![[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA](/upload/1124/V77339.png)
| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
NPY Y1 receptor NPY Y4 receptor NPY Y5 receptor
Neuropeptide Y Y1 receptor (NPY1R). [Leu31,Pro34]-Neuropeptide Y is a high-affinity and specific agonist for the Y1 receptor subtype, a Gi-protein-coupled receptor. It also shows significant activation of Y4 and Y5 receptors but has very low affinity for Y2 (Ki > 1000 nM). The Y1 receptor mediates key physiological actions of NPY, including potent vasoconstriction, anxiolysis, and the orexigenic (appetite-stimulating) effect in the hypothalamus. |
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| ln Vitro |
For Y1, Y4, and Y5, in HEK cell lines, [Leu31,Pro34]-Neuropeptide Y (human,rat) TFA has Ki values of 0.39 nM, 0.499 nM, and 0.31 nM. In HEK cell lines, [Leu31,Pro34]-Neuropeptide Y (human,rat) TFA has a Ki of >1000 for Y2[2].
In HEK cell lines stably expressing human NPY receptors, [Leu31,Pro34]-NPY has Ki values of 0.39 nM for Y1, 0.499 nM for Y4, and 0.31 nM for Y5, demonstrating high potency. It acts as a full agonist at these receptors, inhibiting forskolin-stimulated cAMP accumulation in a dose-dependent manner. Its activity at the Y2 receptor is negligible (Ki > 1000 nM), confirming its high selectivity for the Y1 subtype. |
| ln Vivo |
Food intake in rats (350±400 g) is increased by [Leu31,Pro34]-Neuropeptide Y (human,rat) TFA (30 pmol; microinjected into paraventricular nucleus)[3].
In vivo, [Leu31,Pro34]-Neuropeptide Y is a potent orexigenic agent. When microinjected into the paraventricular nucleus (PVN) of the hypothalamus in rats (30 pmol), it produces a robust and significant increase in food intake. It also elevates blood pressure in anesthetized rats due to its Y1-mediated vasoconstrictor effect on the peripheral vasculature. These effects can be blocked by selective Y1 receptor antagonists, confirming target specificity. |
| Enzyme Assay |
To determine receptor binding affinity, a radioligand competitive binding assay is performed. Membranes from HEK-293 cells expressing human NPY Y1 receptors are incubated with the high-affinity radioligand [125I]-PYY (peptide YY) or [125I]-NPY. Varying concentrations of the unlabeled [Leu31,Pro34]-Neuropeptide Y (0.01-1000 nM) are added to compete for binding. After incubation at room temperature for 60-90 minutes, the mixture is filtered through GF/C filters pre-soaked in polyethylenimine (PEI). Bound radioactivity is counted to calculate the Ki value.
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| Cell Assay |
A functional cAMP inhibition assay is used to confirm agonist activity. CHO-K1 or HEK-293 cells stably expressing the NPY Y1 receptor are seeded in 96-well plates and pre-incubated with 1 mM IBMX to inhibit phosphodiesterase. Cells are then treated with varying concentrations of [Leu31,Pro34]-NPY (0.01-1000 nM) in the presence of 1-5 uM forskolin to stimulate cAMP production. After 30-60 minutes, the cells are lysed, and intracellular cAMP levels are measured using a homogeneous time-resolved fluorescence (HTRF) or ELISA-based kit. The EC50 is calculated from the dose-dependent inhibition of the forskolin-induced cAMP signal.
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| Animal Protocol |
The orexigenic effect is studied in male Sprague-Dawley rats (weighing 350-400 g) surgically implanted with a guide cannula aimed at the paraventricular nucleus (PVN) of the hypothalamus. After recovery, the animals are fasted overnight. [Leu31,Pro34]-Neuropeptide Y (30 pmol in 0.5-1 uL saline) or vehicle control is microinjected into the PVN. Food intake is measured by weighing pre-weighed chow at 1, 2, and 4 hours post-injection. The cumulative food intake is significantly higher in the peptide-treated group compared to the vehicle control group, validating the Y1-mediated orexigenic effect.
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| ADME/Pharmacokinetics |
As a 36-amino acid peptide, the TFA salt form is soluble in H2O (~50 mg/mL). However, it has very poor oral bioavailability due to degradation in the GI tract and is typically administered via intracerebroventricular (ICV) or intraparenchymal microinjection for CNS studies, or intravenously (IV) for cardiovascular studies. The plasma half-life is short (minutes) due to rapid proteolysis. The peptide must be stored as a lyophilized powder at -80degC to maintain integrity; dissolved solutions should be stored at -80degC.
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| Toxicity/Toxicokinetics |
As a research peptide, the toxicity of [Leu31,Pro34]-Neuropeptide Y TFA is associated with its pharmacological effects rather than inherent chemical toxicity. At the doses used for orexigenic studies (30 pmol ICV), the peptide induces a robust increase in food intake without causing systemic toxicity. When administered systemically at high doses, it can cause profound and prolonged hypertension and bradycardia via Y1 receptor activation. No acute organ toxicity or genotoxicity has been reported.
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| References |
[1]. K McCrea, et al. 2-36[K4,RYYSA(19-23)]PP a novel Y5-receptor preferring ligand with strong stimulatory effect on food intake. Regul Pept. 2000 Feb 8;87(1-3):47-58.
[2]. J Fuhlendorff, et al. [Leu31, Pro34]neuropeptide Y: a specific Y1 receptor agonist. Proc Natl Acad Sci U S A. 1990 Jan;87(1):182-6. [3]. A Kask, et al. Evidence for involvement of neuropeptide Y receptors in the regulation of food intake: studies with Y1-selective antagonist BIBP3226. Br J Pharmacol. 1998 Aug;124(7):1507-15. |
| Additional Infomation |
[Leu31,Pro34]-Neuropeptide Y TFA is a research-grade chemical tool used exclusively for studying NPY receptor pharmacology. It is the standard selective Y1 receptor agonist used worldwide to validate the role of NPY and its receptors in obesity, metabolic syndrome, cardiovascular diseases, and anxiety disorders. Key references include Fuhlendorff et al. (1990), which first characterized its selectivity (PNAS), and Kask et al. (1998), which used it to study food intake regulation. This product is for research use only (RUO) and is not a clinical drug; it has no FDA approval or clinical trial status.
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| Molecular Formula |
C191H285F3N54O58S
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| Molecular Weight |
4354.76
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| Related CAS # |
[Leu31,Pro34]-Neuropeptide Y(human,rat);132699-73-1
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O :~50 mg/mL (~11.48 mM)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2296 mL | 1.1482 mL | 2.2963 mL | |
| 5 mM | 0.0459 mL | 0.2296 mL | 0.4593 mL | |
| 10 mM | 0.0230 mL | 0.1148 mL | 0.2296 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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