Cyproheptadine hydrochloride sesquihydrate

Name: Cyproheptadine hydrochloride sesquihydrate
Brand: MedChemExpress
SKU: HY-B1165
Rating: 5.0 (3 reviews)

Cat. No.: HY-B1165 Purity: 99.82%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2.

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

Cyproheptadine hydrochloride sesquihydrate Chemical Structure

CAS No. : 41354-29-4

Size	Stock	Quantity

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 g	In-stock	Estimated Time of Arrival: December 31
5 g	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Cyproheptadine hydrochloride sesquihydrate:

Cyproheptadine hydrochloride In-stock
Cyproheptadine Get quote
Cyproheptadine (hydrochloride sesquihydrate) (Standard) Get quote

3 Publications Citing Use of MCE Cyproheptadine hydrochloride sesquihydrate

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2.

IC₅₀ & Target

5-HT₂ Receptor

In Vitro

Cyproheptadine (20-120 μM; 24 h) hydrochloride sesquihydrate inhibits proliferation of hepatocellular carcinoma cells (HepG2 and Huh-7) by blocking cell cycle progression through the activation of P38 MAP kinase^[1].
Cyproheptadine hydrochloride (5-30 μM; 24-72 h) sesquihydrate reduces the viability of myeloma and leukemia cell lines^[2].
Cyproheptadine (62.5-95 μM; 24-72 h) hydrochloride sesquihydrate causes apoptosis and decreases inflammation by disrupting thiol/disulfide balance and enhancing the levels of SIRT1 in C6 glioblastoma cells as well as inhibits cell proliferation^[3].
Cyproheptadine (50 μM; 24 h) hydrochloride sesquihydrate inhibits cell proliferation, induces cell cycle arrest in the G1 phase, and subsequently causes apoptosis and necrosis in bladder cancer cell lines^[4].
Cyproheptadine (20 nM-20 μM) hydrochloride sesquihydrate enhances the delayed rectifier outward potassium current in a concentration - dependent manner in mouse cortical neurons^[5].
Cyproheptadine (20-30 μM; 24-72 h) hydrochloride sesquihydrate inhibits the growth, migration and invasion of LLC1 and A549 cells^[6].
Cyproheptadine (10 μM) hydrochloride sesquihydrate increases the excitability of pyramidal neurons in mouse medial prefrontal cortex slices, as indicated by increased action potential frequency, reduced current density for generating action potentials, depolarized resting membrane potential, decreased delay time to elicit an action potential, and reduced spike threshold potential^[8].

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

Cell Viability Assay^[1]

Cell Line:	HepG2 and Huh-7 cells
Concentration:	20, 40, 60, 80, 100, 120 μM
Incubation Time:	24 h
Result:	Inhibited cell proliferation in a dose-dependent manner. Showed IC₅₀ of 44.4 and 44.7 μM in HepG2 cells and Huh-7 cells, respectively.

In Vivo

Cyproheptadine (40 mg/kg; i.p.; per day; 5 days) hydrochloride sesquihydrate completely inhibits the formation of malignant ascites in mice injected intraperitoneally with MDAY-D2 leukemia cells^[2].
Cyproheptadine (20 mg/kg; i.p.; 3 times per week) hydrochloride sesquihydrate significantly reduces LLC1 tumor growth rate and tumor weight in Setd7 knockout (KO) and wild-type (WT) C57BL/6J mice injected subcutaneously with LLC1 cells^[6].
Cyproheptadine hydrochloride (4 mg/kg; i.p.) sesquihydrate reduces the seizure threshold, increases the severity of seizures, and decreases the efficacy of clinically used anti-epileptic drugs in the mouse seizure models induced by Pentylenetetrazol (PTZ), Picrotoxin (HY-101391), and maximal electroshock (MES)^[7].
Cyproheptadine (45 mg/kg; p.o.; 8 days) hydrochloride sesquihydrate causes significant hyperglycaemia in male albino mice^[9].

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

Animal Model:	DBA2 mice with intraperitoneal injection of MDAY-D2 murine leukemia cells; NOD/SCID mice with subcutaneous injection of LP-1 myeloma cells^[2]
Dosage:	40 mg/kg (DBA2 mice), 36 mg/kg (NOD/SCID mice)
Administration:	5 days (DBA2 mice), 7 weeks (NOD/SCID mice)
Result:	Completely abolished the formation of malignant ascites in DBA2 mice. Delayed tumor growth, with approximately a 2-fold reduction in tumor volume in NOD/SCID mice, at the end of treatment.

Molecular Weight

350.88

Formula

C₂₁H₂₁N.3/2H₂O.HCl

CAS No.

41354-29-4

Appearance

Solid

Color

White to off-white

SMILES

CN1CC/C(CC1)=C2C3=CC=CC=C3C=CC4=CC=CC=C/24.[H]Cl.O

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 : 33.33 mg/mL (94.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 0.67 mg/mL (1.91 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8500 mL	14.2499 mL	28.4998 mL
5 mM	0.5700 mL	2.8500 mL	5.7000 mL
10 mM	0.2850 mL	1.4250 mL	2.8500 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 3 mg/mL (8.55 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: ≥ 3 mg/mL (8.55 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 3 mg/mL (8.55 mM); Clear solution

This protocol yields a clear solution of ≥ 3 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 (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 99.82%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (253 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Feng YM, et al. Cyproheptadine, an antihistaminic drug, inhibits proliferation of hepatocellular carcinoma cells by blocking cell cycle progression through the activation of P38 MAP kinase. BMC Cancer. 2015 Mar 17;15:134. [Content Brief]

[2]. Mao X, et al. Cyproheptadine displays preclinical activity in myeloma and leukemia. Blood. 2008 Aug 1;112(3):760-9. [Content Brief]

[3]. Kacar S, et al. Cyproheptadine causes apoptosis and decreases inflammation by disrupting thiol/disulfide balance and enhancing the levels of SIRT1 in C6 glioblastoma cells. Toxicol In Vitro. 2021 Jun;73:105135. [Content Brief]

[4]. Hsieh HY, et al. Cyproheptadine exhibits antitumor activity in urothelial carcinoma cells by targeting GSK3β to suppress mTOR and β-catenin signaling pathways. Cancer Lett. 2016 Jan 1;370(1):56-65. [Content Brief]

[5]. He YL, et al. Cyproheptadine enhances the I(K) of mouse cortical neurons through sigma-1 receptor-mediated intracellular signal pathway. PLoS One. 2012;7(7):e41303. [Content Brief]

[6]. Shannar A, et al. Cyproheptadine inhibits in vitro and in vivo lung metastasis and drives metabolic rewiring. Mol Biol Rep. 2024 Nov 10;51(1):1139. [Content Brief]

[7]. Singh D, et al. Proconvulsant potential of cyproheptadine in experimental animal models. Fundam Clin Pharmacol. 2010 Aug;24(4):451-5. [Content Brief]

[8]. He YL, et al. Cyproheptadine Regulates Pyramidal Neuron Excitability in Mouse Medial Prefrontal Cortex. Neurosci Bull. 2018 Oct;34(5):759-768. [Content Brief]

[9]. Cakici I, et al. Hypoglycaemic effect of Momordica charantia extracts in normoglycaemic or cyproheptadine-induced hyperglycaemic mice. J Ethnopharmacol. 1994 Oct;44(2):117-21. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.8500 mL	14.2499 mL	28.4998 mL	71.2494 mL
DMSO	5 mM	0.5700 mL	2.8500 mL	5.7000 mL	14.2499 mL
	10 mM	0.2850 mL	1.4250 mL	2.8500 mL	7.1249 mL
	15 mM	0.1900 mL	0.9500 mL	1.9000 mL	4.7500 mL
	20 mM	0.1425 mL	0.7125 mL	1.4250 mL	3.5625 mL
	25 mM	0.1140 mL	0.5700 mL	1.1400 mL	2.8500 mL
	30 mM	0.0950 mL	0.4750 mL	0.9500 mL	2.3750 mL
	40 mM	0.0712 mL	0.3562 mL	0.7125 mL	1.7812 mL
	50 mM	0.0570 mL	0.2850 mL	0.5700 mL	1.4250 mL
	60 mM	0.0475 mL	0.2375 mL	0.4750 mL	1.1875 mL
	80 mM	0.0356 mL	0.1781 mL	0.3562 mL	0.8906 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.