BIIE-0246
Based on 2 publication(s) in Google Scholar
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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The BIIE-0246 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- Purity: 99.10%
- CAS No.: 246146-55-4
- 화학식: C49H57N11O6
- 분자량:896.05
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BIIE-0246
MoreAll Neuropeptide Y Receptor Isoforms
More
Biological Activity
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NPY Y2 receptor 15±3 nM (IC50) |
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.
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Cell Line:Mouse podocytes[3]
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Concentration:1 µM
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Incubation Time:24 h
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Result:Blocked the NPY-stimulated phosphorylation of Akt and p44/42 MAPK.
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.
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Animal Model:Homozygous transgenic male OE-NPYDβH and WT C57Bl/6N mice[1]
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Dosage:1.3 mg/kg
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Administration:I.p.; daily for 2 or 4.5 weeks
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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.
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Animal Model:Male BALB/c mice[3]
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Dosage:10 µg/day
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Administration:I.p.; daily for 14 days
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Result:Reduces albuminuria in ADR nephropathy.
Chemical Information
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CAS No. 246146-55-4
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Appearance Solid
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분자량 896.05
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화학식 C49H57N11O6
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Color White to off-white
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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
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Synonyms
AR-H 053591
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Sci Rep
Combined effects of red light and direct-current electric fields on neurite growth in 3D neural cell cultures. [Abstract]2025 Nov 29;16(1):408. PMID: 41318831 -
In Vivo
Ghrelin Induces the Production of Hypothalamic NPY Through the AMPK-mTOR Pathway to Alleviate Cancer-induced Bone Pain. [Abstract]2024 May-Jun;38(3):1133-1142. PMID: 38688635
용액&용해도
DMSO : ≥ 100 mg/mL (111.60 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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]
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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