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Chemical Structure| 944808-88-2 Chemical Structure| 944808-88-2

Structure of CAY10566
CAS No.: 944808-88-2

Chemical Structure| 944808-88-2

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CAY10566 is a selective SCD1 inhibitor with bioavailability, commonly used in studies of fatty acid metabolism regulation and metabolic diseases.

4.5 *For Research Use Only !

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Product Citations

Product Citations

Nicholatos, Justin W ; Groot, Joost ; Dhokai, Shekhar ; Tran, David ; Hrdlicka, Lori ; Carlile, Thomas M , et al.

Abstract: Here, we report the independent discovery and validation of stearoyl-CoA desaturase (SCD) as a modulator of α-synuclein (αSyn)-induced pathology and toxicity in cell-based Parkinson’s disease (PD) models. We identified SCD as top altered gene from transcriptional profiling in primary neurons exogenously expressing αSyn with the amplified familial PD mutation 3K. Thus, we sought to further explore SCD as a therapeutic target in neurodegeneration. We report that SCD inhibitors are toxic to early human and rat neuron cultures while displaying minimal toxicity to late cultures. The fatty acid product of SCD, oleic acid (OLA), fully rescues this toxicity in early cultures, suggesting on-target toxicity. Furthermore, SCD inhibition rescues αSyn 3K-induced toxicity in late primary neurons. We also confirm that SCD inhibitors reduce formation of αSyn accumulations, while OLA increases these accumulations in an αSyn 3K neuroblastoma model. However, we identify a caveat with this model where αSyn 3K levels can be suppressed by high SCD inhibitor concentrations, obscuring true effect size. Further, we show that both SCD1 or SCD5 knock-down reduce αSyn 3K accumulations and toxicity, making both a putative drug target. Overall, we confirm key findings of published data on SCD inhibition and its benefits in αSyn accumulation and stress models. The differential neurotoxicity induced by SCD inhibition based on neuron culture age must be accounted for when researching SCD in neuron models and has potential clinical implications. Lastly, our gene profiling studies also revealed novel putative genes connected to αSyn neurotoxicity that are worth further study.

Keywords: cell-based assays ; lipids ; neurotoxicity ; Parkinson’s disease ; SCD ; synuclein

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Product Details of CAY10566

CAS No. :944808-88-2
Formula : C18H17ClFN5O2
M.W : 389.81
SMILES Code : CC1=NN=C(C2=NN=C(N3CCC(OC4=CC(F)=CC=C4Cl)CC3)C=C2)O1
MDL No. :MFCD11976899
InChI Key :WFOFPVXMPTVOTJ-UHFFFAOYSA-N
Pubchem ID :16732433

Safety of CAY10566

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of CAY10566

ferroptosis

Isoform Comparison

Biological Activity

Description
CAY10566 is identified as a potent, orally bioavailable, and selective inhibitor of stearoyl-CoA desaturase1 (SCD1), exhibiting IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. It also demonstrates strong cellular efficacy in HepG2 cells by inhibiting the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs, with an IC50 of 7.9 nM or 6.8 nM[1].[2].

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.83mL

2.57mL

1.28mL

25.65mL

5.13mL

2.57mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

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