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Tocris/UBP 310/3621/10/10 mg

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货号: 3621/10

品牌: Tocris

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Description: GLU_K5 antagonist

Chemical Name: (S)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxy-thiophene-3-yl-methyl)-5-methylpyrimidine-2,4-dione

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

GLU_K5 kainate receptor antagonist (IC₅₀ = 130 nM); also blocks recombinant homomeric GLU_K7 receptors. Displays 12,700-fold selectivity for GLU_K5 over GLU_K6. Exhibits no activity at mGlu group I or NMDA receptors at concentrations of up to 10 μM. Apparent K_D value is 18 ± 4 nM for depression of kainate responses on the dorsal root.

Compound Libraries

UBP 310 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	353.35
Formula	C₁₄H₁₅N₃O₆S
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	902464-46-4
PubChem ID	6420160
InChI Key	ZTAZUCRXCRXNSU-VIFPVBQESA-N
Smiles	CC1=CN(C[C@@H](C(O)=O)N)C(N(CC2=C(C(O)=O)SC=C2)C1=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
Solubility	DMSO	35.34	100

Preparing Stock Solutions

The following data is based on the product molecular weight 353.35. 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	2.83 mL	14.15 mL	28.3 mL
5 mM	0.57 mL	2.83 mL	5.66 mL
10 mM	0.28 mL	1.42 mL	2.83 mL
50 mM	0.06 mL	0.28 mL	0.57 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Mayer et al (2006) Crystal structures of the kainate receptor GluR5 ligand binding core dimer with novel GluR5-selective antagonists. J.Neurosci. 26 2852 PMID: 16540562

Dolman et al (2007) Synthesis and pharmacological characterization of N³-substituted willardiine derivatives: Role of the substituent at the 5-position of the uracil ring in development of highly potent and selective GLU_K5 kainate receptor antagonists. J.Med.Chem. 50 1558 PMID: 17348638

Perrais et al (2009) Antagonism of recombinant and native GluK3-containing kainate receptors. Neuropharmacology 56 131 PMID: 18761361

Keywords: UBP 310, supplier, UBP310, kainate, receptors, antagonists, GLUK5, iGlu, ionotropic, glutamate, Kainate, Receptors, Kainate, Receptors, Tocris Bioscience

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