2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. PD-168077 maleate

PD-168077 maleate 

Cat. No.: HY-21098A Purity: 98.74%
COA Handling Instructions

PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.

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

PD-168077 maleate Chemical Structure

PD-168077 maleate Chemical Structure

CAS No. : 630117-19-0

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Solution
10 mM * 1 mL in DMSO USD 110 In-stock
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10 mM * 1 mL
ready for reconstitution
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Solid
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100 mg USD 880 In-stock
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Based on 1 publication(s) in Google Scholar

PD-168077 maleate Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.

IC50 & Target

D4 Receptor

 

In Vitro

PD-168077 is one of the first agents to be identified as putative selective D4 agonists. It shows >100-fold selectivity over other members of the D2-like receptor family and over their D1-like counterparts; PD-168077 shows a 20-fold selectivity over α1, and α2, a 45-fold selectivity over 5-HT1A, and a 460-fold selectivity over 5-HT2A receptors; PD-168077 evidences intrinsic activity at the D4 receptor in terms of quinpirole-like inhibition of forskolin-stimulated cAMP accumulation or stimulation of [3H]thymidine uptake? in CHO cells expressing the human D4 receptor[1]. In the PD-168077-treated cell, p-CaMKII exhibits a significantly increased clustering at synaptic sites, as indicated by the enhanced colocalization with PSD-95[2].

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

PD-168077 maleate Related Antibodies
In Vivo

PD-168077 (0.2-25.0 mg/kg) dose-dependently induces locomotion, which takes an unusual and characteristic ”shuffling” form with uncoordinated movements together with yawning, and episodes of myoclonic jerking; grooming, and rearing are reduced[1].

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

450.49

Appearance

Solid

Formula

C24H26N4O5
CAS No.
SMILES

O=C(NCN1CCN(C2=CC=CC=C2C#N)CC1)C3=CC=CC(C)=C3.O=C(O)/C=C\C(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 : 150 mg/mL (332.97 mM; Need ultrasonic)

H2O : ≥ 0.1 mg/mL (0.22 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2198 mL 11.0990 mL 22.1981 mL
5 mM 0.4440 mL 2.2198 mL 4.4396 mL
10 mM 0.2220 mL 1.1099 mL 2.2198 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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PD-168077 maleate Related Classifications

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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

PD-168077630117-19-0PD168077PD 168077Dopamine ReceptorInhibitorinhibitorinhibit

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