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  4. Cyproheptadine hydrochloride

Cyproheptadine hydrochloride is a potent and orally active 5-HT2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine hydrochloride has antiplatelet and thromboprotective activities. Cyproheptadine hydrochloride can be used for the research of thromboembolic disorders.

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

Cyproheptadine hydrochloride Chemical Structure

Cyproheptadine hydrochloride Chemical Structure

CAS No. : 969-33-5

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Based on 3 publication(s) in Google Scholar

Other Forms of Cyproheptadine hydrochloride:

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Description

Cyproheptadine hydrochloride is a potent and orally active 5-HT2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine hydrochloride has antiplatelet and thromboprotective activities. Cyproheptadine hydrochloride can be used for the research of thromboembolic disorders[1][2].

IC50 & Target[1]

5-HT2 Receptor

 

In Vitro

Cyproheptadine hydrochloride (0.01-100 nM; 1 minute) dose-dependently inhibits serotonin-enhanced ADP-induced mouse platelet aggregation in vitro[2].
Cyproheptadine hydrochloride (10 nM) has the ability to inhibit 15 µM serotonin-enhanced ADP-induced (1 µM) tyrosine phosphorylation in platelets in vitro[2].
Cyproheptadine hydrochloride inhibits human platelet PS exposure (Annexin V), P-selectin, and GPIIb-IIIa (PAC-1 binding) activation in vitro[2].

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

In Vivo

Cyproheptadine hydrochloride can be used in animal modeling to construct diabetes models.

Cyproheptadine hydrochloride (1 mg/kg; i.p.; daily, for 5 days; C57BL/6 mice) exerts thromboprotective properties in vivo[2].

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

Animal Model: C57BL/6 mice (8-10 weeks old)[2]
Dosage: 1 mg/kg
Administration: Intraperitoneal injection, daily, for 5 days
Result: Prolonged occlusion times and tail bleeding times in mice.
Clinical Trial
Molecular Weight

323.86

Formula

C21H22ClN

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN1CC/C(CC1)=C2C3=CC=CC=C3C=CC4=CC=CC=C/24.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (154.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0878 mL 15.4388 mL 30.8775 mL
5 mM 0.6176 mL 3.0878 mL 6.1755 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.72 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 (7.72 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:

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).

*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

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 (sealed storage, away from moisture). 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 3.0878 mL 15.4388 mL 30.8775 mL 77.1939 mL
5 mM 0.6176 mL 3.0878 mL 6.1755 mL 15.4388 mL
10 mM 0.3088 mL 1.5439 mL 3.0878 mL 7.7194 mL
15 mM 0.2059 mL 1.0293 mL 2.0585 mL 5.1463 mL
20 mM 0.1544 mL 0.7719 mL 1.5439 mL 3.8597 mL
25 mM 0.1235 mL 0.6176 mL 1.2351 mL 3.0878 mL
30 mM 0.1029 mL 0.5146 mL 1.0293 mL 2.5731 mL
40 mM 0.0772 mL 0.3860 mL 0.7719 mL 1.9298 mL
50 mM 0.0618 mL 0.3088 mL 0.6176 mL 1.5439 mL
60 mM 0.0515 mL 0.2573 mL 0.5146 mL 1.2866 mL
80 mM 0.0386 mL 0.1930 mL 0.3860 mL 0.9649 mL
100 mM 0.0309 mL 0.1544 mL 0.3088 mL 0.7719 mL
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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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Cyproheptadine hydrochloride
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