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

BIIE-0246  (Synonyms: AR-H 053591)

Cat. No.: HY-101986 Purity: 99.10%
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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 Chemical Structure

BIIE-0246 Chemical Structure

CAS No. : 246146-55-4

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Based on 1 publication(s) in Google Scholar

Other Forms of BIIE-0246:

BIIE-0246 Related Antibodies

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1 Publications Citing Use of MCE BIIE-0246

View All Neuropeptide Y Receptor Isoform Specific Products:

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NPY Y1 receptor NPY Y2 receptor NPY Y4 receptor NPY Y5 receptor

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Description

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].

IC50 & Target

NPY Y2 receptor

15±3 nM (IC50)

In Vitro

BIIE-0246 (1 µM; 24 h) decreases the expression of p-AKT S473, P-p44/42 MAPK under the NPY-stimulated (10, 100 ng/mL) in mouse podocytes[3].

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

BIIE-0246 Related Antibodies

Western Blot Analysis[3]

Cell Line: Mouse podocytes[3]
Concentration: 1 µM
Incubation Time: 24 h
Result: Blocked the NPY-stimulated phosphorylation of Akt and p44/42 MAPK.
In Vivo

BIIE-0246 (1.3 mg/kg; I.p.; daily for 2 or 4.5 weeks) prevents diet-induced obesity in OE-NPYDβH mice, but enhances obesity in WT Mice[1].
BIIE-0246 (10 µg/day; i.p.; daily for 14 days) reduces albuminuria in ADR (adriamycin) nephropathy[3].

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

Animal Model: Homozygous transgenic male OE-NPYDβH and WT C57Bl/6N mice[1]
Dosage: 1.3 mg/kg
Administration: I.p.; daily for 2 or 4.5 weeks
Result: Increased body weight gain in both genotypes on the chow diet caused metabolic disturbances, especially in WT mice. During energy surplus (i.e., on Western diet), blocking of Y2-receptors induced obesity in WT mice and OE-NPYDβH mice showed a reduced fat mass gain, hepatic glycogen and serum cholesterol levels relative to body adiposity.
Animal Model: Male BALB/c mice[3]
Dosage: 10 µg/day
Administration: I.p.; daily for 14 days
Result: Reduces albuminuria in ADR nephropathy.
Molecular Weight

896.05

Formula

C49H57N11O6
CAS No.
Appearance

Solid

Color

White to off-white

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
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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1160 mL 5.5800 mL 11.1601 mL 27.9002 mL
5 mM 0.2232 mL 1.1160 mL 2.2320 mL 5.5800 mL
10 mM 0.1116 mL 0.5580 mL 1.1160 mL 2.7900 mL
15 mM 0.0744 mL 0.3720 mL 0.7440 mL 1.8600 mL
20 mM 0.0558 mL 0.2790 mL 0.5580 mL 1.3950 mL
25 mM 0.0446 mL 0.2232 mL 0.4464 mL 1.1160 mL
30 mM 0.0372 mL 0.1860 mL 0.3720 mL 0.9300 mL
40 mM 0.0279 mL 0.1395 mL 0.2790 mL 0.6975 mL
50 mM 0.0223 mL 0.1116 mL 0.2232 mL 0.5580 mL
60 mM 0.0186 mL 0.0930 mL 0.1860 mL 0.4650 mL
80 mM 0.0140 mL 0.0698 mL 0.1395 mL 0.3488 mL
100 mM 0.0112 mL 0.0558 mL 0.1116 mL 0.2790 mL
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BIIE-0246 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BIIE-0246246146-55-4AR-H 053591BIIE0246BIIE 0246Neuropeptide Y ReceptorNPY receptorp-AKT S473P-p44/42 MAPKMouse podocytesobesitynephropathyInhibitorinhibitorinhibit

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