Art. -Nr.: HY-10349

WAY-100635

14 Cited Publications

Kundenbewertung

Based on 14 publication(s) in Google Scholar

WAY-100635 is a potent and selective 5-HT_1A Receptor antagonist with a pIC₅₀ of 8.87, an apparent pA₂ of 9.71. WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC₅₀ value of 0.91 nM and K_i value of 0.39 nM. WAY-100635 has pIC₅₀ values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D₄ receptor agonist.

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Reinheit: 99.97%
CAS. Nr.: 162760-96-5
Formel: C₂₅H₃₄N₄O₂
Molecular Weight:422.56

Speicherung:

Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

WAY-100635 Chemical Structure

CAS. Nr.: 162760-96-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

D₄ Receptor

5-HT_1A Receptor

8.87 (pIC₅₀)

5-HT_1A Receptor

9.71 (pA2)

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	7.1 nM Compound: 1	Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells	[PMID: 15239661]
CHO	EC₅₀	7.1 nM Compound: 1	Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor	[PMID: 15239661]
CHO	IC₅₀	7.1 nM Compound: 4, WAY-100635	Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level	[PMID: 20443629]
HEK293-EBNA	IC₅₀	0.91 nM Compound: 1, WAY-100635	Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting	[PMID: 21520940]
JAR	IC₅₀	>4500 nM Compound: 1	Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells	[PMID: 15239661]

In Vitro

The functional properties and binding affinities of WAY-100635 are evaluated in HEK 293 cells stably expressing dopamine D_2L or D_4.4 receptors^[1].
WAY-100635 displays 940, 370, and 16 nM binding affinities at D_2L, D₃, and D_4.2 receptors, respectively. Saturation analyses demonstrat that the K_d of [³H] WAY-100635 at D_4.2 receptors is 2.4 nM. WAY-100635 is potent agonist in HEK-D_4.4 cells with EC₅₀ of 9.7 nM. WAY-100635 possesses high affinity for D_4.4 receptor (3.3 nM) ^[1].

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

In Vivo

WAY-100635 (1 mg/kg; subcutaneous injection; male Sprague-Dawley rats) treatment abolishes the reduction of the severity of abstinence signs induced by Rhodiola rosea administration in nicotine-dependent rat^[2].

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

Animal Model:

Male Sprague-Dawley rats (220-240 g)^[2]
Dosage:

1 mg/kg
Administration:

Subcutaneous injection (Pharmacokinetic study)
Result:

Reduced total abstinence score, increased immobility time and the burying behavior was increased.

Chemical Information

CAS. Nr. 162760-96-5
Appearance Solid-Liquid Mixture
Molecular Weight 422.56
Formel C₂₅H₃₄N₄O₂
Color Off-white to light yellow
SMILES

O=C(N(C1=NC=CC=C1)CCN2CCN(CC2)C3=CC=CC=C3OC)C4CCCCC4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (14)

All In Vivo Efficacy StudyRT-PCR

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Journal Impact Factor

Nat Neurosci

Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties. [Abstract]

2022 Jan;25(1):39-49. PMID: 34887590
Neuropsychopharmacology

Psilocybin improves novel object recognition in a rat model of Fragile X Syndrome through the modulation of the BDNF/TrkB signaling pathway. [Abstract]

2026 Feb 13. PMID: 41688761
Br J Pharmacol

5-HT2A receptors in the prelimbic cortex VIP-expressing interneurons: A mechanism for psychedelic-induced innate fear attenuation. [Abstract]

2026 Feb 27. PMID: 41761564
Chin Med

Shaoyao Decoction reduced T lymphocyte activation by regulating of intestinal flora and 5-hydroxytryptamine metabolism in ulcerative colitis. [Abstract]

2024 Jun 15;19(1):87. PMID: 38879471

WAY-100635 purchased from MedChemExpress. Usage Cited in: Chin Med. 2024 Jun 15;19(1):87. [Abstract]

5-HT promoted the inflammation in H9 cells. NC, negative control; 5-HT: 5-HT (10 μM) treatment; Way: 5-HT (10 μM) and Way100635 (10 μM) treatment; Tro: 5-HT (10 μM) and Tropisetron (25 μM) treatment; Way + Tro: 5-HT (10 μM), Way100635 (10 μM) and Tropisetron (25 μM) treatment.
Int J Mol Sci

Cannabidiol Attenuates Methamphetamine-Induced Autophagy in Primary Rat Neurons via the 5-HT1A/AC/cAMP/PKA/CREB Signaling Pathway. [Abstract]

2026 Jan;27(13):5677. PMID: 42449951
Int Immunopharmacol

Hypidone hydrochloride (YL-0919) protects mice from meningitis via Sigma1R-STAT1-NLRP3-GSDMD pathway. [Abstract]

2024 Feb 15:128:111524. PMID: 38232537
Neuropharmacology

Antidepressant-like activity of JZ-1201 in male rodents: a novel selective 5-HT/NE reuptake inhibitor and 5-HT1A receptor partial agonist. [Abstract]

2026 Nov 1:298:111009. PMID: 42107524
Neuropharmacology

Novel mechanism of hypidone hydrochloride (YL-0919) in Parkinson's disease: inhibiting neuronal ferroptosis by targeting the Sigma1R-PI3K-AKT-ACSL4 axis. [Abstract]

2026 Jul 1:292:110950. PMID: 41887568
iScience

Oxygen-dependent regulation of serotonin receptor 5-HT 1A in hypoxic response and flight performance in bumblebees, Bombus terrestris. [Abstract]

2025 Nov 25;28(12):114211. PMID: 41384043

WAY-100635 purchased from MedChemExpress. Usage Cited in: iScience. 2025 Nov 25;28(12):114211. [Abstract]

Experimental design for in vivo functional validation of 5-HT1A. 5-HT1A activity was inhibited by injection of 5-HT1A antagonist, WAY-100635.
Biomedicines

5-Hydroxytryptophan, a Precursor for Serotonin Synthesis, Alleviated Cognitive Dysfunction in a Mouse Model of Sepsis-Associated Encephalopathy. [Abstract]

2025 Sep 23;13(10):2319. PMID: 41153606

WAY-100635 purchased from MedChemExpress. Usage Cited in: Biomedicines. 2025 Sep 23;13(10):2319. [Abstract]

Effects of 5-HTP (10 mg/kg) and WAY100635 (1 mg/kg) on cognitive behavior and motor functions in healthy mice. The BM performance (learning and probe trials) across groups.

WAY-100635 purchased from MedChemExpress. Usage Cited in: Biomedicines. 2025 Sep 23;13(10):2319. [Abstract]

Effects of 5-HTP (10 mg/kg) and WAY100635 (1 mg/kg) on cognitive behavior and motor functions in healthy mice. NORT discrimination index across group.

WAY-100635 purchased from MedChemExpress. Usage Cited in: Biomedicines. 2025 Sep 23;13(10):2319. [Abstract]

Impact of WAY100635 pretreatment on 5-HTP's effects in LPS-induced SAE model. Performance during learning phase of BM between groups.
Psychopharmacology (Berl)

5-hydroxytryptamine 2C/1A receptors modulate the biphasic dose response of the head twitch response and locomotor activity induced by DOM in mice. [Abstract]

2024 Nov;241(11):2315-2330. PMID: 38916640
Psychopharmacology (Berl)

Contrasting effects of DOI and lisuride on impulsive decision-making in delay discounting task. [Abstract]

2022 Nov;239(11):3551-3565. PMID: 36107207
Chin J Integr Med

Combination of Geniposide and Eleutheroside B Exerts Antidepressant-like Effect on Lipopolysaccharide-Induced Depression Mice Model. [Abstract]

2021 Jul;27(7):534-541. PMID: 31784933
Cereb Cortex

A circuit from lateral hypothalamic to dorsal hippocampal dentate gyrus modulates behavioral despair in mice. [Abstract]

2024 Oct 3;34(10):bhae399. PMID: 39367727

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 66.67 mg/mL (157.78 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

2.3665 mL

11.8326 mL

23.6653 mL

5 mM

0.4733 mL

2.3665 mL

4.7331 mL

10 mM

0.2367 mL

1.1833 mL

2.3665 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. 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: ≥ 2.5 mg/mL (5.92 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.92 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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (5.92 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 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 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]. Chemel BR, et al. WAY-100635 is a potent dopamine D4 receptor agonist. Psychopharmacology (Berl). 2006 Oct;188(2):244-51. [Content Brief]

[2]. Mannucci C, et al. Serotonin involvement in Rhodiola rosea attenuation of nicotine withdrawal signs in rats. Phytomedicine. 2012 Sep 15;19(12):1117-24. [Content Brief]

[3]. Al Hussainy R, et al. Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinatedanalogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A receptor. J Med Chem. 2011 May 26;54(10):3480-91. [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

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3665 mL	11.8326 mL	23.6653 mL	59.1632 mL
	5 mM	0.4733 mL	2.3665 mL	4.7331 mL	11.8326 mL
	10 mM	0.2367 mL	1.1833 mL	2.3665 mL	5.9163 mL
	15 mM	0.1578 mL	0.7888 mL	1.5777 mL	3.9442 mL
	20 mM	0.1183 mL	0.5916 mL	1.1833 mL	2.9582 mL
	25 mM	0.0947 mL	0.4733 mL	0.9466 mL	2.3665 mL
	30 mM	0.0789 mL	0.3944 mL	0.7888 mL	1.9721 mL
	40 mM	0.0592 mL	0.2958 mL	0.5916 mL	1.4791 mL
	50 mM	0.0473 mL	0.2367 mL	0.4733 mL	1.1833 mL
	60 mM	0.0394 mL	0.1972 mL	0.3944 mL	0.9861 mL
	80 mM	0.0296 mL	0.1479 mL	0.2958 mL	0.7395 mL
	100 mM	0.0237 mL	0.1183 mL	0.2367 mL	0.5916 mL

Keywords

WAY-100635

14 Cited Publications

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WAY-100635

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Antidepressant Compound Library

5-HT Receptor Compound Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Dopamine Receptor Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Publications Citing Use of MedChemExpress (MCE) WAY-100635

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

WAY-100635

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Antidepressant Compound Library

5-HT Receptor Compound Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Dopamine Receptor Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Publications Citing Use of MedChemExpress (MCE) WAY-100635

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

WAY-100635 Related Classifications

HY-10349 Related Classifications