharmacol Res. 2020 Sep;159:104960. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/32473310/
In vivo activity:
Cetilistat is a novel inhibitor of pancreatic lipase. The aim of this report is to evaluate the anti-obesity action of cetilistat in diet-induced obesity (DIO) rats. Cetilistat inhibited rat and human pancreatic lipase activity with an IC (50) of 54.8 nmol/l, and 5.95 nmol/l, respectively, meaning that it is 9.2 times more potent for human pancreatic lipase than for that of rat. Cetilistat was orally administered simultaneously with fat emulsion to Sprague-Dawley rats. Plasma triglyceride (TG) concentrations were measured before and after oral fat loading. The elevation in plasma triglyceride concentration by oral fat loading was reduced by cetilistat in a dose-dependent manner at 3, 10, 30, and 100 mg/kg, indicating that cetilistat reduces intestinal fat absorption in rats. Cetilistat was administered to DIO F344 rats as food admixture in a high-fat diet at 4.9, 14.9, or 50.7 mg/kg/day for three weeks. Both triglyceride and nonesterified fatty acid content in the feces were dose-dependently and drastically increased, suggesting the intestinal breakdown of fat and excretion. Body weight (BW) gain and white adipose tissue (WAT) weight were reduced in a dose-dependent manner. In addition, leptin, TG, and total cholesterol (TC) in plasma were reduced and there were no reports of oily stools. These results suggest that cetilistat ameliorates obesity and hyperlipidemia in DIO rats, a plausible animal model of the most common type of human obesity. Reference: Horm Metab Res. 2008 Aug;40(8):539-43. https://www.thieme-connect.com/DOI/DOI?10.1055/s-2008-1076699
Solvent mg/mL mM
Solubility
DMSO 3.0 7.47
Ethanol 8.0 19.92
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 401.59 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
1. Yuan S, Chan JFW, Chik KKH, Chan CCY, Tsang JOL, Liang R, Cao J, Tang K, Chen LL, Wen K, Cai JP, Ye ZW, Lu G, Chu H, Jin DY, Yuen KY. Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening system. Pharmacol Res. 2020 Sep;159:104960. doi: 10.1016/j.phrs.2020.104960. Epub 2020 May 28. PMID: 32473310; PMCID: PMC7254006. 2. Yamada Y, Kato T, Ogino H, Ashina S, Kato K. Cetilistat (ATL-962), a novel pancreatic lipase inhibitor, ameliorates body weight gain and improves lipid profiles in rats. Horm Metab Res. 2008 Aug;40(8):539-43. doi: 10.1055/s-2008-1076699. Epub 2008 May 21. PMID: 18500680.
In vivo protocol:
1. Yamada Y, Kato T, Ogino H, Ashina S, Kato K. Cetilistat (ATL-962), a novel pancreatic lipase inhibitor, ameliorates body weight gain and improves lipid profiles in rats. Horm Metab Res. 2008 Aug;40(8):539-43. doi: 10.1055/s-2008-1076699. Epub 2008 May 21. PMID: 18500680.
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