BIIE 0246 hydrochloride

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Cat.No. 7377 - BIIE 0246 hydrochloride | C49H57N11O6.HCl
Description: Potent, selective and competitive non-peptide NPY Y2 receptor antagonist; active in vivo
Alternative Names: BIIE 0246 HCl, BIIE0246 HCl
Chemical Name: N-[(1S)-4-[(Aminoiminomethyl)amino]-1-[[[2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]amino]carbonyl]butyl]-1-[2-[4-(6,11-dihydro-6-oxo-5H-dibenz[b,e]azepin-11-yl)-1-piperazinyl]-2-oxoethyl]-cyclopentaneacetamide hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (4)

Biological Activity

Potent, selective and competitive nonpeptide antagonist for the neuropeptide Y Y2 receptor (IC50 = 15 nM). Displays > 650-fold selectivity for NPY Y2 over Y1, Y4 and Y5 receptors. Active in vivo.

Technical Data

M. Wt 932.51
Formula C49H57N11O6.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
InChI Key VYCYUWJROWCJJH-MFNWJDDUSA-N
Smiles O=C(C1=C2C=CC=C1)NC3=CC=CC=C3C2N(CC4)CCN4C(CC5(CCCC5)CC(N[C@@H](CCCNC(N)=N)C(NCCN6C(N(C7=CC=CC=C7)N(C8=CC=CC=C8)C6=O)=O)=O)=O)=O.Cl

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 4.66 5

Preparing Stock Solutions

The following data is based on the product molecular weight 932.51. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.05 mM 21.45 mL 107.24 mL 214.47 mL
0.25 mM 4.29 mL 21.45 mL 42.89 mL
0.5 mM 2.14 mL 10.72 mL 21.45 mL
2.5 mM 0.43 mL 2.14 mL 4.29 mL

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References

References are publications that support the biological activity of the product.

Doods et al (1999) BIIE0246: a selective and high affinity neuropeptide Y Y2 receptor antagonist. Eur.J.Pharmacol. 384 R3 PMID: 10611450

Dumont et al (2000) BIIE0246, a potent and highly selective non-peptide neuropeptide Y Y2 receptor antagonist. Br.J.Pharmacol. 129 1075 PMID: 10725255

Malmstrom et al (2001) Vascular pharmacology of BIIE0246, the first selective non-peptide neuropeptide Y Y2 receptor antagonist, in vivo. Br.J.Pharmacol. 133 1073 PMID: 11487518


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1 Citation for BIIE 0246 hydrochloride

Citations are publications that use Tocris products. Selected citations for BIIE 0246 hydrochloride include:

Sanchez et al (2021) Photo-induced receptor confinement drives ligand-independent GPCR signaling. Science PMID: 33632896


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Literature in this Area

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