索取文献 | Tocris 生物科学,Tocris/GS 39783/2001/50/50 mg-蚂蚁淘生物

Description: Positive modulator at GABA_B receptors Chemical Name: N,N\'-Dicyclopentyl-2-(methylthio)-5-nitro-4,6-pyrimidinediamine Purity: ≥98% (HPLC) Biological Activity Technical Data Solubility Calculators DatasheetsReferences

Biological Activity

Positive allosteric modulator of GABA_B receptor function. Potentiates the effects of GABA on [³⁵S]GTPγS binding at recombinant and native GABA_B receptors (EC₅₀ values are 2.1 and 3.1μM respectively). Decreases cocaine self-administration, blocks the rewarding properties of nicotine and produces anxiolytic-like activity without the side effects associated with baclofen or benzodiazepines.

Technical Data

M. Wt	337.44
Formula	C₁₅H₂₃N₅O₂S
Storage	Store at RT
Purity	≥98% (HPLC)
CAS Number	39069-52-8
PubChem ID	6604928
InChI Key	GSGVDKOCBKBMGG-UHFFFAOYSA-N
Smiles	CSC1=NC(NC2CCCC2)=C(C(NC2CCCC2)=N1)[N+]([O-])=O

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	3.37	10
ethanol	1.69	5

Preparing Stock Solutions

The following data is based on the product molecular weight 337.44. 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	2.96 mL	14.82 mL	29.63 mL
5 mM	0.59 mL	2.96 mL	5.93 mL
10 mM	0.3 mL	1.48 mL	2.96 mL
50 mM	0.06 mL	0.3 mL	0.59 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet Safety Datasheet Select another language: English German French Spanish View SDS

References

References are publications that support the products\' biological activity.

Urwyler et al (2003) N,N\'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of γ-aminobutyric acid_B receptor function. J.Pharmacol.Exp.Ther. 307 322 PMID: 12954816

Cryan et al (2004) Behavioral characterization of the novel GABA_B receptor-positive modulator GS39783 (N,N\'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine: anxiolytic-like activity without side effects associated with baclofen or benzo J.Pharmacol.Exp.Ther. 310 952 PMID: 15113848

Mombereau et al (2007) GABA_B receptor-positive modulation-induced blockade of the rewarding effects of nicotine is associated with a reduction in nucleus accumbens ΔFosB accumulation. J.Pharmacol.Exp.Ther. 321 172 PMID: 17215447

Keywords: GS 39783, supplier, Positive, modulators, GABAB, receptors, GS39783, GABAB, Receptors, GABAB, Receptors, Tocris Bioscience