1. Metabolic Enzyme/Protease
  2. Lipase
  3. Cetilistat

Cetilistat  (Synonyms: ATL-962)

Cat. No.: HY-14471 Purity: ≥98.0%
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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.

For research use only. We do not sell to patients.

Cetilistat Chemical Structure

Cetilistat Chemical Structure

CAS No. : 282526-98-1

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

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[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 IC50 of 54.8 nM. Also, Cetilistat inhibits human pancreatic lipase activity with an IC50 of 5.95 nM, which is 9.2 times more potent than for rat pancreatic lipase[1].

MedChemExpress (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].

MedChemExpress (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
Molecular Weight

401.58

Formula

C25H39NO3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=CC=C(N=C(OCCCCCCCCCCCCCCCC)OC2=O)C2=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

Ethanol : 2.5 mg/mL (6.23 mM; ultrasonic and warming and heat to 60°C)

DMSO : 1 mg/mL (2.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 0.1 mg/mL (0.25 mM; Need ultrasonic)

*Cetilistat is usually formulated as a suspension.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% Saline

    Solubility: 0.25 mg/mL (0.62 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 0.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (2.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in Saline)

    Solubility: 0.25 mg/mL (0.62 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 0.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (2.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 2.4902 mL 12.4508 mL 24.9016 mL 62.2541 mL
Ethanol 5 mM 0.4980 mL 2.4902 mL 4.9803 mL 12.4508 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Cetilistat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Cetilistat
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