Molecular structure of BIIE 0246, CAS Number: 246146-55-4
BIIE 0246 (CAS 246146-55-4)
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Alternate Names:
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-dih ydro-6-oxo-5H-dibenz[b,e]azepin-11-yl)-1-piperazin yl]-2-oxoethyl]-cyclopentaneacetamide
Application:
BIIE 0246 is a selective and competitive NPY2-R antagonist
CAS Number:
246146-55-4
Purity:
≥98%
Molecular Weight:
896.05
Molecular Formula:
C49H57N11O6
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Available in US only.
Available in US only.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
BIIE 0246 is a selective non-peptide antagonist which binds to the neuropeptide NPY2-R in a competitive manner. In addition, BIIE 0246 suppresses another neuropeptide, [ahx5-24]NPY. Moreover, studies suggest that BIIE 0246 is highly lipophilic and as a result BIIE 0246 builds up at membranes near the receptors. Furthermore, studies indicate that the antagonistic effects of BIIE 0246 on neuropeptide Y (NPY) are insurmountable, which may result from the lipophilic nature of the antagonist.
BIIE 0246 (CAS 246146-55-4) References
- BIIE0246: a selective and high affinity neuropeptide Y Y(2) receptor antagonist. | Doods, H., et al. 1999. Eur J Pharmacol. 384: R3-5. PMID: 10611450
- BIIE0246, a potent and highly selective non-peptide neuropeptide Y Y(2) receptor antagonist. | Dumont, Y., et al. 2000. Br J Pharmacol. 129: 1075-88. PMID: 10725255
- Vascular pharmacology of BIIE0246, the first selective non-peptide neuropeptide Y Y(2) receptor antagonist, in vivo. | Malmström, RE. 2001. Br J Pharmacol. 133: 1073-80. PMID: 11487518
- Antihyperalgesic effects of intrathecal neuropeptide Y during inflammation are mediated by Y1 receptors. | Taiwo, OB. and Taylor, BK. 2002. Pain. 96: 353-363. PMID: 11973010
- Blockade of neuropeptide Y(2) receptors and suppression of NPY's anti-epileptic actions in the rat hippocampal slice by BIIE0246. | El Bahh, B., et al. 2002. Br J Pharmacol. 136: 502-9. PMID: 12055128
- Antagonistic interaction between BIIE 0246, a neuropeptide Y Y2-receptor antagonist, and omega-conotoxin GVIA, a Ca2+ channel antagonist, in presynaptic transmitter releases in dog splenic arteries. | Yang, XP. and Chiba, S. 2002. Jpn J Pharmacol. 89: 188-91. PMID: 12120763
- Neuropeptide Y inhibits double peaked vasoconstrictor responses to periarterial nerve stimulation primarily through prejunctional Y2 receptor subtype in canine splenic arteries. | Yang, XP. and Chiba, S. 2002. Auton Autacoid Pharmacol. 22: 119-26. PMID: 12568129
- The effect of intrahippocampal injection of group II and III metobotropic glutamate receptor agonists on anxiety; the role of neuropeptide Y. | Smiałowska, M., et al. 2007. Neuropsychopharmacology. 32: 1242-50. PMID: 17133262
- Lateral septal infusions of the neuropeptide Y Y2 receptor agonist, NPY(13-36) differentially affect different defensive behaviors in male, Long Evans rats. | Trent, NL. and Menard, JL. 2013. Physiol Behav. 110-111: 20-9. PMID: 23274501
- Role of peptide YY(3-36) in the satiety produced by gastric delivery of macronutrients in rats. | Reidelberger, R., et al. 2013. Am J Physiol Endocrinol Metab. 304: E944-50. PMID: 23482449
- Blockage of peripheral NPY Y1 and Y2 receptors modulates barorefex sensitivity of diabetic rats. | Liu, J., et al. 2013. Cell Physiol Biochem. 31: 421-31. PMID: 23548582
- Inhibition of peripheral NPY Y1 and Y2 receptors ameliorates the aberrant baroreceptor reflex sensitivity in streptozotocin induced diabetic rats. | Niu, HF., et al. 2013. Sheng Li Xue Bao. 65: 370-80. PMID: 23963068
- Increase in neuropeptide Y activity impairs social behaviour in association with glutamatergic dysregulation in diabetic mice. | Ueda, D., et al. 2021. Br J Pharmacol. 178: 726-740. PMID: 33197050
- Neuropeptide Y and glutamatergic mechanisms in the amygdala and ventral hippocampus differentially mediate impaired social behavior in diabetic mice. | Ueda, D., et al. 2021. Behav Brain Res. 405: 113195. PMID: 33617904
- Intracolonic Neuropeptide Y Y1 Receptor Inhibition Attenuates Intestinal Inflammation in Murine Colitis and Cytokine Release in IBD Biopsies. | Chandrasekharan, B., et al. 2022. Inflamm Bowel Dis. 28: 502-513. PMID: 34613372
Inhibitor of:
Neuropeptide Y (NPY), NPY, NPY1-R, and NPY2-R.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
BIIE 0246, 1 mg | sc-203530 | 1 mg | $321.00 | |||
| US: Only available in the US | ||||||
BIIE 0246, 10 mg | sc-203530A | 10 mg | $530.00 | |||
| US: Only available in the US | ||||||