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

WAY-100635 Maleate 

Cat. No.: HY-10349A Purity: >98.0%
Handling Instructions

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.

WAY-100635 Maleate Chemical Structure

WAY-100635 Maleate Chemical Structure

CAS No. : 1092679-51-0

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Based on 1 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]

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].

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].

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.

1092679-51-0

SMILES

O=C(O)/C=C\C(O)=O.O=C(N(C1=NC=CC=C1)CCN2CCN(CC2)C3=CC=CC=C3OC)C4CCCCC4.[1:1]

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 250 mg/mL (464.13 mM)

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
10 mM 0.1857 mL 0.9283 mL 1.8565 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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WAY-100635 Maleate
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HY-10349A
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