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

Nelotanserin  (Synonyms: APD125)

製品番号: HY-10559 純度: 99.66%
COA 取扱説明書 Technical Support

Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.

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Nelotanserin

Nelotanserin 構造式

CAS 番号 : 839713-36-9

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 110 在庫あり
Solution
10 mM * 1 mL in DMSO USD 110 在庫あり
Solid
5 mg $100 在庫あり
10 mg $150 在庫あり
25 mg $250 在庫あり
50 mg $450 在庫あり
100 mg $660 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 2 publication(s) in Google Scholar

Other Forms of Nelotanserin:

Nelotanserin 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

Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.

IC50 & Target

5-HT2A Receptor

 

5-HT2B Receptor

 

5-HT2C Receptor

 

5-HT2A Receptor

1.7 nM (IC50)

5-HT2C Receptor

79 nM (IC50)

5-HT2B Receptor

791 nM (IC50)

体外実験

Results from IP accumulation assays suggest that Nelotanserin is a potent 5-HT2A full inverse agonist (IC50=1.7 nM), a moderately potent 5-HT2C partial inverse agonist (IC50=79 nM) (maximal response was 62% of the response obtained for the reference inverse agonist clozapine), and a weak 5-HT2B inverse agonist (IC50=791 nM). Nelotanserin displays high affinity for recombinant human 5-HT2A receptors (Ki=0.35 nM), moderate affinity for human 5-HT2C receptors (Ki=100 nM), and low affinity for human 5-HT2B receptors (2000 nM) stably expressed in HEK293 cells. The results suggest that Nelotanserin has a 262-fold higher affinity for human 5-HT2A than 5-HT2C receptors and a 6610-fold higher affinity for human 5-HT2A than 5-HT2B receptors[1].

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

Nelotanserin 関連抗体
体内実験

Each compound is tested in a minimum of five rats by oral gavage with administration occurring in the middle of the inactive period, 6 h after light onset. The delta power during non-REM sleep (NREMS) is significantly different between all the analogues tested and the vehicle control. Nelotanserin (Compound 39) produces significant increases in delta power that persist for the first 4 h following dosing. Significant differences are found, however, in NREMS bout length. Nelotanserin significantly increases NREMS bout length during the first hour following dosing, and 3 does so during the second hour. In conjunction with this increased NREM bout duration, the number of NREM bouts decrease during the first hour for Nelotanserin (p<0.01) as well as for compound 15 (p<0.05)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

437.24

分子式

C18H15BrF2N4O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

COC1=C(C2=C(Br)C=NN2C)C=C(NC(NC3=C(F)C=C(F)C=C3)=O)C=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 32 mg/mL (73.19 mM; 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 2.2871 mL 11.4354 mL 22.8707 mL
5 mM 0.4574 mL 2.2871 mL 4.5741 mL
10 mM 0.2287 mL 1.1435 mL 2.2871 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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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

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体積 （開始）

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濃度 （終了）

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体積 （終了）

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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
純度とドキュメンテーション
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2871 mL 11.4354 mL 22.8707 mL 57.1768 mL
5 mM 0.4574 mL 2.2871 mL 4.5741 mL 11.4354 mL
10 mM 0.2287 mL 1.1435 mL 2.2871 mL 5.7177 mL
15 mM 0.1525 mL 0.7624 mL 1.5247 mL 3.8118 mL
20 mM 0.1144 mL 0.5718 mL 1.1435 mL 2.8588 mL
25 mM 0.0915 mL 0.4574 mL 0.9148 mL 2.2871 mL
30 mM 0.0762 mL 0.3812 mL 0.7624 mL 1.9059 mL
40 mM 0.0572 mL 0.2859 mL 0.5718 mL 1.4294 mL
50 mM 0.0457 mL 0.2287 mL 0.4574 mL 1.1435 mL
60 mM 0.0381 mL 0.1906 mL 0.3812 mL 0.9529 mL
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Nelotanserin 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:

Nelotanserin839713-36-9APD125APD 125APD-1255-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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