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  4. Cyproheptadine

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

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Cyproheptadine

Cyproheptadine 構造式

CAS 番号 : 129-03-3

容量 価格(税別) 在庫状況 数量
5 mg $80 在庫あり
10 mg $130 在庫あり
25 mg $240 在庫あり
50 mg $350 在庫あり
100 mg $520 在庫あり
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カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Other Forms of Cyproheptadine:

Top Publications Citing Use of Products
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製品説明

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

IC50 & Target

5-HT2A Receptor

 

体外実験

Cyproheptadine (0.01-100 nM; 1 minute) dose-dependently inhibits serotonin-enhanced ADP-induced mouse platelet aggregation in vitro[2].
Cyproheptadine (10 nM) has the ability to inhibit 15 μM serotonin-enhanced ADP-induced (1 μM) tyrosine phosphorylation in platelets in vitro[2].
Cyproheptadine 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.

体内実験

Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

Cyproheptadine can be used in animal modeling to create diabetes models. In rats, Cyproheptadine undergoes demethylation and oxidation to form desmethylcyproheptadine (DMCPHepo), while cyproheptadine epoxide (CPHepo) is a minor metabolite. DMCPHepo accumulates in tissues and persists longer than predicted by its plasma concentration profile. DMCPHepo may be an active metabolite of Cyproheptadine and could be associated with islet cell damage. Additionally, the remaining dose of Cyproheptadine may be excreted via feces in the form of the parent compound or its metabolites[1].

Induction of Diabetes Disease[1].
Background
Cyproheptadine and its several metabolites, including desmethyl Cyproheptadine epoxide (DMCPH epoxide), desmethyl Cyproheptadine (DMCPH) and Cyproheptadine epoxide, inhibit insulin synthesis as well as glucose and stimulated insulin release[1].
Specific Modeling Methods
Rat: Wistar• male• weighing 150-225 g[3]
Administration: 0-90 mg/kg• p.o. or i.p.• daily for 14 days[3]
Mice: Swiss Webster• male• weighing 25-30 g[3]
Administration: 0-90 mg/kg• p.o.• daily for 14 days[3]
Rabbits: New Zealand white• male• weighing 1000-1500 g[3]
Administration: 0, 225mg/kg• p.o.• daily for 14 days[3]
Hamsters: Golden• male• weighing 100-150 g[3]
Administration: 0-90 mg/kg• p.o.• daily for 14 days[3]
Note
(1)Oral doses of Cyproheptadine were administered in aqueous solution or in an aqueous suspension containing 0.15 % methylcellulose. Intraperitoneally (ip)-treated rats received cyproheptadine in saline solution. Animals were sacrificed 24 h after the last dose[3].
(2)Animals were allowed food and water ad libitum throughout the study unless otherwise stated[3].
Modeling Indicators
Morphological change: Cyproheptadine caused a depression in weight gain and exhibited a markedly diminished glucose tolerance in animals[3].
Histological analysis: Cyproheptadine induced marked cytoplasmic vacuolization of islet cells in rat pancreas. Vacuoles varied in size and in the most severely affected cells occupied the major portion of the cytoplasm, displacing and slightly compressing the nucleus[3].
Organelle change: The majority of islet cells, presumably the β cell population, showed marked alteration of the rough endoplasmic reticulum and loss of secretory granules. Rough endoplasmic reticulum was vesiculated and the cisternae contained finely granular electron-dense material[3].

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.
臨床実験
分子量

287.40

分子式

C21H21N

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 3.17 mg/mL (11.03 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C; 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 3.4795 mL 17.3974 mL 34.7947 mL
5 mM 0.6959 mL 3.4795 mL 6.9589 mL
10 mM 0.3479 mL 1.7397 mL 3.4795 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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一般には略語で表示されます:C1V1 = C2V2

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In Vivo Dissolution Calculator
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純度とドキュメンテーション
参考文献

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 3.4795 mL 17.3974 mL 34.7947 mL 86.9868 mL
5 mM 0.6959 mL 3.4795 mL 6.9589 mL 17.3974 mL
10 mM 0.3479 mL 1.7397 mL 3.4795 mL 8.6987 mL
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  • Dilution Calculator

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

質量   濃度   体積   分子量 *
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The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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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Inquiry Information

製品名:
Cyproheptadine
製品番号:
HY-B1622
数量:
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