2. Membrane Transporter/Ion Channel Neuronal Signaling Epigenetics Cell Cycle/DNA Damage NF-κB Apoptosis
  3. GABA Receptor Sirtuin Keap1-Nrf2 Apoptosis
  4. Cipepofol

Cipepofol  (Synonyms: Ciprofol; HSK3486)

Cat. No.: HY-116152 Purity: 99.42% ee.: 100.00%
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Cipepofol (Ciprofol), a novel 2,6-disubstituted phenol derivative, is a positive allosteric modulator and direct agonist of the GABAA receptor. Cipepofol can cause the central nerve inhibition and promote sleep based on the structural modification of Propofol (HY-B0649). Cipepofol can activate the sirtuin1 (Sirt1)/Nrf2 pathway. Cipepofol protects the heart against Isoproterenol (ISO; HY-B0468)-induced myocardial infarction by reducing cardiac oxidative stress, inflammatory response and cardiomyocyte apoptosis.

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

Cipepofol Chemical Structure

Cipepofol Chemical Structure

CAS No. : 1637741-58-2

Size Price Stock Quantity
Liquid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 231 In-stock
Solution
10 mM * 1 mL in DMSO USD 231 In-stock
Liquid
1 mg USD 103 In-stock
5 mg USD 228 In-stock
10 mg USD 364 In-stock
25 mg USD 728 In-stock
50 mg USD 1165 In-stock
100 mg USD 1860 In-stock
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Based on 1 publication(s) in Google Scholar

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Cipepofol Related Antibodies

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Description

Cipepofol (Ciprofol), a novel 2,6-disubstituted phenol derivative, is a positive allosteric modulator and direct agonist of the GABAA receptor. Cipepofol can cause the central nerve inhibition and promote sleep based on the structural modification of Propofol (HY-B0649). Cipepofol can activate the sirtuin1 (Sirt1)/Nrf2 pathway. Cipepofol protects the heart against Isoproterenol (ISO; HY-B0468)-induced myocardial infarction by reducing cardiac oxidative stress, inflammatory response and cardiomyocyte apoptosis[1][2].

In Vitro

Cipepofol (Ciprofol) can trigger chloride influx by competitive binding to butylbicyclophosphorothionate and t-butylbicycloorthobenzoate targets in the chloride channels of GABAA receptors. The influx of chloride can cause hyperpolarization of nerve cell membranes by increasing the intracellular chloride concentration and further activating GABAergic neurons to achieve central nerve inhibition[1].
Cipepofol (5 μM before ISO insult for 6 h) blunts the contents of CK-MB, LDH and cTnT were increased in ISO-treated H9c2 cells. Cipepofol attenuates ISO-induced cardiomyocyte apoptosis in vitro[2].

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

Cipepofol Related Antibodies
In Vivo

Cipepofol (Ciprofol; 100 μL; implanted into the abdomen of mice 1 h before ISO) suppresses ISO-induced myocardial damage, cardiac dysfunction, and inflammation and cardiomyocyte apoptosis[2].

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

Animal Model: Eighty male C57BL/6 mice (20-24 g, 8-10 weeks)[2]
Dosage: 100 μl
Administration: Implanted into the abdomen of mice 1 h before ISO
Result: Attenuated increased the content of serum CK-MB, LDH, and cTnT by ISO insults (100 mg/kg; sc; for 2 consecutive days to induce experimental myocardial infarction).
Significantly improved ISO-induced LV systolic and diastolic dysfunction.
Largely suppressed the increases in IL-6 IL-17 and TNF-α expression.
Clinical Trial
Molecular Weight

204.31

Formula

C14H20O
CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

CC(C1=CC=CC([C@@H](C2CC2)C)=C1O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (489.45 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 4.8945 mL 24.4726 mL 48.9452 mL
5 mM 0.9789 mL 4.8945 mL 9.7890 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Mass
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Concentration
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Volume
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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (12.24 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 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% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (12.24 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.
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:
%
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.8945 mL 24.4726 mL 48.9452 mL 122.3631 mL
5 mM 0.9789 mL 4.8945 mL 9.7890 mL 24.4726 mL
10 mM 0.4895 mL 2.4473 mL 4.8945 mL 12.2363 mL
15 mM 0.3263 mL 1.6315 mL 3.2630 mL 8.1575 mL
20 mM 0.2447 mL 1.2236 mL 2.4473 mL 6.1182 mL
25 mM 0.1958 mL 0.9789 mL 1.9578 mL 4.8945 mL
30 mM 0.1632 mL 0.8158 mL 1.6315 mL 4.0788 mL
40 mM 0.1224 mL 0.6118 mL 1.2236 mL 3.0591 mL
50 mM 0.0979 mL 0.4895 mL 0.9789 mL 2.4473 mL
60 mM 0.0816 mL 0.4079 mL 0.8158 mL 2.0394 mL
80 mM 0.0612 mL 0.3059 mL 0.6118 mL 1.5295 mL
100 mM 0.0489 mL 0.2447 mL 0.4895 mL 1.2236 mL
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Cipepofol 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.

Keywords:

Cipepofol1637741-58-2Ciprofol HSK3486HSK3486HSK 3486HSK-3486GABA ReceptorSirtuinKeap1-Nrf2ApoptosisGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptor2,6-disubstituted phenolcentral nervesirtuin1Sirt1heartmyocardial infarctioncardiac oxidative stressinflammatorycardiomyocyteInhibitorinhibitorinhibit

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