JNJ-18038683

Cat. No.: HY-19889 Purity: 99.76%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

JNJ-18038683 Chemical Structure

CAS No. : 851376-05-1

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 105	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 105	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 95	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 170	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Description

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

pKi: 8.19 (rat 5-HT₇ receptor), 8.20 (human 5-HT₇ receptor)^[1].

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

Molecular Weight

529.97

Formula

C₂₆H₂₈ClN₃O₇

CAS No.

851376-05-1

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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: ≥ 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.
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 (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.
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 (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

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.

Purity & Documentation

Purity: 99.76%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (252 KB) LCMS (269 KB)

Handling Instructions (2659 KB)

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].

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].

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

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

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:

JNJ-18038683851376-05-1JNJ18038683JNJ 18038683Inhibitorinhibitorinhibit

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