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Tocris/GSK 1562590 hydrochloride/5110/10/10 mg

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货号: 5110/10

品牌: Tocris

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Description: High affinity, selective urotensin II (UT) receptor antagonist

Chemical Name: N-[(1R)-1-[3'-(Aminocarbonyl)[1,1'-biphenyl]-4-yl]-2-(1-pyrrolidinyl)ethyl]-6,7-dichloro-2,3-dihydro-N-methyl-3-oxo-4H-1,4-benzoxazine-4-acetamide hydrochloride

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

High affinity and selective urotensin II (UT) receptor antagonist (pK_i values are 9.14, 9.28, 9.34, 9.64 and 9.66 at monkey, human, mouse, cat and rat recombinant receptors respectively). Exhibits selectivity for UT receptors over a range of GPCRs, ion channels, enzymes and neurotransmitter transporters. Supresses human urotensin-II (hU-II)-induced contraction of isolated rat aorta in vitro and ex vivo. Inhibits the hU-II-induced increase in mean blood pressure in vivo. Orally active.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Compound Libraries

GSK 1562590 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	617.95
Formula	C₃₀H₃₀Cl₂N₄O₄.HCl
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	1003878-07-6
PubChem ID	46909864
InChI Key	XTVXEMMIPYMBLL-SNYZSRNZSA-N
Smiles	NC(C1=CC=CC(C2=CC=[C@@]([C@@H](N(C(CN4C(C=C(Cl)C(Cl)=C5)=C5OCC4=O)=O)C)CN3CCCC3)C=C2)=C1)=O.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
Solubility	DMSO	61.8	100

Preparing Stock Solutions

The following data is based on the product molecular weight 617.95. 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	1.62 mL	8.09 mL	16.18 mL
5 mM	0.32 mL	1.62 mL	3.24 mL
10 mM	0.16 mL	0.81 mL	1.62 mL
50 mM	0.03 mL	0.16 mL	0.32 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Behm et al (2010) GSK1562590, a slowly dissociating urotensin-II receptor antagonist, exhibits prolonged pharmacodynamic activity ex vivo. Br.J.Pharmacol. 161 207 PMID: 20718751

Keywords: GSK 1562590 hydrochloride, supplier, GSK1562590, hydrochloride, high, affinity, selective, urotensin-II, receptors, antagonists, UT, hU-II, orally, active, peptides, Urotensin-II, Receptors, Urotensin-II, Receptors, Tocris Bioscience

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