1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor

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

目录号: HY-107836 纯度: 99.32%
产品使用指南

Methiothepin mesylate 是一种有效的,非选择性的 5-HT2 receptor 拮抗剂,pKd 值为 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) 和 8.99 (5-HT7),pKi 值为 8.50 (5HT2A),8.68 (5HT2B) 和 8.35 (5HT2C)。

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Methiothepin mesylate Chemical Structure

Methiothepin mesylate Chemical Structure

CAS No. : 74611-28-2

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥660 In-stock
10 mg ¥600 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Description

Methiothepin 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

pKd: 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D)[1], 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), 8.99 (5-HT7)[3]
pKi: 8.50 (5-HT2A), 8.68 (5-HT2B), 8.35 (5-HT2C)[2]

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].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (276.15 mM)

* "≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

452.65

Formula

C₂₁H₂₈N₂O₃S₃

CAS No.

74611-28-2

SMILES

CN1CCN(C2CC3=CC=CC=C3SC4=CC=C(SC)C=C24)CC1.CS(=O)(O)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
Methiothepin mesylate
目录号:
HY-107836
需求量:

Methiothepin mesylate

Cat. No.: HY-107836