Art. -Nr.: HY-19889

JNJ-18038683

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT₇) receptor antagonist, with pK_is of 8.19, 8.20 for rat and human 5-HT₇ in HEK293 cells, respectively.

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Reinheit: 98.31%
CAS. Nr.: 851376-05-1
Formel: C₂₆H₂₈ClN₃O₇
Molecular Weight:529.97

Speicherung:

4°C, sealed storage, away from moisture

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

JNJ-18038683 Chemical Structure

CAS. Nr.: 851376-05-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT₇) receptor antagonist, with pK_is of 8.19, 8.20 for rat and human 5-HT₇ in HEK293 cells, respectively.

IC₅₀ & Target^[1]

Rat 5-HT₇ Receptor

8.19 (pKi, in HEK293 cells )

5-HT₇ Receptor

Human 5-HT₇ Receptor

8.20 (pKi, in HEK293 cells )

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

JNJ-18038683 displaced, with high affinity, specific [³H]5-CT binding sites from rat and human 5-HT₇ receptor express in HEK293 cells (pK_i=8.19±0.02 and 8.20±0.01, respectively). Similar values are obtained on the native 5-HT₇ in membranes from rat thalamus (pK_i=8.50±0.20). Hill slope values are close to unity, suggesting one-site competitive binding. Antagonist potency of JNJ-18038683 is determined by the measurement of adenylate cyclase activity in HEK293 cells expressing the human or rat 5-HT₇ receptor. 5-HT stimulates adenylyl cyclase activity in rat and human 5-HT₇/HEK293 cells with a pEC₅₀ of 8.09 and 8.12, respectively. JNJ-18038683 produces a concentration-dependent decrease of 5-HT (100 nM)-stimulated adenylyl cyclase. The pK_B values determined for JNJ-18038683 are in good agreement with the corresponding K_i values determined from [³H]5-CT binding studies^[1].

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

In Vivo

JNJ-18038683 dose-dependently suppresses REM sleep mainly during the first 4 h after the treatment. The duration of REM sleep is significantly decreased from the dose of 1 mg/kg onward (P<0.05) during the first 4 h after oral administration. Concomitantly, the REM sleep latency tends to be prolonged in a dose-related manner with a significant increase in REM latency occurring only at the highest dose tested (10 mg/kg; P<0.05). These alterations in REM sleep seem to be state-specific. A separate study is conducted to determine whether repeated administration of JNJ-18038683 for 7 days would result in an adaptation of the EEG sleep response in particular on REM sleep in rats during the course of the treatment and after its discontinuation. JNJ-18038683 is administered for 7 consecutive days (1 mg/kg s.c. per day) at 2 h into the light phase. On the first day of treatment, JNJ-18038683 produces a significant decrease in the time spent in REM sleep during the first 8 h after the injection and a prolongation of the REM sleep latency. The REM sleep latency is increased during the 7-day repeated treatment and is normalized on the first recovery day after cessation of treatment. The significant decrease in REM sleep time is maintained during the 7-day repeated treatment, with a rebound occurring on the first recovery day after treatment discontinuation. The NREM sleep latency and the total NREM sleep time are not affected during the entire treatment^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 851376-05-1
Appearance Solid
Molecular Weight 529.97
Formel C₂₆H₂₈ClN₃O₇
Color White to off-white
SMILES

ClC1=CC=C(C2=NN(CC3=CC=CC=C3)C4=C2CCNCC4)C=C1.O=C(CC(C(O)=O)(O)CC(O)=O)O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Publications (1)

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Journal Impact Factor

J Physiol

5-HT7 antagonists confer analgesia via suppression of neurotrophin overproduction in submucosal nerves of mouse models with visceral hypersensitivity. [Abstract]

2025 Sep;603(17):4723-4745. PMID: 40757652

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 200 mg/mL (377.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8869 mL

9.4345 mL

18.8690 mL

5 mM

0.3774 mL

1.8869 mL

3.7738 mL

10 mM

0.1887 mL

0.9434 mL

1.8869 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (9.43 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (9.43 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (9.43 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[1]

HEK-293 cells stably expressing the rat 5-HT₇ receptor are preincubated for 10 min with seven concentrations of JNJ-18038683 (10 μM-100 pM) followed by incubation with 100 nM of the agonist (5-HT). cAMP measurements are determined. SB-2699970 is used as the reference compound₇receptor^[1].

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

Animal Administration^[1]

Mice^[1]
Rat telemetry experiments are performed. In brief, telemetric devices are implanted in the peritoneal cavity of rats. After a 7-day recovery period, body temperature is measured noninvasively by radiotelemetry. On the day of the experiment, the baseline is monitored for 60 min before drug injection. Rat core temperature is continuously recorded, before and after injection, and averaged over each 2-min collection period. JNJ-18038683 (0.09, 0.9, and 9.0 mg/kg) is administered orally 6 h before 5-CT (0.1 mg/kg, i.p.) administration or intraperitoneally (0.027, 0.09, 0.18, 0.27, and 0.9 mg/kg) 20 min before 5-CT (0.1 mg/kg i.p.) administration (n=5 in each group). Change in core body temperature is calculated for all animals by comparing baseline before dosing to the minimal temperature reached after drug administration^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Bonaventure P, et al. Translational evaluation of JNJ-18038683, a 5-hydroxytryptamine type 7 receptor antagonist, on rapid eye movement sleep and in major depressive disorder. J Pharmacol Exp Ther. 2012 Aug;342(2):429-40. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8869 mL	9.4345 mL	18.8690 mL	47.1725 mL
	5 mM	0.3774 mL	1.8869 mL	3.7738 mL	9.4345 mL
	10 mM	0.1887 mL	0.9434 mL	1.8869 mL	4.7172 mL
	15 mM	0.1258 mL	0.6290 mL	1.2579 mL	3.1448 mL
	20 mM	0.0943 mL	0.4717 mL	0.9434 mL	2.3586 mL
	25 mM	0.0755 mL	0.3774 mL	0.7548 mL	1.8869 mL
	30 mM	0.0629 mL	0.3145 mL	0.6290 mL	1.5724 mL
	40 mM	0.0472 mL	0.2359 mL	0.4717 mL	1.1793 mL
	50 mM	0.0377 mL	0.1887 mL	0.3774 mL	0.9434 mL
	60 mM	0.0314 mL	0.1572 mL	0.3145 mL	0.7862 mL
	80 mM	0.0236 mL	0.1179 mL	0.2359 mL	0.5897 mL
	100 mM	0.0189 mL	0.0943 mL	0.1887 mL	0.4717 mL

Keywords

JNJ-18038683

1 Cited Publications

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JNJ-18038683

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Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

JNJ-18038683

Anti-COVID-19 Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Targeted Diversity Library

5-HT Receptor Compound Library

Coagulation and Anti-coagulation Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) JNJ-18038683

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

JNJ-18038683 Related Classifications

HY-19889 Related Classifications