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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Description

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].

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

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].

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

Molecular Weight

896.05

Formula

C₄₉H₅₇N₁₁O₆

CAS No.

246146-55-4

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
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)

Preparing
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.
References
Animal Administration
[2]

Mice[2]
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.

References

Purity: >99.0%

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Keywords:

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

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Product Name:
BIIE-0246
Cat. No.:
HY-101986
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