| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Peptide YY (3-36) primarily targets neuropeptide Y (NPY) receptor family members, including Y2 and Y5 receptors, which are involved in appetite regulation. It exhibits high affinity for the Y2 receptor, which mediates its anorectic effects, while also binding with lower affinity to other NPY receptor subtypes such as Y1 and Y5. The compound acts as an agonist at these receptors, modulating feeding behavior and energy homeostasis.
|
|---|---|
| ln Vitro |
In vitro studies demonstrate that PYY(3-36) binds with high affinity to recombinant human Y2 receptors and inhibits forskolin-stimulated cAMP accumulation, confirming its functional agonist activity at this receptor. The N-terminal truncation enhances Y2 receptor selectivity compared to full-length PYY(1-36), which is critical for its appetite-suppressing effects.
|
| ln Vivo |
In vivo, peripheral administration of PYY(3-36) significantly reduces food intake and decreases plasma acyl-ghrelin levels in pigs, confirming its anorexigenic properties. This effect is mediated through Y2 receptors in the hypothalamus, leading to decreased appetite and caloric intake. The peptide is rapidly metabolized to inactive PYY(3-34) in circulation, limiting its duration of action.
|
| Enzyme Assay |
A typical in vitro receptor binding assay involves incubating Y2 receptor-expressing cell membranes with radiolabeled PYY (e.g., ¹2⁵I-PYY) in the presence of increasing concentrations of unlabeled test compound. After incubation at room temperature for 60-90 minutes, bound radioligand is separated by rapid filtration through glass fiber filters, and radioactivity is quantified by gamma counting to calculate IC50 or Ki values.
|
| Cell Assay |
Saturation binding studies are performed on membranes from cells stably expressing Y2 receptors using radiolabeled PYY(3-36) to determine binding affinity. Functional assays involve measuring cAMP accumulation using a homogeneous time-resolved fluorescence (HTRF) platform in cells treated with forskolin (to stimulate cAMP production) and varying concentrations of test compound, comparing inhibition of cAMP production to full-length PYY as a reference agonist.
|
| Animal Protocol |
Male Wistar rats or pigs are fasted overnight, then administered PYY(3-36) via intraperitoneal or intravenous injection at doses typically ranging from 10-100 microg/kg. Food intake is measured at multiple time points (1, 2, 4, 6, 12, and 24 hours) post-administration. Plasma samples are collected for ghrelin measurement by ELISA and for pharmacokinetic analysis to assess the peptide's metabolic stability and clearance.
|
| ADME/Pharmacokinetics |
The elimination half-life (t½) of PYY(3-36) in circulation is very short (approximately 10-20 minutes) due to rapid degradation by dipeptidyl peptidase IV (DPP-IV) and other proteases that cleave the N-terminus, converting it to the inactive metabolite PYY(3-34). The compound is primarily cleared by renal excretion and proteolytic degradation, with minimal protein binding in plasma.
|
| Toxicity/Toxicokinetics |
No significant toxicity has been reported for porcine PYY(3-36) at experimental doses. Based on the well-established safety profile of related gut hormones and endogenous peptide analogs, adverse effects are expected to be minimal. In preclinical models, the compound does not cause behavioral changes or organ toxicity at doses up to 10-fold higher than those required for anorectic effects, although detailed toxicological studies are limited.
|
| References | |
| Additional Infomation |
Endogenous PYY(3-36) is released from intestinal L-cells postprandially and acts as a "ileal brake" signal. The PYY system remains a validated target for obesity therapeutics; however, the short half-life of native PYY(3-36) has driven development of long-acting analogs and DPP-IV-resistant derivatives. No drug containing porcine-derived PYY(3-36) TFA has received regulatory approval; it is strictly a preclinical research tool. This compound is highly similar in pharmacology to its human sequence counterpart (which differs at positions 3 and 18) and is exclusively utilized in academic and industrial research settings to dissect Y receptor signaling, appetite circuits, and metabolic control.
|
| Molecular Formula |
C176H272N52O54.C2HF3O2
|
|---|---|
| Molecular Weight |
4094.44
|
| Related CAS # |
Peptide YY (PYY) (3-36), porcine;126339-09-1
|
| Appearance |
Solid powder
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O :~100 mg/mL (~24.42 mM)
DMSO :~100 mg/mL (~24.42 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (12.21 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2442 mL | 1.2212 mL | 2.4423 mL | |
| 5 mM | 0.0488 mL | 0.2442 mL | 0.4885 mL | |
| 10 mM | 0.0244 mL | 0.1221 mL | 0.2442 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
