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| 5mg |
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| Targets |
Neuropeptide Y (NPY) receptors, particularly the Y2 receptor subtype. PYY also interacts with Y1, Y4, and Y5 receptor subtypes with varying affinities. As an agonist at these receptors, PYY activates GPCR-mediated signaling pathways that regulate appetite, energy homeostasis, and gastrointestinal function. The Y2 receptor mediates the anorexigenic (appetite-suppressing) effects of PYY.
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| ln Vitro |
Like PP and neuropeptide Y (NPY), intestinal hormone peptide YY (PYY) is a member of the pancreatic polypeptide (PP) family. NPY receptors, of which there are several subtypes (Y1, Y2, Y4, and Y5), are the pathway by which these peptides elicit their effects [1]. A little peptide of 36 amino acids is called pancreatic polypeptide YY (Peptide YY). It has since been found in different areas of the body, having initially been extracted from the pig gut and secreted by neuroendocrine cells (L cells) of the gastrointestinal mucosa. connected to the gastrointestinal tract [2].
PYY belongs to the pancreatic polypeptide family along with PP and neuropeptide Y (NPY). These peptides mediate their effects through NPY receptor subtypes Y1, Y2, Y4, and Y5. PYY shows high affinity for the Y2 receptor, which is involved in appetite regulation. The peptide is 36 amino acids in length and was originally isolated from porcine intestine. It has been localized to various locations associated with the digestive system. |
| ln Vivo |
Pancreatic secretion stimulated by secretin is significantly inhibited by peptide YY. Pancreatic bicarbonate and fluid secretion induced by a single dose of secretin (0.1 units/kg) were dramatically decreased by very modest doses of peptide YY (10–20 pmol/kg). Peptide YY doses of 100–200 pmol/kg cause a 70–80% decrease in fluid secretion and pancreatic bicarbonate [3]. In rabbits, peptide YY localizes to atherosclerotic plaques and blood arteries. The vascular tree experiences vasoconstriction as a result [2].
In vivo, PYY strongly inhibits secretin-stimulated pancreatic secretion. A very low dose of PYY (10-20 pmol/kg) significantly decreases pancreatic secretion of bicarbonate and fluid stimulated by a single dose of secretin (0.1 unit/kg). A dose of 100-200 pmol/kg causes a 70-80% reduction in pancreatic bicarbonate and fluid secretion. PYY is localized to blood vessels and atherosclerotic plaques in rabbits and causes vasoconstriction of the vascular tree. |
| Enzyme Assay |
In vitro receptor binding assays are performed using membrane preparations from cells expressing recombinant NPY receptor subtypes (Y1, Y2, Y4, Y5). Increasing concentrations of PYY (0.01 nM - 1 μM) are incubated with a fixed concentration of radiolabeled NPY (e.g., [¹²⁵I]-PYY) in assay buffer (50 mM HEPES, pH 7.4, 5 mM MgCl₂, 1 mM CaCl₂, 0.1% BSA) for 60-120 minutes at room temperature. Nonspecific binding is determined using 1 μM unlabeled NPY. Bound radioactivity is separated by filtration and quantified. IC50 or Ki values are calculated by nonlinear regression.
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| Cell Assay |
No specific cell-based assay protocols are extensively documented for PYY. For cellular functional assays, cells expressing NPY receptors are treated with varying concentrations of PYY (0.01 nM - 1 μM) for 30-60 minutes. Receptor activation is measured by detecting intracellular calcium mobilization, cAMP accumulation (for Gi-coupled Y2 receptors), or ERK phosphorylation. PYY-mediated inhibition of forskolin-stimulated cAMP accumulation is a common readout for Y2 receptor activity. Dose-response curves are generated and EC50 values are calculated.
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| Animal Protocol |
In animal studies, PYY is administered via intravenous infusion or injection. In anesthetized adult cats (4 kg), secretin and CCK (1.5 units/kg/hr each) are infused through the saphenous vein using a perfusion pump at 10 ml/hr. PYY (10-250 pmol/kg) is infused or injected through the saphenous vein. Pancreatic juice is collected from the cannulated pancreatic duct in 10-minute periods. Juice volume and bicarbonate content are measured. In rabbits, New Zealand White rabbits are fed an atherogenic diet for 4 weeks; immunohistochemistry is used to determine PYY and eNOS localization in the aorta and other arteries.
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| ADME/Pharmacokinetics |
PYY is a 36-amino acid peptide with a molecular weight of 4309.75. It is soluble in water at 100 mg/mL (23.20 mM) with ultrasonication. As a peptide, it has a short half-life in circulation due to rapid proteolytic degradation. It should be stored as powder at -80°C for up to 2 years, at -20°C for up to 1 year, or in solution at -80°C for 6 months and at -20°C for 1 month, sealed, away from moisture and light, under nitrogen. The peptide is stable when stored properly.
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| Toxicity/Toxicokinetics |
No specific toxicity data are documented for Peptide YY (PYY), human. As an endogenous gut hormone, PYY is naturally produced in the body and is generally well-tolerated at physiological concentrations. In research settings, standard laboratory safety practices should be followed when handling the peptide. The compound is intended for research use only and is not approved for human therapeutic applications. Toxicity profiling would be required for any therapeutic development beyond its natural physiological role.
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| References | |
| Additional Infomation |
See also: Peptide YY (Notes moved to).
PYY (human) is a 36-amino acid peptide amide with the sequence YPIKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY-NH2. It is a member of the neuropeptide Y family and is highly conserved across species. PYY has been investigated as a potential appetite suppressant for obesity treatment. It is secreted postprandially in proportion to caloric intake and acts as a "ileal brake" to slow gastrointestinal transit. PYY levels are reduced in obese individuals, making it a therapeutic target for metabolic disorders. The compound is for research use only. |
| Molecular Formula |
C194H295N55O57
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|---|---|
| Molecular Weight |
344.3618
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| Exact Mass |
4309.194
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| CAS # |
118997-30-1
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| PubChem CID |
126455957
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| Appearance |
White to off-white solid powder
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| LogP |
-13.8
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| Hydrogen Bond Donor Count |
63
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| Hydrogen Bond Acceptor Count |
64
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| Rotatable Bond Count |
138
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| Heavy Atom Count |
306
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| Complexity |
10700
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| Defined Atom Stereocenter Count |
37
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| SMILES |
OC1=CC=C(C[C@@H](C(N[C@@H](CC2=CC=C(O)C=C2)C(=O)O)=O)N)C=C1
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| InChi Key |
YNXLOPYTAAFMTN-SBUIBGKBSA-N
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| InChi Code |
InChI=1S/C194H295N55O57/c1-17-99(12)154(244-183(299)143-36-25-73-247(143)188(304)115(196)80-104-37-47-110(253)48-38-104)185(301)228-125(28-18-19-67-195)189(305)248-74-26-34-141(248)181(297)225-122(59-64-149(264)265)159(275)218-102(15)187(303)246-72-24-33-140(246)180(296)214-90-147(261)219-120(58-63-148(262)263)164(280)240-137(88-152(270)271)169(285)217-101(14)158(274)242-139(92-251)190(306)249-75-27-35-142(249)182(298)226-124(61-66-151(268)269)166(282)224-123(60-65-150(266)267)167(283)230-128(77-95(4)5)171(287)238-135(86-145(198)259)176(292)222-117(30-21-69-211-192(203)204)162(278)234-132(83-107-43-53-113(256)54-44-107)174(290)235-131(82-106-41-51-112(255)52-42-106)168(284)216-100(13)157(273)241-138(91-250)179(295)233-127(76-94(2)3)170(286)221-118(31-22-70-212-193(205)206)163(279)237-134(85-109-89-209-93-215-109)175(291)236-133(84-108-45-55-114(257)56-46-108)173(289)231-129(78-96(6)7)172(288)239-136(87-146(199)260)177(293)232-130(79-97(8)9)178(294)243-153(98(10)11)184(300)245-155(103(16)252)186(302)227-119(32-23-71-213-194(207)208)160(276)223-121(57-62-144(197)258)165(281)220-116(29-20-68-210-191(201)202)161(277)229-126(156(200)272)81-105-39-49-111(254)50-40-105/h37-56,89,93-103,115-143,153-155,250-257H,17-36,57-88,90-92,195-196H2,1-16H3,(H2,197,258)(H2,198,259)(H2,199,260)(H2,200,272)(H,209,215)(H,214,296)(H,216,284)(H,217,285)(H,218,275)(H,219,261)(H,220,281)(H,221,286)(H,222,292)(H,223,276)(H,224,282)(H,225,297)(H,226,298)(H,227,302)(H,228,301)(H,229,277)(H,230,283)(H,231,289)(H,232,293)(H,233,295)(H,234,278)(H,235,290)(H,236,291)(H,237,279)(H,238,287)(H,239,288)(H,240,280)(H,241,273)(H,242,274)(H,243,294)(H,244,299)(H,245,300)(H,262,263)(H,264,265)(H,266,267)(H,268,269)(H,270,271)(H4,201,202,210)(H4,203,204,211)(H4,205,206,212)(H4,207,208,213)/t99-,100-,101-,102-,103+,115-,116-,117-,118-,119-,120-,121-,122-,123-,124-,125-,126-,127-,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,138-,139-,140-,141-,142-,143-,153-,154-,155-/m0/s1
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| Chemical Name |
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-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-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-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]-3-hydroxy-1-oxopropan-2-yl]amino]-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]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S,3S)-2-[[(2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-4-carboxybutanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-5-oxopentanoic 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 | 2.9039 mL | 14.5197 mL | 29.0394 mL | |
| 5 mM | 0.5808 mL | 2.9039 mL | 5.8079 mL | |
| 10 mM | 0.2904 mL | 1.4520 mL | 2.9039 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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