2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Methiothepin mesylate

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

Cat. No.: HY-107836 Purity: 99.60%
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COA
Handling Instructions Technical Support

Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).

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

Methiothepin mesylate Chemical Structure

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
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Based on 1 publication(s) in Google Scholar

Other Forms of Methiothepin mesylate:

Methiothepin mesylate Related Antibodies

Top Publications Citing Use of Products

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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

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Description

Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).

IC50 & Target

5-HT1A Receptor

7.10 (pKd)

5-HT1A Receptor

 

5-HT1B Receptor

 

5-HT1C Receptor

 

5-HT1D Receptor

 

5-HT2A Receptor

 

5-HT2B Receptor

 

5-HT2C Receptor

 

5-HT5A Receptor

 

5-HT5B Receptor

 

5-HT6 Receptor

 

5-HT7 Receptor

 

5-HT1B Receptor

7.28 (pKd)

5-HT1C Receptor

7.56 (pKd)

5-HT1D Receptor

6.99 (pKd)

5-HT5A Receptor

7.0 (pKd)

5-HT5B Receptor

7.8 (pKd)

5-HT6 Receptor

8.74 (pKd)

5-HT7 Receptor

8.99 (pKd)

5-HT2A Receptor

8.50 (pKi)

5-HT2B Receptor

8.68 (pKi)

5-HT2C 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 pKds of 7.10, 7.28, 7.56, and 6.99 for 5-HT1A, 5HT1B, 5HT1C, 5HT1D[1]. Methiothepin mesylate also shows pKds of 7.0, 7.8, 8.74, and 8.99 for 5-HT5A, 5-HT5B, 5-HT6, and 5-HT7, respectively[2]. Methiothepin exhibits high affinity at 5-HT2A, 5HT2B, and 5HT2C with pKis 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.

Methiothepin mesylate Related Antibodies
Molecular Weight

452.65

Formula

C21H28N2O3S3
CAS No.
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 : 250 mg/mL (552.30 mM; Need ultrasonic; 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 2.2092 mL 11.0461 mL 22.0921 mL
5 mM 0.4418 mL 2.2092 mL 4.4184 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.

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.60%

SDS (393 KB)

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

Handling Instructions (2659 KB)
References

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 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
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Methiothepin mesylate 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:

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

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