JNJ-5207852 dihydrochloride

Name: JNJ-5207852 dihydrochloride
Brand: MedChemExpress
SKU: HY-12190A
Rating: 4.5 (0 reviews)

Art. -Nr.: HY-12190A Reinheit: 98.49%: Data Sheet
COA

SDS
Handling Instructions
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JNJ-5207852 dihydrochloride is a selective and potent histamine H₃ receptor (H₃R) antagonist, with pK_is of 8.9, 9.24 for rat and human H₃R, respectively.

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JNJ-5207852 dihydrochloride Chemische Struktur

CAS. Nr. : 1782228-76-5

Größe	Verfügbarkeit	Menge
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
Solid
5 mg	Auf Lager	Estimated Time of Arrival: December 31
10 mg	Auf Lager	Estimated Time of Arrival: December 31
25 mg	Auf Lager	Estimated Time of Arrival: December 31
50 mg	Auf Lager	Estimated Time of Arrival: December 31
100 mg	Auf Lager	Estimated Time of Arrival: December 31
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Other Forms of JNJ-5207852 dihydrochloride:

JNJ-5207852 In-stock

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biologische Aktivität
Reinheit & Dokumentation
Verweise
Kundenbewertung

Beschreibung

JNJ-5207852 dihydrochloride is a selective and potent histamine H₃ receptor (H₃R) antagonist, with pK_is of 8.9, 9.24 for rat and human H₃R, respectively.

IC₅₀ & Target^[1]

H₃ Receptor

8.9 (pKi, for rat)

H₃ Receptor

9.24 (pKi, for human)

In Vivo

JNJ-5207852 (1-10mg/kg s.c.) increases time spent awake and decreases REM sleep and slow-wave sleep, but fails to have an effect on wakefulness or sleep in H₃ receptor knockout mice. The wake promoting effects of this H₃ receptor antagonist are not associated with hypermotility. A 4-week daily treatment of mice with JNJ-5207852 (10 mg/kg i.p.) does not lead to a change in body weight. JNJ-5207852 is extensively absorbed after oral administration and reaches high brain levels^[1].

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

Animal Model:	Male, Sprague-Dawley rats weighing 282-334 g^[1].
Dosage:	3, 10, 30 mg/kg.
Administration:	S.C.
Result:	Iincreased time spent awake and decreased REM sleep and slow-wave sleep.

Molekulargewicht

389.40

Formel

C₂₀H₃₄Cl₂N₂O

CAS. Nr.

1782228-76-5

Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.[H]Cl.N1(CCCOC2=CC=C(CN3CCCCC3)C=C2)CCCCC1

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

H₂O : 25 mg/mL (64.20 mM; Need ultrasonic)

DMSO : 7.14 mg/mL (18.34 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	2.5681 mL	12.8403 mL	25.6805 mL
5 mM	0.5136 mL	2.5681 mL	5.1361 mL
10 mM	0.2568 mL	1.2840 mL	2.5681 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner
Verdünnungsrechner

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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: ≥ 0.71 mg/mL (1.82 mM); Clear solution

This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 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: ≥ 0.71 mg/mL (1.82 mM); Clear solution

This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 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: ≥ 0.71 mg/mL (1.82 mM); Clear solution

This protocol yields a clear solution of ≥ 0.71 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 (7.1 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.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Reinheit & Dokumentation

Purity: 98.49%

Select Batch:

Data Sheet (272 KB) SDS (394 KB)

COA (245 KB) HNMR (263 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

Verweise

[1]. Barbier AJ, et al. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61. [Content Brief]

[2]. Abuhamdah RM, et al. Effects of methimepip and JNJ-5207852 in Wistar rats exposed to an open-field with and without object and in Balb/c mice exposed to a radial-arm maze. Front Syst Neurosci. 2012 Jul 16;6:54. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO / H₂O	1 mM	2.5681 mL	12.8403 mL	25.6805 mL	64.2013 mL
	5 mM	0.5136 mL	2.5681 mL	5.1361 mL	12.8403 mL
	10 mM	0.2568 mL	1.2840 mL	2.5681 mL	6.4201 mL
	15 mM	0.1712 mL	0.8560 mL	1.7120 mL	4.2801 mL
H₂O	20 mM	0.1284 mL	0.6420 mL	1.2840 mL	3.2101 mL
	25 mM	0.1027 mL	0.5136 mL	1.0272 mL	2.5681 mL
	30 mM	0.0856 mL	0.4280 mL	0.8560 mL	2.1400 mL
	40 mM	0.0642 mL	0.3210 mL	0.6420 mL	1.6050 mL
	50 mM	0.0514 mL	0.2568 mL	0.5136 mL	1.2840 mL
	60 mM	0.0428 mL	0.2140 mL	0.4280 mL	1.0700 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.