SB 242084 dihydrochloride

Name: SB 242084 dihydrochloride
Brand: MedChemExpress
SKU: HY-13409A
Rating: 5.0 (6 reviews)

製品番号: HY-13409A 純度: 98.12%: Data Sheet SDS COA 取扱説明書
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SB 242084 dihydrochloride is a selective, competitive and high-affinity (pK_i=9.0) 5-HT_2C receptor antagonist (crosses the blood-brain barrier). SB 242084 dihydrochloride increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 dihydrochloride also increases mitochondrial gene expression and oxidative metabolism via 5-HT_2A receptor. SB 242084 dihydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

SB 242084 dihydrochloride 構造式

CAS 番号 : 1049747-87-6

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 116	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 116	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$113	在庫あり	Estimated Time of Arrival: December 31
10 mg	$158	在庫あり	Estimated Time of Arrival: December 31
25 mg	$300	在庫あり	Estimated Time of Arrival: December 31
50 mg	$490	在庫あり	Estimated Time of Arrival: December 31
100 mg	$760	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 6 publication(s) in Google Scholar

Other Forms of SB 242084 dihydrochloride:

SB 242084 在庫あり
SB 242084 monohydrochloride お問い合わせ
SB 242084 dihydrochloride (Standard) お問い合わせ

顧客検証

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

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

5-HT_2A Receptor

5-HT_2C Receptor

9.0 (pKi)

体外実験

SB 242084 dihydrochloride (100 nM; 45 min) exhibits antagonism of the 5-HT stimulated increase in phosphatidylinositol hydrolysis at the human 5-HT_2C receptor in SH-SY5Y cells^[1].
SB 242084 dihydrochloride (1-100 nM; 24 h) increases RPTC respiration and PGC-1α mRNA expression in RPTC^[2].

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

Cell Viability Assay^[1]

Cell Line:	SH-SY5Y cells
Concentration:	100 nM
Incubation Time:	45 min
Result:	Antagonized 5-HT induced concentration-related increase in PI hydrolysis.

RT-PCR^[2]

Cell Line:	RPTC cells
Concentration:	1-100 nM
Incubation Time:	24 h
Result:	Increased FCCP-uncoupled respiration and PGC-1α mRNA expression.

体内実験

SB 242084 dihydrochloride (0.1-1 mg/kg; i.p.; single; 20 min pre-test) improves the behavior of rats in social interaction tests^[1].
SB 242084 dihydrochloride (5 mg/kg; i.p.; single; 20 min pre-test) improves mCPP-induced hypophagia in rats^[1].
SB 242084 dihydrochloride (5, 10 mg/kg; i.p.; single) increases the levels of basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens of rats^[3].
SB 242084 dihydrochloride (160-640 μg/kg; i.v.; single) dose-dependently and significantly increases the basal firing rate of VTA (ventral tegmental area) dopaminergic neurons, and the bursting activity is also enhanced in the same area, in vivo^[3].

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

Animal Model:	Male Sprague-Dawley (CD) rats^[1].
Dosage:	0.1-1 mg/kg
Administration:	Intraperitoneal injection; single; 20 min pre-test
Result:	Significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliartest box.

Animal Model:	Male Sprague-Dawley (CD) rats(mCPP-induced hypophagia model)^[1].
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; single; 20 min pre-test
Result:	Significantly reduced the amount of food consumed by 23 h food-deprivedrats over a 1hr test period from the time of food presentation.

Animal Model:	Rats^[2].
Dosage:	5, 10 mg/kg
Administration:	Intraperitoneal injection; single
Result:	Significantly increased basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens.

分子量

467.78

分子式

C₂₁H₂₁Cl₃N₄O₂

CAS 番号

1049747-87-6

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N1CCC2=C1C=C(Cl)C(C)=C2)NC3=CC=C(OC4=CC=CN=C4C)N=C3.[H]Cl.[H]Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

-20°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (213.78 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	2.1378 mL	10.6888 mL	21.3776 mL
5 mM	0.4276 mL	2.1378 mL	4.2755 mL
10 mM	0.2138 mL	1.0689 mL	2.1378 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 (stored under nitrogen, 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)

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）

体内:

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: ≥ 5 mg/mL (10.69 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (10.69 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (10.69 mM); Clear solution

This protocol yields a clear solution of ≥ 5 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 98.12%

Select Batch:

データシート (285 KB) SDS (393 KB)

COA (258 KB) HNMR (141 KB) RP-HPLC (273 KB) MS (312 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Kennett GA, et al. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20. [Content Brief]

[2]. Harmon JL, et al. 5-HT2 Receptor Regulation of Mitochondrial Genes: Unexpected Pharmacological Effects of Agonists and Antagonists. J Pharmacol Exp Ther. 2016 Apr;357(1):1-9. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.1378 mL	10.6888 mL	21.3776 mL	53.4439 mL
	5 mM	0.4276 mL	2.1378 mL	4.2755 mL	10.6888 mL
	10 mM	0.2138 mL	1.0689 mL	2.1378 mL	5.3444 mL
	15 mM	0.1425 mL	0.7126 mL	1.4252 mL	3.5629 mL
	20 mM	0.1069 mL	0.5344 mL	1.0689 mL	2.6722 mL
	25 mM	0.0855 mL	0.4276 mL	0.8551 mL	2.1378 mL
	30 mM	0.0713 mL	0.3563 mL	0.7126 mL	1.7815 mL
	40 mM	0.0534 mL	0.2672 mL	0.5344 mL	1.3361 mL
	50 mM	0.0428 mL	0.2138 mL	0.4276 mL	1.0689 mL
	60 mM	0.0356 mL	0.1781 mL	0.3563 mL	0.8907 mL
	80 mM	0.0267 mL	0.1336 mL	0.2672 mL	0.6680 mL
	100 mM	0.0214 mL	0.1069 mL	0.2138 mL	0.5344 mL