1. GPCR/G Protein
    Neuronal Signaling
  2. Neuropeptide Y Receptor
  3. BIIE-0246

BIIE-0246 (Synonyms: AR-H 053591)

Cat. No.: HY-101986 Purity: >99.0%
Handling Instructions

BIIE-0246 is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, with an IC50 of 15 nM.

For research use only. We do not sell to patients.

BIIE-0246 Chemical Structure

BIIE-0246 Chemical Structure

CAS No. : 246146-55-4

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1 mg USD 210 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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BIIE-0246 is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, with an IC50 of 15 nM.

IC50 & Target

NPYY2 receptor

15±3 nM (IC50)

In Vitro

Receptor binding assays in HEK 293 cells transfected with the rat Y2 receptor cDNA demonstrate that BIIE-0246 competes with high affinity (IC50=15±3 nM) against specific [125I]PYY3-36 binding sites. In contrast, BIIE-0246, at concentrations up to 10 μM, fails to compete for significant amounts of specific [125I]GR231118, [125I]hPP and [125I][Leu31, Pro34]PYY binding sites in HEK 293 cells transfected with the rat Y1, Y4 or Y5 receptor cDNA, respectively[1].

In Vivo

On chow diet, genetically obese NPY mice show increased gain in body weight and adiposity. Treatment with BIIE-0246 promotes body weight gain in both genotypes after 4.5 weeks, and already at 2 weeks. BIIE-0246 has no significant effect on fat mass gain. In DIO, BIIE-0246 has different effects on body weight and composition depending on the genotype (treatment×genotype interaction in body weight P<0.05, in fat mass P<0.001 and in lean mass P<0.05). In DIO-WT group, post hoc analysis reveals increased body weight and fat mass gain, and a tendency to decrease lean mass gain. In DIO-NPY, BIIE-0246 inhibits fat mass gain (P=0.05). Interestingly, increased cholesterol levels are detected also in WT mice treated with BIIE-0246 for 2 weeks, but not in the 4.5-week cohort. In DIO-NPY mice in both treatment groups, cholesterol levels correlate positively with body fat mass (DIO-NPY vehicle P<0.01; DIO-NPY BIIE-0246 P<0.001), but not in any other group, and the slope of the regression curve of cholesterol and fat mass is significantly decreased in BIIE-0246-treated DIO-NPY group when compared with vehicle-treated group[2].

Molecular Weight







O=C(N[[email protected]](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


Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (111.60 mM; Need ultrasonic)

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1160 mL 5.5800 mL 11.1601 mL
5 mM 0.2232 mL 1.1160 mL 2.2320 mL
10 mM 0.1116 mL 0.5580 mL 1.1160 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (2.79 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (2.79 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (2.79 mM); Clear solution

*All of the co-solvents are provided by MCE.
Animal Administration

Homozygous transgenic male OE-NPYDbH and WT mice are used. The mice are housed at 21±3°C with a 12-h light/12-h dark cycle. To study the effect of Y2-receptor antagonism in healthy conditions, standard rodent chow is fed ad libitum to OE-NPYDbH (NPY) and WT mice. To study the effect in DIO, western diet is fed for 8 weeks prior to the drug administration. Drug treatment is studied at the age of 20 weeks. Prior to treatments the mice are habituated for 2 weeks to the handling stress with daily saline injections (i.p). Mice receive 1.3 mg/kg of Y2-receptor antagonist (BIIE-0246) or vehicle with daily IP injections. At termination, mice are fasted for 3 h and blood glucose is measured from awake animals. Mice are then anesthetized with ketamine (75 mg/kg i.p) and medetomidine (1 mg/kg i.p). Subcutaneous, epididymal, retroperitoneal and mesenteric white adipose tissue (WAT) pads, interscapular brown adipose tissue (BAT) and liver are collected and weighed[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Purity: >99.0%

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BIIE-0246AR-H 053591BIIE0246BIIE 0246Neuropeptide Y ReceptorNPY receptorInhibitorinhibitorinhibit

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