1. Metabolic Enzyme/Protease Neuronal Signaling
  2. Apolipoprotein Amyloid-β
  3. CS-6253 TFA

CS-6253 TFA is an agonist of ABCA1. CS-6253 TFA can regulate lipoprotein metabolism, promote high-density lipoprotein biogenesis, and cellular cholesterol efflux. CS-6253 TFA also has certain neuroprotective effects and can clear from the brain. CS-6253 TFA can be used for research on cholesterol metabolism and diseases such as Alzheimer’s disease.

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

CS-6253 TFA Chemical Structure

CS-6253 TFA Chemical Structure

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Based on 1 publication(s) in Google Scholar

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Description

CS-6253 TFA is an agonist of ABCA1. CS-6253 TFA can regulate lipoprotein metabolism, promote high-density lipoprotein biogenesis, and cellular cholesterol efflux. CS-6253 TFA also has certain neuroprotective effects and can clear from the brain. CS-6253 TFA can be used for research on cholesterol metabolism and diseases such as Alzheimer’s disease[1][2][3].

In Vitro

CS-6253 (1 μM; 45 min-24 h) TFA increases the release of cholesterol-containing microvesicles in ABCA1-expressing BHK cells, which is positively correlated with high-density lipoprotein biogenesis[1].

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

In Vivo

CS-6253 (75-225 mg/kg; intravenous injection; once every other day; 5 times in total) TFA transiently increases plasma triglycerides, apolipoprotein E, and Aβ42/40 ratio, while reducing high-density lipoprotein cholesterol and total cholesterol in cynomolgus monkeys[2].
CS-6253 (20 mg/kg; intraperitoneal injection; once every other day; 6 weeks) TFA has improvement in a genetic risk model of Alzheimer’s disease[3].

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

Animal Model: Male apoE4-targeted replacement mice aged 2.5 months old (25 g), in which the endogenous mouse apoE was replaced by either human apoE3 or apoE4[3]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection; once every other day; 6 weeks
Result: Increased the lipidation level of apoE4.
Reversed apoE4-induced Aβ42 accumulation, tau hyperphosphorylation, synaptic damage, and cognitive deficits in hippocampal neurons.
Molecular Weight

3055.48 (free base)

Formula

C136H228N36O43.xC2HF3O2

Appearance

Solid

Color

White to off-white

Sequence

Glu-Val-{Cit}-Ser-Lys-Leu-Glu-Glu-Trp-Leu-Ala-Ala-Leu-{Cit}-Glu-Leu-Ala-Glu-Glu-Leu-Leu-Ala-Arg-Leu-Lys-Ser

Sequence Shortening

EV-{Cit}-SKLEEWLAAL-{Cit}-ELAEELLARLKS

SMILES

OC(CC[C@H](N)C(N[C@@H](C(C)C)C(N[C@@H](CCCNC(N)=O)C(N[C@@H](CO)C(N[C@@H](CCCCN)C(N[C@@H](CC(C)C)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCC(O)=O)C(N[C@H](C(N[C@@H](CC(C)C)C(N[C@@H](C)C(N[C@@H](C)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=O)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC(C)C)C(N[C@@H](C)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@@H](CCCCN)C(N[C@@H](CO)C(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CC1=CNC2=CC=CC=C12)=O)=O)=O)=O)=O)=O)=O)=O)=O.O=C(O)C(F)(F)F.[x]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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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: ≥ 5 mg/mL; Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL; Clear solution

    This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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
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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:
CS-6253 TFA
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HY-P6306A
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