2. GPCR/G Protein Neuronal Signaling Anti-infection
  3. 5-HT Receptor Parasite
  4. Cyclobenzaprine hydrochloride

Cyclobenzaprine hydrochloride  (Synonyms: MK130 hydrochloride; シクロベンザプリン塩酸塩)

製品番号: HY-B0740 純度: 99.95%
COA 取扱説明書 Technical Support

Cyclobenzaprine (MK130) hydrochloride is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine hydrochloride acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases.

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Cyclobenzaprine hydrochloride

Cyclobenzaprine hydrochloride 構造式

CAS 番号 : 6202-23-9

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 44 在庫あり
Solution
10 mM * 1 mL in DMSO USD 44 在庫あり
Solid
1 g $40 在庫あり
5 g $110 在庫あり
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* アイテムを追加する前、数量をご選択ください

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Other Forms of Cyclobenzaprine hydrochloride:

Cyclobenzaprine hydrochloride 関連抗体

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5-HT Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

Parasite アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

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製品説明

Cyclobenzaprine (MK130) hydrochloride is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine hydrochloride acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases[1][2][3][4][5].

IC50 & Target[1]

5-HT2 Receptor

 

体外実験

Cyclobenzaprine (0-50 μM, 72 h) demonstrates a concentration-dependent activity in Leishmania infantum promastigotes growth, with an IC50 value of 14.5 μM[4].
Cyclobenzaprine (0-50 μM, 72 h) reduces the number of intracellular amastigotes in Leishmania infantum-infected macrophages, with an IC50 value of 12.6 μM[4].
Cyclobenzaprine (0-50 μM, 6 h) induces oxidative stress in Leishmania infantum in a concentration- and time-dependent manner[4].

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

Cyclobenzaprine hydrochloride 関連抗体
体内実験

Cyclobenzaprine (starting dose of 4 mg/kg, p.o., at 60-minute intervals with incremental doses until the EMG frequency is reduced to below 10 Hz) continuously suppresses high quadriceps activity in the ischemic spinal cord rigidity cat model, with an ED100 of 4-12 mg/kg[3].
Cyclobenzaprine (22.8 mg/kg, p.o., single dose) prevents tonic-extensor seizures in the seizure model of male albino CF1 mice (induced by electrical stimulation or Pentylenetetrazol and Strychnine)[3].
Cyclobenzaprine (12.32-49.28 mg/kg, i.g.,, once daily for 5 days) reduces the parasite load in BALB/c mice infected with Leishmania infantum[4].
Cyclobenzaprine hydrochloride (0.3-3.0 mg/kg, i.v., single dose) blocks tonic α-motoneuronal excitation produced by serotonergic descending neurons in Spinalized Male Wistar rats[5].

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

Animal Model: Spinalized Male Wistar rats; Non-spinalized/Intact Male Wistar rats[5]
Dosage: 0.3, 1.0, 3.0 mg/kg
Administration: Intravenous injection (i.v.), single dose
Result: Dose-dependently reduced the monosynaptic reflex amplitude in non-spinalized rats, whereas it did not change the monosynaptic reflex amplitude in spinalized rats.
Significantly inhibited the effect of the 5-HT2 receptor agonist DOI at the dose of 1 mg/kg, which had significantly increased the monosynaptic reflex in spinalized rats at 5 minutes.
Animal Model: Leishmania infantum-infected BALB/c mice model[3]
Dosage: 12.32, 24.64 and 49.28 mg/kg
Administration: Oral gavage (p.o.), once daily for 5 days
Result: Was effective in reducing the parasite load by 40.4% and 66.7% in spleen at 24.64 and 49.28 mg/kg, respectively and by 85.6% and 89.3% in liver at 24.64 and 49.28 mg/kg.
分子量

311.85

分子式

C20H22ClN
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

CN(C)CC/C=C1C2=CC=CC=C2C=CC3=CC=CC=C\13.Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

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

H2O : ≥ 100 mg/mL (320.67 mM)

DMSO : 50 mg/mL (160.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2067 mL 16.0333 mL 32.0667 mL
5 mM 0.6413 mL 3.2067 mL 6.4133 mL
10 mM 0.3207 mL 1.6033 mL 3.2067 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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 (8.02 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 (8.02 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 110 mg/mL (352.73 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
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 (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 / H2O 1 mM 3.2067 mL 16.0333 mL 32.0667 mL 80.1667 mL
5 mM 0.6413 mL 3.2067 mL 6.4133 mL 16.0333 mL
10 mM 0.3207 mL 1.6033 mL 3.2067 mL 8.0167 mL
15 mM 0.2138 mL 1.0689 mL 2.1378 mL 5.3444 mL
20 mM 0.1603 mL 0.8017 mL 1.6033 mL 4.0083 mL
25 mM 0.1283 mL 0.6413 mL 1.2827 mL 3.2067 mL
30 mM 0.1069 mL 0.5344 mL 1.0689 mL 2.6722 mL
40 mM 0.0802 mL 0.4008 mL 0.8017 mL 2.0042 mL
50 mM 0.0641 mL 0.3207 mL 0.6413 mL 1.6033 mL
60 mM 0.0534 mL 0.2672 mL 0.5344 mL 1.3361 mL
80 mM 0.0401 mL 0.2004 mL 0.4008 mL 1.0021 mL
100 mM 0.0321 mL 0.1603 mL 0.3207 mL 0.8017 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.

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Cyclobenzaprine hydrochloride Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

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.

Keywords:

Cyclobenzaprine6202-23-9MK130MK 130MK-1305-HT ReceptorParasiteSerotonin Receptor5-hydroxytryptamine ReceptorLeishmania infantum,Muscle relaxationAntiparasiticInfectionNeurological DiseaseInhibitorinhibitorinhibit

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Cyclobenzaprine hydrochloride
製品番号:
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