1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor Dopamine Receptor
  3. WAY-100635 maleate

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.

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WAY-100635 maleate Chemical Structure

WAY-100635 maleate Chemical Structure

CAS No. : 1092679-51-0

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10 mM * 1 mL in DMSO
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Based on 4 publication(s) in Google Scholar

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Description

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[1][2][3].

IC50 & Target[1]

D4 Receptor

 

sPLA2

8.87 (pIC50)

sPLA2

9.71 (pA2)

In Vitro

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.

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.
Molecular Weight

538.64

Formula

C29H38N4O6

CAS No.
Appearance

Solid

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)

Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8565 mL 9.2826 mL 18.5653 mL
5 mM 0.3713 mL 1.8565 mL 3.7131 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Concentration (final)

C2

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In Vivo:

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.

  • Protocol 1

    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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).
Purity & Documentation

Purity: 99.89%

References

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.

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  • 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.

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WAY-100635 maleate
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