JNJ-37822681 dihydrochloride

Name: JNJ-37822681 dihydrochloride
Brand: MedChemExpress
SKU: HY-111066A
Rating: 4.5 (0 reviews)

製品番号: HY-111066A 純度: 98.69%: Data Sheet SDS COA 取扱説明書
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JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D₂ receptor antagonist with a moderate binding affinity for the dopamine D_2L receptor (K_i =158 nM), which has potential for the treatment of schizophrenia and bipolar disorder.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。

JNJ-37822681 dihydrochloride 構造式

CAS 番号 : 2108806-02-4

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
>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 44	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 44	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$40	在庫あり	Estimated Time of Arrival: December 31
10 mg	$60	在庫あり	Estimated Time of Arrival: December 31
25 mg	$100	在庫あり	Estimated Time of Arrival: December 31
50 mg	$150	在庫あり	Estimated Time of Arrival: December 31
100 mg	$230	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 0 publication(s) in Google Scholar

Other Forms of JNJ-37822681 dihydrochloride:

JNJ-37822681 dihydrochloride (Standard) 在庫あり
JNJ-37822681 お問い合わせ

Dopamine 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

Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ 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

Ki: 158 nM (D₂)^[1]

体内実験

JNJ-37822681 (0.0025-40 mg/kg; i.h.; once) blocks D₂ receptors in rat brain at relatively low doses with an ED₅₀ value of 0.39 mg/kg and has effective in animal models of psychosis^[2].
JNJ-37822681 (0.01-2.5 mg/kg; i.h.; once) induces minimal prolactin release at the lowest doses required for central D₂ receptor blockade^[2].

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

Animal Model:	Female Sprague-Dawley rats with apomorphine-induced, d-amphetamine-induced, or phencyclidine-induced^[2]
Dosage:	0.0025-40 mg/kg
Administration:	Subcutaneous injection; once
Result:	Inhibited of D-amphetamine-induced hyperlocomotion with an ED₅₀ value of 1.0 mg/kg. Inhibited of apomorphine-induced stereotypy with an ED₅₀ value of 0.19 mg/kg. Inhibited of phencyclidine-induced hyperlocomotion with an ED₅₀ value of 4.7 mg/kg.

Animal Model:	Female Sprague-Dawley rats^[2]
Dosage:	0.01, 0.02, 0.04, 0.08, 0.16, 0.31, 0.63, 1.25, and 2.5 mg/kg
Administration:	Subcutaneous injection; once
Result:	Increased prolactin release in a dose-dependent manner.

臨床実験

分子量

445.26

分子式

C₁₇H₁₉Cl₂F₅N₄

CAS 番号

2108806-02-4

Appearance

Solid

Color

White to off-white

SMILES

FC(C1=NN=C(NC2CCN(CC3=CC=C(F)C(F)=C3)CC2)C=C1)(F)F.Cl.Cl

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 : 33.33 mg/mL (74.86 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	2.2459 mL	11.2294 mL	22.4588 mL
5 mM	0.4492 mL	2.2459 mL	4.4918 mL
10 mM	0.2246 mL	1.1229 mL	2.2459 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)

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: ≥ 2.5 mg/mL (5.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (sealed storage, 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: 98.69%

Select Batch:

データシート (273 KB) SDS (252 KB)

COA (246 KB) HNMR (140 KB) LCMS (100 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Langlois X, et, al. Pharmacology of JNJ-37822681, a specific and fast-dissociating D2 antagonist for the treatment of schizophrenia. J Pharmacol Exp Ther. 2012 Jul;342(1):91-105. [Content Brief]

[2]. de Waal EJ, et, al. Differential responses to JNJ-37822681, a specific and fast dissociating dopamine D2 receptor antagonist, in cynomolgus monkey and Sprague-Dawley rat general toxicology studies: clinical observations, prolactin levels, mammary histopat [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.2459 mL	11.2294 mL	22.4588 mL	56.1470 mL
	5 mM	0.4492 mL	2.2459 mL	4.4918 mL	11.2294 mL
	10 mM	0.2246 mL	1.1229 mL	2.2459 mL	5.6147 mL
	15 mM	0.1497 mL	0.7486 mL	1.4973 mL	3.7431 mL
	20 mM	0.1123 mL	0.5615 mL	1.1229 mL	2.8073 mL
	25 mM	0.0898 mL	0.4492 mL	0.8984 mL	2.2459 mL
	30 mM	0.0749 mL	0.3743 mL	0.7486 mL	1.8716 mL
	40 mM	0.0561 mL	0.2807 mL	0.5615 mL	1.4037 mL
	50 mM	0.0449 mL	0.2246 mL	0.4492 mL	1.1229 mL
	60 mM	0.0374 mL	0.1872 mL	0.3743 mL	0.9358 mL