PD 168568
PD 168568 is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 contains an isoindolinone and is selective for the D4 receptor versus D2 and D3, with Ki values of 8.8, 1842, and 2682 nM, respectively. PD 168568 can be used for glioblastoma (GBM) research.
For research use only. We do not sell to patients.
- CAS No.: 210688-56-5
- Formula: C22H27N3O
- Molecular Weight:349.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Dopamine Receptor Isoforms
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Biological Activity
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D4 Receptor 8.8 nM (Ki) |
D2 Receptor 1842 nM (Ki) |
D3 Receptor 2682 nM (Ki) |
PD 168568 shows selectivity inhibition toward glioblastoma neural stem cells (GNS), with IC50 of 25-50 µM[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.
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Animal Model:Rat[1]
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Dosage:3 mg/kg
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Administration:Oral administration
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Result:Inhibited amphetamine (0.5 mg/kg, i.p.) stimulated locomotor activity.
Chemical Information
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CAS No. 210688-56-5
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Molecular Weight 349.47
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Formula C22H27N3O
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SMILES
O=C1NC(CCN2CCN(C3=CC=C(C)C(C)=C3)CC2)C4=C1C=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Dolma S, et al. Inhibition of Dopamine Receptor D4 Impedes Autophagic Flux, Proliferation, and Survival of Glioblastoma Stem Cells. Cancer Cell. 2016 Jun 13;29(6):859-873. [Content Brief]
[2]. Lindsley CW, et al. Return of D4 Dopamine Receptor Antagonists in Drug Discovery. J Med Chem. 2017 Sep 14;60(17):7233-7243. [Content Brief]
[3]. Belliotti TR, et al. Isoindolinone enantiomers having affinity for the dopamine D4 receptor. Bioorg Med Chem Lett. 1998 Jun 16;8(12):1499-502. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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