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BIIE-0246 is a selective NPY2R antagonist with an IC50 of 15 nM at the rat [125I]PYY3-36 site. It reduces NPY-stimulated expression of p-AKT S473 and P-p44/42 MAPK.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $69 | Inquiry | Inquiry |
| Description | BIIE-0246 is a selective NPY2R antagonist with an IC50 of 15 nM at the rat [125I]PYY3-36 site. It reduces NPY-stimulated expression of p-AKT S473 and P-p44/42 MAPK. |
| Targets&IC50 | NPYY2 receptor:15±3 nM |
| In vitro | BIIE-0246 (1 µM, 24 hours) pretreatment significantly inhibited NPY-induced phosphorylation activation of Akt and MAPK in mouse podocytes [3]. |
| In vivo | BIIE-0246 (10 μg/day, administered via intraperitoneal injection or subcutaneous osmotic minipump for 14 days) significantly reduced the urinary albumin-to-creatinine ratio (uACR) in the adriamycin nephropathy (AN) mouse model, ameliorated renal histopathological damage (such as glomerulosclerosis and reduced tubular casts), and markedly alleviated podocyte foot process effacement as confirmed by electron microscopy analysis [3]. |
| Synonyms | BIIE0246, AR-H053591, AR-H 053591 |
| Molecular Weight | 896.05 |
| Formula | C49H57N11O6 |
| Cas No. | 246146-55-4 |
| Smiles | O=C1C=2C(C(C=3C(N1)=CC=CC3)N4CCN(C(CC5(CC(N[C@H](C(NCCN6C(=O)N(N(C6=O)C7=CC=CC=C7)C8=CC=CC=C8)=O)CCCNC(=N)N)=O)CCCC5)=O)CC4)=CC=CC2 |
| Relative Density. | 1.38 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO: ≥ 80 mg/mL, Sonication is recommended. |
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (3.68 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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