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Tocris/PG 01037 dihydrochloride/3887/10/10 mg

价格: ¥2268.00 市场价: 3780.00

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货号: 3887/10

品牌: Tocris

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Description: D₃ receptor selective antagonist

Chemical Name: N-[(2E)-4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]-2-buten-1-yl]-4-(2-pyridyl)-benzamide dihydrochloride

Purity: ≥98%

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Dopamine D₃ receptor antagonist; 133-fold selective for D₃ over D₂ receptors in vitro (K_i values are 0.70, 93.3 and 375 nM for D₃, D₂ and D₄ receptors respectively). Attenuates abnormal involuntary movements associated with L-DOPA (Cat. No. 3788) in rat models of Parkinson's disease. Inhibits the effects of methamphetamine; attenuates drug-induced behaviors in vivo.

Technical Data

M. Wt	554.34
Formula	C₂₆H₂₆Cl₂N₄O.2HCl
Storage	Desiccate at +4°C
Purity	≥98%
CAS Number	675599-62-9
PubChem ID	90488894
InChI Key	DACFFMAXBWGOKQ-CZEFNJPISA-N
Smiles	ClC(C(Cl)=CC=C4)=C4N(CC3)CCN3C/C=C/CNC(C1=CC=C(C2=NC=CC=C2)C=C1)=O.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	55.43	100
	water	11.09	20mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 554.34. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.8 mL	9.02 mL	18.04 mL
5 mM	0.36 mL	1.8 mL	3.61 mL
10 mM	0.18 mL	0.9 mL	1.8 mL
50 mM	0.04 mL	0.18 mL	0.36 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Grundt et al (2005) Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor. J.Med.Chem. 48 839 PMID: 15689168

Grundt et al (2007) Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents. J.Med.Chem. 50 4135 PMID: 17672446

Kumar et al (2009) Evaluation of the D3 dopamine receptor selective antagonist PG01037 on L-dopa-dependent abnormal involuntary movements in rats. Neuropharmacology 56 944 PMID: 19371585

Mason et al (2010) Characterization of the transport, metabolism, and pharmacokinetics of the dopamine D3 receptor-delective fluorenyl-and 2-pyridylphenyl amides developed for treatment of psychostimulant abuse. J.Pharm.Exp.Ther. 333 854 PMID:

Keywords: PG 01037 dihydrochloride, supplier, PG01037, dopamine, receptors, D3, antagonists, dopaminergic, parkinsons, antiparkinsonian, parkinson's, D3, Receptors, D3, Receptors, Tocris Bioscience

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