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

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

製品番号: HY-107836 純度: 99.36%
COA 取扱説明書 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).

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Methiothepin mesylate

Methiothepin (mesylate) 構造式

CAS 番号 : 74611-28-2

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 40 在庫あり
Solution
10 mM * 1 mL in DMSO USD 40 在庫あり
Solid
5 mg $37 在庫あり
10 mg $60 在庫あり
50 mg   お問い合わせ  
100 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 2 publication(s) in Google Scholar

Other Forms of Methiothepin mesylate:

Methiothepin (mesylate) 関連抗体

Top Publications Citing Use of Products

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

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製品説明

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 1
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
56 1
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
56 1
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 1
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]
CHO-K1 IC50
71 1
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]
CHO-K1 IC50
71 1
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]
体外実験

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) 関連抗体
分子量

452.65

分子式

C21H28N2O3S3
CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

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

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
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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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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

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体積 （終了）

V2

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
純度とドキュメンテーション

純度: 99.36%

COA (253 KB) HNMR (246 KB) RP-HPLC (223 KB)

取扱説明書 (2659 KB)
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 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

  • 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:

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

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製品名:
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