| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Neuropeptide Y2 receptor (Y2R).
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|---|---|
| ln Vitro |
Neuropeptide Y (13-36), amide, human is a selective agonist at the NPY Y2 receptor. It binds with high affinity to Y2 receptors but has low affinity for Y1 receptors. Activation of Y2 receptors inhibits adenylyl cyclase and reduces cAMP levels.
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| ln Vivo |
There was a dose-dependent increase in mean arterial blood pressure (up to 14%; ED50 for overall effect 0.3 nmol, peak effect 0.97 nmol) with neuropeptide Y (13–36) (intracerebroventricular injection; 25–3000 pmol). Male rats, awake, unconstrained, heart rate unaltered. Significant vasodepressant and bradycardic effects are produced by central injection of porcine neuropeptide Y (13–36) in conscious unrestrained male rats under α-chloralose anesthesia [1]. The NPY Y2 receptor antagonist BIIE 0246 can suppress the effect of injecting neuropeptide Y (13–36) (intracerebroventricular injection; 50 ng; alone; injected 30 and 15 min before assessment) into young rats. This effect affects social novelty preference but not sociability.
Centrally injected Neuropeptide Y (13-36) produces vasopressor effects and antagonizes the vasodepressor action of Neuropeptide Y (1-36) in awake male rats. It is involved in the regulation of blood pressure and cardiovascular function. |
| Enzyme Assay |
Y2 receptor binding assays are performed using membrane preparations from cells expressing human Y2 receptors. Radiolabeled ligand (e.g., [¹2⁵I]-PYY3-36) displacement assays determine the compound's affinity. Functional assays measure the inhibition of forskolin-stimulated cAMP accumulation in Y2-expressing cells.
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| Cell Assay |
Cells expressing Y2 receptors (e.g., CHO or HEK-293 cells) are treated with the peptide. Receptor-mediated signaling is assessed by measuring cAMP levels (inhibition of forskolin-stimulated cAMP), ERK phosphorylation, or calcium mobilization. Potency (EC50) is determined from concentration-response curves.
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| Animal Protocol |
Animal/Disease Models: Male ICR mice (4-7 weeks old) [2]
Doses: 50 ng/mouse Route of Administration: Intracerebroventricular injection Experimental Results: Interaction with Novel Strange Mice in Section 3 of NPY 13-36 Time is Dramatically diminished. Animal models (e.g., rats) are used to assess the central effects of the peptide. Intracerebroventricular or intrahypothalamic injection of Neuropeptide Y (13-36) is performed. Blood pressure, heart rate, food intake, and anxiety-like behavior are measured. The Y2 receptor-mediated vasopressor effects are characterized. |
| ADME/Pharmacokinetics |
As a peptide, Neuropeptide Y (13-36) has poor oral bioavailability and does not cross the blood-brain barrier effectively. It is typically administered centrally (i.c.v.) for in vivo studies. The half-life in plasma is short due to rapid proteolytic degradation.
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| Toxicity/Toxicokinetics |
No significant toxicity reported at research doses. As a neuropeptide fragment, it is expected to have low toxicity. Standard safety pharmacology studies would be required for therapeutic development.
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| References |
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| Additional Infomation |
Neuropeptide Y (13-36), amide, human is a research tool for studying NPY Y2 receptor biology and its role in cardiovascular regulation, appetite, and anxiety. It has not been approved for clinical use. The compound is valuable for understanding the therapeutic potential of Y2 receptor modulation in obesity, hypertension, and anxiety disorders.
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| Molecular Formula |
C134H207N41O36S
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|---|---|
| Molecular Weight |
3000.40000
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| Exact Mass |
2998.53
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| CAS # |
122341-40-6
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| PubChem CID |
44208913
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| Appearance |
White to off-white solid powder
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| LogP |
5.221
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| Hydrogen Bond Donor Count |
48
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| Hydrogen Bond Acceptor Count |
43
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| Rotatable Bond Count |
100
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| Heavy Atom Count |
212
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| Complexity |
6800
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCC(C)C(C(=O)NC(CC(=O)N)C(=O)NC(CC(C)C)C(=O)NC(C(C)CC)C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC1=CC=C(C=C1)O)C(=O)N)NC(=O)C(CC2=CC=C(C=C2)O)NC(=O)C(CC3=CNC=N3)NC(=O)C(CCCNC(=N)N)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CO)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(CC5=CC=C(C=C5)O)NC(=O)C(CCCNC(=N)N)NC(=O)C(C)NC(=O)C(CCSC)NC(=O)C(CC(=O)O)NC(=O)C(CCC(=O)O)NC(=O)C(C)NC(=O)C6CCCN6
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| InChi Key |
WPVRWBQWAYQJSX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C134H207N41O36S/c1-14-67(7)104(128(209)171-97(60-101(136)183)123(204)165-92(54-66(5)6)125(206)174-105(68(8)15-2)129(210)175-106(72(12)177)130(211)162-86(25-20-51-151-134(144)145)113(194)160-87(42-44-100(135)182)117(198)158-84(23-18-49-149-132(140)141)114(195)163-90(107(137)188)55-73-26-34-78(178)35-27-73)173-126(207)95(58-76-32-40-81(181)41-33-76)168-122(203)96(59-77-62-146-64-152-77)169-116(197)85(24-19-50-150-133(142)143)159-119(200)91(53-65(3)4)164-110(191)71(11)155-127(208)99(63-176)172-121(202)94(57-75-30-38-80(180)39-31-75)167-120(201)93(56-74-28-36-79(179)37-29-74)166-115(196)83(22-17-48-148-131(138)139)156-108(189)70(10)154-112(193)89(46-52-212-13)161-124(205)98(61-103(186)187)170-118(199)88(43-45-102(184)185)157-109(190)69(9)153-111(192)82-21-16-47-147-82/h26-41,62,64-72,82-99,104-106,147,176-181H,14-25,42-61,63H2,1-13H3,(H2,135,182)(H2,136,183)(H2,137,188)(H,146,152)(H,153,192)(H,154,193)(H,155,208)(H,156,189)(H,157,190)(H,158,198)(H,159,200)(H,160,194)(H,161,205)(H,162,211)(H,163,195)(H,164,191)(H,165,204)(H,166,196)(H,167,201)(H,168,203)(H,169,197)(H,170,199)(H,171,209)(H,172,202)(H,173,207)(H,174,206)(H,175,210)(H,184,185)(H,186,187)(H4,138,139,148)(H4,140,141,149)(H4,142,143,150)(H4,144,145,151)
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| Chemical Name |
5-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[4-amino-1-[[1-[[1-[[1-[[1-[[5-amino-1-[[1-[[1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-5-oxo-4-[2-(pyrrolidine-2-carbonylamino)propanoylamino]pentanoic acid
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.3333 mL | 1.6664 mL | 3.3329 mL | |
| 5 mM | 0.0667 mL | 0.3333 mL | 0.6666 mL | |
| 10 mM | 0.0333 mL | 0.1666 mL | 0.3333 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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