Methiothepin mesylate (Synonyms: Metitepine mesylate; Ro 8-6837 mesylate)

Name: Methiothepin mesylate
Brand: MedChemExpress
SKU: HY-107836
Rating: 4.5 (1 reviews)

Cat. No.: HY-107836 Purity: 99.60%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT₂ receptor antagonist, with pK_ds of 7.10 (5-HT_1A), 7.28 (5HT_1B), 7.56 (5HT_1C), 6.99 (5HT_1D), 7.0 (5-HT_5A), 7.8 (5-HT_5B), 8.74 (5-HT₆), and 8.99 (5-HT₇), and pK_is of 8.50 (5HT_2A), 8.68 (5HT_2B), and 8.35 (5HT_2C).

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

Methiothepin mesylate Chemical Structure

CAS No. : 74611-28-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 40	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 40	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 37	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Methiothepin mesylate:

Methiothepin maleate Get quote
Methiothepin Get quote

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View All 5-HT Receptor Isoform Specific Products:

View All Isoforms

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

IC₅₀ & Target

5-HT_1A Receptor

7.10 (pKd)

5-HT_1B Receptor

7.28 (pKd)

5-HT_1C Receptor

7.56 (pKd)

5-HT_1D Receptor

6.99 (pKd)

5-HT_5A Receptor

7.0 (pKd)

5-HT_5B Receptor

7.8 (pKd)

5-HT₆ Receptor

8.74 (pKd)

5-HT₇ Receptor

8.99 (pKd)

5-HT_2A Receptor

8.50 (pKi)

5-HT_2B Receptor

8.68 (pKi)

5-HT_2C Receptor

8.35 (pKi)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	56 nM Compound: Methiothepin mesylate	Antagonistic activity at 5-HT2A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assay Antagonistic activity at 5-HT2A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assay	[PMID: 27487565]
CHO-K1	IC₅₀	71 nM Compound: Methiothepin mesylate	Antagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assay Antagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assay	[PMID: 27487565]

In Vitro

Methiothepin mesylate is a 5-HT receptor antagonist, with pK_ds of 7.10, 7.28, 7.56, and 6.99 for 5-HT_1A, 5HT_1B, 5HT_1C, 5HT_1D^[1]. Methiothepin mesylate also shows pK_ds of 7.0, 7.8, 8.74, and 8.99 for 5-HT_5A, 5-HT_5B, 5-HT₆, and 5-HT₇, respectively^[2]. Methiothepin exhibits high affinity at 5-HT_2A, 5HT_2B, and 5HT_2C with pK_is of 8.50, 8.68, and 8.35, respectively^[3].

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

Molecular Weight

452.65

Formula

C₂₁H₂₈N₂O₃S₃

CAS No.

74611-28-2

Appearance

Solid

Color

White to light yellow

SMILES

CN1CCN(C2CC3=CC=CC=C3SC4=CC=C(SC)C=C24)CC1.CS(=O)(O)=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 : 62.5 mg/mL (138.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (110.46 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2092 mL	11.0461 mL	22.0921 mL
5 mM	0.4418 mL	2.2092 mL	4.4184 mL
10 mM	0.2209 mL	1.1046 mL	2.2092 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: ≥ 2.08 mg/mL (4.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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: 100 mg/mL (220.92 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: 99.60%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (253 KB) HNMR (266 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Schoeffter P, et al. 5-Hydroxytryptamine (5-HT)-induced endothelium-dependent relaxation of pig coronary arteries is mediated by 5-HT receptors similar to the 5-HT1D receptor subtype. J Pharmacol Exp Ther. 1990 Jan;252(1):387-95. [Content Brief]

[2]. Knight AR, et al. Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23. Epub 2004 Jul 30. [Content Brief]

[3]. Hoyer D, et al. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol Rev. 1994 Jun;46(2):157-203. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	2.2092 mL	11.0461 mL	22.0921 mL	55.2303 mL
	5 mM	0.4418 mL	2.2092 mL	4.4184 mL	11.0461 mL
	10 mM	0.2209 mL	1.1046 mL	2.2092 mL	5.5230 mL
	15 mM	0.1473 mL	0.7364 mL	1.4728 mL	3.6820 mL
	20 mM	0.1105 mL	0.5523 mL	1.1046 mL	2.7615 mL
	25 mM	0.0884 mL	0.4418 mL	0.8837 mL	2.2092 mL
	30 mM	0.0736 mL	0.3682 mL	0.7364 mL	1.8410 mL
	40 mM	0.0552 mL	0.2762 mL	0.5523 mL	1.3808 mL
	50 mM	0.0442 mL	0.2209 mL	0.4418 mL	1.1046 mL
	60 mM	0.0368 mL	0.1841 mL	0.3682 mL	0.9205 mL
	80 mM	0.0276 mL	0.1381 mL	0.2762 mL	0.6904 mL
	100 mM	0.0221 mL	0.1105 mL	0.2209 mL	0.5523 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.

Methiothepin mesylate Related Classifications

Neurological Disease

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:

Methiothepin74611-28-2MetitepineRo 8-68375-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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Methiothepin mesylate (Synonyms: Metitepine mesylate; Ro 8-6837 mesylate)

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Other Forms of Methiothepin mesylate:

Methiothepin mesylate Related Antibodies

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Purity & Documentation

References

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Methiothepin mesylate Related Antibodies

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Complete Stock Solution Preparation Table

Methiothepin mesylate Related Classifications

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