| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
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| ln Vitro |
In mouse podocytes induced by NPY (10, 100 ng/mL), BIIE-0246 hydrochloride (1 µM; 24 h) decreases the expression of p-AKT S473 and P-p44/42 MAPK [3].
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| ln Vivo |
While BIIE-0246 hydrochloride (1.3 mg/kg; Ip; daily for 2 or 4.5 weeks) causes a rise in obesity in WT mice, it protects diet-induced obesity in OE-NPYDβH mice [1]. In individuals with ADR nephropathy, BIIE-0246 hydrochloride (10 µg/day; ip; daily for 14 days) lowers albuminuria [3].
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| Cell Assay |
Western Blot Analysis[3]
Cell Types: Mouse podocytes Tested Concentrations: 1 µM Incubation Duration: 24 h Experimental Results: Blocked the NPY-stimulated phosphorylation of Akt and p44/42 MAPK. |
| Animal Protocol |
Animal/Disease Models: Homozygous transgenic male OE-NPYDβH and WT C57Bl/6N mice[1]
Doses: 1.3 mg/kg Route of Administration: Ip; daily for 2 or 4.5 weeks Experimental Results: Increased body weight gain in both genotypes on the chow diet caused metabolic disturbances , especially in WT mice. During energy surplus (ie, on Western diet), blocking of Y2-receptors induced obesity in WT mice and OE-NPYDβH mice demonstrated a decreased fat mass gain, hepatic glycogen and serum cholesterol levels relative to body adiposity. Animal/Disease Models: Male balb/c (Bagg ALBino) mouse[3] Doses: 10 µg/day Route of Administration: Ip; daily for 14 days Experimental Results: Reduces albuminuria in ADR nephropathy. |
| 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.
[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. [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. |
| Molecular Formula |
C49H57N11O6.XHCL
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|---|---|
| Related CAS # |
BIIE-0246;246146-55-4
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| Solubility (In Vitro) |
DMSO :~40 mg/mL
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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