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[CAS NO. 1637741-58-2]  Cipepofol

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PRODUCTS SPECIFICATIONS [1637741-58-2]

Fulfillment
Catalog
HY-116152
Brand
MCE
CAS
1637741-58-2

DESCRIPTION [1637741-58-2]

Overview

MDL-
Molecular Weight204.31
Molecular FormulaC14H20O
SMILESCC(C1=CC=CC([C@@H](C2CC2)C)=C1O)C

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

Summary

Cipepofol (Ciprofol), a novel 2,6-disubstituted phenol derivative, is a positive allosteric modulator and direct agonist of the GABA A 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

NCT Number Sponsor Condition Start Date Phase
NCT04294056 Haisco Pharmaceutical Group Co., Ltd.
Anesthesia
May 26, 2020 Phase 1
NCT04147416 Sichuan Haisco Pharmaceutical Group Co., Ltd|Haisco Pharmaceutical Group Co., Ltd.
Sedation
November 22, 2019 Phase 2
NCT03745625 Sichuan Haisco Pharmaceutical Group Co., Ltd|Haisco Pharmaceutical Group Co., Ltd.
Anesthesia|Sedation
January 9, 2019 Phase 1

Appearance

Liquid


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)

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
10 mM 0.4895 mL 2.4473 mL 4.8945 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (12.24 mM); Clear solution

* All of the co-solvents are available by MedChemExpress (MCE).


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