Cyclobenzaprine hydrochloride (Synonyms: MK130 hydrochloride)

Cat. No.: HY-B0740 Purity: 99.59%: FAQs
Data Sheet SDS COA Handling Instructions

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Cyclobenzaprine hydrochloride (MK130 hydrochloride) is a skeletal muscle relaxant and a central nervous system (CNS) depressant.

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

Cyclobenzaprine hydrochloride Chemical Structure

CAS No. : 6202-23-9

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10 mM * 1 mL in DMSO ready for reconstitution	USD 44	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 44	In-stock	Estimated Time of Arrival: December 31
Solid
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Other Forms of Cyclobenzaprine hydrochloride:

Cyclobenzaprine hydrochloride (Standard) Get quote
Cyclobenzaprine-d₃ hydrochloride Get quote
Cyclobenzaprine-¹³C,d₃ hydrochloride Get quote
Cyclobenzaprine-d₆ hydrochloride Get quote

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5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor 5-HT Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

Cyclobenzaprine hydrochloride (MK130 hydrochloride) is a skeletal muscle relaxant and a central nervous system (CNS) depressant. Target: 5-HT Receptor 2A Cyclobenzaprine hydrochloride is a skeletal muscle relaxant and a central nervous system (CNS) depressant. Cyclobenzaprine hydrochloride was thought to be an alpha 2-adrenoceptor agonist that reduced muscle tone by decreasing the activity of descending noradrenergic neurons. Cyclobenzaprine hydrochloride reduced the monosynaptic reflex amplitude dose dependently and this effect was not inhibited by the alpha 2-adrenoceptor antagonists idazoxan and yohimbine. Cyclobenzaprine-induced monosynaptic reflex depression was not attenuated by noradrenergic neuronal lesions produced by 6-hydroxydopamine. Cyclobenzaprine hydrochloride is a 5-HT2 receptor antagonist and that its muscle relaxant effect is due to inhibition of serotonergic, not noradrenergic, descending systems in the spinal cord [1]. The inhibitory effects of Cyclobenzaprine hydrochloride on mono- and polysynaptic reflex potentials are due to the inhibition of descending serotonergic systems through 5-HT(2) receptors in the spinal cord [2].

Clinical Trial

Molecular Weight

311.85

Formula

C₂₀H₂₂ClN

CAS No.

6202-23-9

Appearance

Solid

Color

White to off-white

SMILES

CN(C)CC/C=C1C2=CC=CC=C2C=CC3=CC=CC=C\13.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:

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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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 (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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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)

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).

Purity & Documentation

Purity: 99.59%

Select Batch:

Data Sheet (278 KB) SDS (0 KB)

COA (257 KB) RP-HPLC (245 KB)

Handling Instructions (2659 KB)

References

[1]. Kobayashi, H., Y. Hasegawa, and H. Ono, Cyclobenzaprine, a centrally acting muscle relaxant, acts on descending serotonergic systems. Eur J Pharmacol, 1996. 311(1): p. 29-35. [Content Brief]

[2]. Honda, M., T. Nishida, and H. Ono, Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors. Eur J Pharmacol, 2003. 458(1-2): p. 91-9. [Content Brief]

Complete Stock Solution Preparation Table

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.

Cyclobenzaprine hydrochloride Related Classifications

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 ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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