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Tocris/PSB 11 hydrochloride/2012/50/50 mg

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货号: 2012/50

品牌: Tocris

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Description: Potent, selective hA₃ receptor antagonist/inverse agonist

Chemical Name: (8R)-8-Ethyl-1,4,7,8-tetrahydro-4-5H-imidazo[2,1-i]purin-5-one hydrochloride

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent and selective antagonist for the human adenosine A₃ receptor, with low affinity for the rat A₃ receptor (K_i values are 2.3 and > 10000 nM respectively). Displays > 1000-fold selectivity over human A₁ and A_2A receptors (K_i values are 4.1 and 3.3 μM respectively) and > 180-fold selectivity over rat A₁, rat A_2A and mouse A_2B receptors. Acts as an inverse agonist in the [³⁵S]GTPγS binding assay in hA₃-CHO cells (IC₅₀ = 36 nM).

Compound Libraries

PSB 11 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	331.8
Formula	C₁₆H₁₇N₅O.HCl
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	453591-58-7
PubChem ID	16759152
InChI Key	JAUSHKIWPLHBCN-RFVHGSKJSA-N
Smiles	Cl[H].CC[C@@H]1CN2C(=N1)C1=C(N=C(N1)C1=CC=CC=C1)N(C)C2=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
Solubility	DMSO	5.91	20mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 331.8. 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	3.01 mL	15.07 mL	30.14 mL
5 mM	0.6 mL	3.01 mL	6.03 mL
10 mM	0.3 mL	1.51 mL	3.01 mL
50 mM	0.06 mL	0.3 mL	0.6 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Muller et al (2002) Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A_2A- and A₃-adenosine receptor antagonists. J.Med.Chem. 45 3440 PMID: 12139454

Muller (2003) Medicinal chemistry of adenosine A₃ receptor ligands. Curr.Top.Med.Chem. 3 445 PMID: 12570761

Ozola et al (2003) 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at human A₃ adenosine receptors. Bioorg.Med.Chem. 11 347 PMID: 12517430

Keywords: PSB 11 hydrochloride, supplier, Potent, selective, human, A3, receptor, antagonists, inverse, agonists, Receptors, adenosines, PSB11, hydrochloride, Adenosine, A3, Receptors, Adenosine, A3, Receptors, Tocris Bioscience

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