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

PD-168077 maleate 

製品番号: HY-21098A 純度: 98.44%
取扱説明書

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

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PD-168077 maleate 構造式

PD-168077 maleate 構造式

CAS 番号 : 630117-19-0

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 110 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 100 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 150 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 310 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 520 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 880 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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製品説明

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

IC50 & Target

Ki: 9 nM (Dopamine D4 receptor)[1].

体外実験

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].

体内実験

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].

分子量

450.49

分子式

C₂₄H₂₆N₄O₅

CAS 番号

630117-19-0

SMILES

O=C(NCN1CCN(C2=CC=CC=C2C#N)CC1)C3=CC=CC(C)=C3.O=C(O)/C=C\C(O)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 150 mg/mL (332.97 mM; Need ultrasonic)

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.
体内:
  • 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 provided by MCE.
参考文献
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Keywords:

PD-168077PD168077PD 168077Dopamine ReceptorInhibitorinhibitorinhibit

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Inquiry Information

製品名:
PD-168077 maleate
製品番号:
HY-21098A
数量:
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