1. Metabolic Enzyme/Protease
  2. Stearoyl-CoA Desaturase (SCD)
  3. CAY10566

CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. CAY10566 also shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM).

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

CAY10566 Chemical Structure

CAY10566 Chemical Structure

CAS No. : 944808-88-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 163 In-stock
Solution
10 mM * 1 mL in DMSO USD 163 In-stock
Solid
1 mg USD 60 In-stock
5 mg USD 190 In-stock
10 mg USD 290 In-stock
25 mg USD 590 In-stock
50 mg USD 950 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. CAY10566 also shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM)[1][2].

IC50 & Target

IC50: 4.5 nM (SCD1 in mouse), 26 nM (SCD1 in human)[2]

In Vitro

CAY10566 (0.0001-10 μM; 24 hours) concentration-dependently decreases Swiss 3T3 cell proliferation[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[3]

Cell Line: Swiss 3T3 cells
Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 24 hours
Result: Swiss 3T3 cell proliferation was concentration-dependently decreased.
In Vivo

After establishment of palpable tumors, the mice are treated with vehicle or SCD1 inhibitor (2.5 mg/kg CAY10566 orally twice daily). The effect of SCD1 inhibition on the Akt-driven tumors is greater than on the Ras-driven tumors, with the mean tumor volume at day 13 or 14 post therapy, relative to untreated tumors, 0.5±0.04 and 0.67±0.05 respectively (P=0.01 for Ras-Akt comparison, by two-tailed t test)[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

389.81

Formula

C18H17ClFN5O2

CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

CC1=NN=C(C2=NN=C(N3CCC(OC4=CC(F)=CC=C4Cl)CC3)C=C2)O1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (64.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5654 mL 12.8268 mL 25.6535 mL
5 mM 0.5131 mL 2.5654 mL 5.1307 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • 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% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Purity: 99.73%

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5654 mL 12.8268 mL 25.6535 mL 64.1338 mL
5 mM 0.5131 mL 2.5654 mL 5.1307 mL 12.8268 mL
10 mM 0.2565 mL 1.2827 mL 2.5654 mL 6.4134 mL
15 mM 0.1710 mL 0.8551 mL 1.7102 mL 4.2756 mL
20 mM 0.1283 mL 0.6413 mL 1.2827 mL 3.2067 mL
25 mM 0.1026 mL 0.5131 mL 1.0261 mL 2.5654 mL
30 mM 0.0855 mL 0.4276 mL 0.8551 mL 2.1378 mL
40 mM 0.0641 mL 0.3207 mL 0.6413 mL 1.6033 mL
50 mM 0.0513 mL 0.2565 mL 0.5131 mL 1.2827 mL
60 mM 0.0428 mL 0.2138 mL 0.4276 mL 1.0689 mL
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CAY10566 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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Product Name:
CAY10566
Cat. No.:
HY-15823
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