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Submit ReviewBIIE 0246 hydrochloride
Description: Potent, selective and competitive non-peptide NPY Y2 receptor antagonist; active in vivo
Alternative Names: BIIE 0246 2HCl,BIIE0246 2HCl
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 dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity for BIIE 0246 hydrochloride
BIIE 0246 hydrochloride is a 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 for BIIE 0246 hydrochloride
| M. Wt | 968.98 |
| Formula | C49H57N11O6.2HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 246146-31-6 |
| InChI Key | UESZCTPNTRZXHQ-SICTUBFJSA-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.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 for BIIE 0246 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 96.9 | 100 |
Preparing Stock Solutions for BIIE 0246 hydrochloride
The following data is based on the product molecular weight 968.98. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.03 mL | 5.16 mL | 10.32 mL |
| 5 mM | 0.21 mL | 1.03 mL | 2.06 mL |
| 10 mM | 0.1 mL | 0.52 mL | 1.03 mL |
| 50 mM | 0.02 mL | 0.1 mL | 0.21 mL |
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Product Datasheets for BIIE 0246 hydrochloride
References for BIIE 0246 hydrochloride
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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Keywords: BIIE 0246 hydrochloride, BIIE 0246 hydrochloride supplier, BIIE0246, dihydrochloride, 2HCl, Potent, selective, non-peptide, NPY, Y2, antagonists, Neuropeptide, Y, Receptors, neuropeptides, BIIE, 0246, 7377, Tocris Bioscience
2 Citations 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 371 PMID: 33632896
Yue et al (2022) mTOR-neuropeptide Y signaling sensitizes nociceptors to drive neuropathic pain. JCI Insight 7 PMID: 36194480
Do you know of a great paper that uses BIIE 0246 hydrochloride from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.