| 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 1 nM (Kd) NPY Y2 receptor 670 nM (Kd)
Neuropeptide Y (NPY) receptor subtype Y1 (NPY1R). NPY is a potent orexigenic peptide involved in many physiological processes including appetite regulation, anxiety, memory, and vasoconstriction. The Y1 receptor is one of several GPCRs that mediate these effects. (Leu31,Pro34)-Peptide YY is a selective agonist for the Y1 receptor, helping to dissociate its functions from those of other NPY receptors. |
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| ln Vitro |
(Leu31,Pro34)-Peptide YY (human) (TFA) is a potent and selective Y1 agonist with a KD of 1.0 nM. This high binding affinity makes it a valuable tool for specifically activating Y1 receptors in vitro without significantly affecting other NPY receptors. It is a derivative of Peptide YY (PYY), a naturally occurring gut hormone, and its activity is enhanced by the specific leucine and proline substitutions.
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| ln Vivo |
In vivo activity data is not provided in the available datasheets. As a Y1 agonist, it is a powerful tool for studying the physiological roles of the Y1 receptor in animal models. By activating Y1 receptors, this peptide can induce specific biological responses, such as vasoconstriction or anxiolysis, depending on the site of action, making it valuable for dissecting complex neuropeptide Y signaling pathways.
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| Enzyme Assay |
To assess binding affinity, a radioligand binding assay is performed using membranes prepared from cells that overexpress the human Y1 receptor. The membranes are incubated with a radiolabeled version of a known Y1 ligand, such as [125I]-PYY, in the presence of varying concentrations of the test peptide. After incubation, the mixture is filtered to separate bound from free radioligand, and the radioactivity is counted to calculate the KD value.
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| Cell Assay |
A standard cell-based assay for GPCR activation involves measuring the accumulation of intracellular cAMP. Cells expressing the Y1 receptor are treated with forskolin to raise cAMP levels. The Y1 receptor is Gi-coupled, so its activation inhibits adenylyl cyclase and reduces cAMP. Cells are exposed to varying concentrations of the peptide, and the resulting cAMP levels are measured using an ELISA or a TR-FRET-based kit to determine the EC50.
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| Animal Protocol |
For in vivo studies of appetite, a fasted mouse model is used. Mice are fasted overnight and then injected intraperitoneally or intracerebroventricularly with the peptide. Food intake is measured at various time points post-injection. Activation of Y1 receptors in the hypothalamus is known to have orexigenic effects, so this peptide can be used to study feeding behavior and the neural circuits controlling appetite.
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| ADME/Pharmacokinetics |
As a 36-amino acid peptide, it has low oral bioavailability. The TFA salt form is water-soluble and is typically administered via injection for in vivo studies. The peptide should be stored as a lyophilized powder at -80degC and protected from moisture. When in solution, it should be stored at -80degC for up to 1 year to prevent degradation.
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| Toxicity/Toxicokinetics |
No toxicity data is provided for this compound. Peptide agonists of GPCRs are generally well-tolerated at low to moderate doses. As with other research chemicals, standard precautions should be taken during handling. A significant concern for systemically administered peptides is the potential for immunogenicity, although this is less of a concern for single-dose or short-term studies.
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| References | |
| Additional Infomation |
This product is a research-grade peptide used for studying NPY receptor pharmacology. The Y1 receptor is a promising target for treating various conditions, including obesity, anxiety, and hypertension. This product is for research use only and is not FDA-approved for human therapy. A key reference is likely the paper describing the design and activity of the peptide.
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| Molecular Formula |
C195H296N54O56.XC2HF3O2
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| Molecular Weight |
4292.75 (free base)
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| Related CAS # |
(Leu31,Pro34)-Peptide YY (human);179986-95-9
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| Appearance |
Solid powder
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 :~100 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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