246146-55-4
Chemical Structure
BIIE-0246
Synonym(s): AR-H 053591
- CAS No.: 246146-55-4
- Formula:C49H57N11O6
- Molecular Weight:896.05
IUPAC Name: (2S)-N-(2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl)-5-guanidino-2-(2-(1-(2-oxo-2-(4-(6-oxo-6,11-dihydro-5H-dibenzo[b,e]azepin-11-yl)piperazin-1-yl)ethyl)cyclopentyl)acetamido)pentanamide
InChIKey: RSJAXPUYVJKAAA-JPGJPTAESA-N
SMILES: O=C(N[C@H](C(NCCN1C(N(C2=CC=CC=C2)N(C3=CC=CC=C3)C1=O)=O)=O)CCCNC(N)=N)CC4(CC(N5CCN(C(C6=CC=CC=C67)C8=CC=CC=C8NC7=O)CC5)=O)CCCC4
Biological Activity: BIIE-0246 (AR-H 053591) is a potent and selective NPY2R (neuropeptide Y receptor 2) antagonist with an IC50 value of 15 nM for rat [125I]PYY3-36. BIIE-0246 decreases the expression of p-AKT S473, P-p44/42 MAPK under the NPY-stimulated. BIIE-0246 reduces albuminuria in ADR nephropathy[1][2][3].
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BIIE-0246 | 99.10% | BIIE-0246 (AR-H 053591) is a potent and selective NPY2R (neuropeptide Y receptor 2) antagonist with an IC50 value of 15 nM for rat [125I]PYY3-36. BIIE-0246 decreases the expression of p-AKT S473, P-p44/42 MAPK under the NPY-stimulated. BIIE-0246 reduces albuminuria in ADR nephropathy. | ||||||||||||||||||||
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BIIE-0246 (Standard) | ≥98% | BIIE-0246 (Standard) is the analytical standard of BIIE-0246 (HY-101986). This product is intended for research and analytical applications. BIIE-0246 (AR-H 053591) is a potent and selective NPY2R (neuropeptide Y receptor 2) antagonist with an IC50 value of 15 nM for rat [125I]PYY3-36. BIIE-0246 decreases the expression of p-AKT S473, P-p44/42 MAPK under the NPY-stimulated. BIIE-0246 reduces albuminuria in ADR nephropathy. | ||||||||||||||||||||
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References
- [1]. Ailanen L, et al. Peripherally Administered Y2-Receptor Antagonist BIIE0246 Prevents Diet-Induced Obesity in Mice With Excess Neuropeptide Y, but Enhances Obesity in Control Mice. Front Pharmacol. 2018 Apr 5;9:319. [Content Brief]
- [2]. Dumont Y, et al. BIIE0246, a potent and highly selective non-peptide neuropeptide Y Y(2) receptor antagonist. Br J Pharmacol. 2000 Mar;129(6):1075-88. [Content Brief]
- [3]. Lay AC, et al. A role for NPY-NPY2R signaling in albuminuric kidney disease. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):15862-15873. [Content Brief]
