WAY-100635 maleate
Based on 12 publication(s) in Google Scholar
WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 maleate has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 maleate is also a potent dopamine D4 receptor agonist.
For research use only. We do not sell to patients.
- Purity: 99.57%
- CAS No.: 1092679-51-0
- Formula: C29H38N4O6
- Molecular Weight:538.64
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
GPCR/G Protein Compound Library
HY-L006
-
Neuronal Signaling Compound Library
HY-L013
-
Anti-diabetic Compound Library
HY-L040
-
Neurotransmitter Receptor Compound Library
HY-L062
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Anti-Parkinson's Disease Compound Library
HY-L085
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Antidepressant Compound Library
HY-L108
-
5-HT Receptor Compound Library
HY-L121
-
Human Metabolite Library
HY-L123
-
Coagulation and Anti-coagulation Compound Library
HY-L136
-
Heterocyclic Compound Library
HY-L138
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Dopamine Receptor Compound Library
HY-L165
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Lactylation Compound Library
HY-L249
Publications Citing Use of MedChemExpress (MCE) WAY-100635 maleate
More- Nat Neurosci. 2022 Jan;25(1):39-49. [Abstract]
- Br J Pharmacol. 2026 Feb 27. [Abstract]
- Neuropsychopharmacology. 2026 Feb 13. [Abstract]
- Chin Med. 2024 Jun 15;19(1):87. [Abstract]
- Int Immunopharmacol. 2024 Feb 15:128:111524. [Abstract]
- Neuropharmacology. 2026 Jul 1:292:110950. [Abstract]
- iScience. 2025 Nov 25;28(12):114211. [Abstract]
- Biomedicines. 2025 Sep 23;13(10):2319. [Abstract]
- Psychopharmacology (Berl). 2024 Nov;241(11):2315-2330. [Abstract]
- Psychopharmacology (Berl). 2022 Nov;239(11):3551-3565. [Abstract]
- Cereb Cortex. 2024 Oct 3;34(10):bhae399. [Abstract]
- Chin J Integr Med. 2021 Jul;27(7):534-541. [Abstract]
Customer Validation & Images
-
In Vivo Efficacy Study
-
In Vivo Efficacy Study
-
In Vivo Efficacy Study
-
In Vivo Efficacy Study
-
RT-PCR
All 5-HT Receptor Isoforms
MoreAll Dopamine Receptor Isoforms
More
Biological Activity
|
D4 Receptor |
5-HT1A Receptor |
sPLA2 8.87 (pIC50) |
sPLA2 9.71 (pA2) |
The functional properties and binding affinities of WAY-100635 are evaluated in HEK 293 cells stably expressing dopamine D2L or D4.4 receptors[1].
WAY-100635 displays 940, 370, and 16 nM binding affinities at D2L, D3, and D4.2 receptors, respectively. Saturation analyses demonstrat that the Kd of [3H] WAY-100635 at D4.2 receptors is 2.4 nM. WAY-100635 is potent agonist in HEK-D4.4 cells with EC50 of 9.7 nM. WAY-100635 possesses high affinity for D4.4 receptor (3.3 nM) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 No. 1092679-51-0
-
Appearance Solid
-
Molecular Weight 538.64
-
Formula C29H38N4O6
-
Color White to off-white
-
SMILES
OC(/C=C\C(O)=O)=O.COC1=C(N2CCN(CC2)CCN(C3=CC=CC=N3)C(C4CCCCC4)=O)C=CC=C1
-
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)
Publications (12)
-
Journal Impact Factor
-
Most Recent
-
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 -
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 -
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 -
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 maleate 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 Immunopharmacol
Hypidone hydrochloride (YL-0919) protects mice from meningitis via Sigma1R-STAT1-NLRP3-GSDMD pathway. [Abstract]2024 Feb 15:128:111524. PMID: 38232537 -
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 maleate 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 maleate 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 maleate 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 maleate 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 -
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 -
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
Solvent & Solubility
DMSO : ≥ 250 mg/mL (464.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 25 mg/mL (46.41 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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.
* 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.
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.
* 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: PBS
Solubility: 25 mg/mL (46.41 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Purity & Documentation
-
Data Sheet (280 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[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]
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.8565 mL | 9.2826 mL | 18.5653 mL | 46.4132 mL |
| 5 mM | 0.3713 mL | 1.8565 mL | 3.7131 mL | 9.2826 mL | |
| 10 mM | 0.1857 mL | 0.9283 mL | 1.8565 mL | 4.6413 mL | |
| 15 mM | 0.1238 mL | 0.6188 mL | 1.2377 mL | 3.0942 mL | |
| 20 mM | 0.0928 mL | 0.4641 mL | 0.9283 mL | 2.3207 mL | |
| 25 mM | 0.0743 mL | 0.3713 mL | 0.7426 mL | 1.8565 mL | |
| 30 mM | 0.0619 mL | 0.3094 mL | 0.6188 mL | 1.5471 mL | |
| 40 mM | 0.0464 mL | 0.2321 mL | 0.4641 mL | 1.1603 mL | |
| DMSO | 50 mM | 0.0371 mL | 0.1857 mL | 0.3713 mL | 0.9283 mL |
| 60 mM | 0.0309 mL | 0.1547 mL | 0.3094 mL | 0.7736 mL | |
| 80 mM | 0.0232 mL | 0.1160 mL | 0.2321 mL | 0.5802 mL | |
| 100 mM | 0.0186 mL | 0.0928 mL | 0.1857 mL | 0.4641 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.
Powered by Bioz