| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Y1 receptor (IC50 = 3.8 nM for displacing [125I-Tyr36]NPY in SK-N-MC cells; Kd = 5.5 nM in saturation binding) [1]
NPY Y1 receptor (agonist) [2] |
|---|---|
| ln Vitro |
In SK-N-MC cells (expressing Y1 receptors), [Leu31,Pro34]Neuropeptide Y (porcine) displaced [125I-Tyr36]monoiodo-NPY with an IC50 of 3.8 nM, almost equipotent to NPY. In SMS-KAN cells (expressing Y2 receptors), it was approximately 1000-fold less potent (IC50 > 100 nM). Saturation binding using [125I-Tyr36]monoiodo-[Leu31,Pro34]Neuropeptide Y (porcine) gave a Kd of 5.5 nM and Bmax of 2.3×10^5 sites per cell on SK-N-MC cells. [1]
In SK-N-MC cells loaded with Fura-2, [Leu31,Pro34]Neuropeptide Y (porcine) (100 nM) caused a transient increase in cytoplasmic free calcium concentration ([Ca2+]i), similar to NPY, whereas the C-terminal fragment NPY-(16-36) had no effect. [1] |
| ln Vivo |
[Leu31,Pro34]-Neuropeptide Y (pig) substitutes radiolabeled NPY in a variety of human neuroblastoma cell lines and rat PC-12 cells expressing Y1 receptors [1].
In anesthetized rats, intravenous administration of [Leu31,Pro34]Neuropeptide Y (porcine) (0.25, 2.5, 25 nmol/kg) produced a dose-dependent increase in arterial blood pressure. It was approximately 5 times more potent than NPY in causing vasoconstriction (P < 0.05 at 0.25 and 2.5 nmol/kg). A parallel decrease in heart rate was observed. At the highest dose (25 nmol/kg), a brief increase in blood pressure was followed by a prolonged hypotension. [1] In rats, unilateral intra-amygdala injection of [Leu31,Pro34]Neuropeptide Y (porcine) (5 and 10 nM) significantly increased the percentage of time spent and number of entries into open arms in the elevated plus maze (EPM) test, indicating anxiolytic-like effects. These effects were reversed by prior administration of α-MSH (250 ng) and were synergistic with subeffective doses of the MC4-R antagonist HS014 (1 nM). No significant effect on closed arm entries was observed, ruling out locomotor changes. [2] |
| Enzyme Assay |
Receptor binding assays were performed using human neuroblastoma cell lines (SK-N-MC for Y1, SMS-KAN for Y2) and rat PC-12 cells. Cells were preincubated for 2 days in poly(Lys-Ala)-coated 6-well plates. For competition binding, 1.2×10^6 cells per well were incubated with 50,000 cpm of radioligand ([125I-Tyr36]monoiodo-NPY or [125I-Tyr36]monoiodo-[Leu31,Pro34]Neuropeptide Y (porcine), specific activity ≈1900 Ci/mmol) and various concentrations of unlabeled peptides in a final volume of 1 ml at 37°C for 60 min. Nonspecific binding was determined in the presence of 1 μM NPY. After incubation, cells were washed three times with cold buffer, lysed with 0.5 M NaOH, and counted. IC50 values were calculated from displacement curves. For saturation binding, a radioligand with low specific activity (18 Ci/fmol) was used. The dissociation constant (Kd) was calculated to be 5.5 nM. [1]
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| Cell Assay |
Intracellular calcium concentration ([Ca2+]i) was measured using the fluorescent probe Fura-2. SK-N-MC cells were harvested, washed, and resuspended at 3×10^6 cells/ml. Fura-2 acetoxymethyl ester was added to a final concentration of 2.5 μM from a 1 mM stock in dimethyl sulfoxide, and cells were incubated for 30 min in the dark at room temperature. After centrifugation, cells were resuspended in Hepes buffer (145 mM NaCl, 5 mM KCl, 1 mM MgSO4, 10 mM glucose, 10 mM Hepes, pH 7.4) containing 150 mg/L bovine serum albumin at a concentration of 2.5×10^6 cells/ml. Fura-2 fluorescence was measured in a spectrofluorometer with excitation at 340 nm and emission at 500 nm, with cells kept in suspension by gentle stirring at 37°C. [Ca2+]i was calculated according to the method of Grykiewicz et al. [1]
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| Animal Protocol |
[1] Animal Protocol: Non-fasted female Sprague-Dawley rats (190-210 g) were anesthetized with sodium pentobarbital. A catheter was placed in the right jugular vein for intravenous administration of test compounds. A second catheter in the carotid artery was connected to a blood pressure transducer. The trachea was cannulated to facilitate respiration. Blood pressure and heart rate were continuously recorded. After cardiovascular stabilization, each rat received consecutive doses of 0.25, 2.5, and 25 nmol/kg of peptide at 10-min intervals. When [Leu31,Pro34]Neuropeptide Y (porcine) was tested, an additional administration of NPY (2.5 nmol/kg) was given at the end. Peptides were dissolved in 1 mM acetic acid and diluted in 0.05 M sodium phosphate buffer immediately before injection to obtain a dose volume of 1 ml/kg. [1][2] Animal Protocol: Male Sprague-Dawley rats (220-250 g) were anesthetized with thiopental sodium (40 mg/kg i.p.) and fixed in a stereotaxic apparatus. A permanent 22-gauge stainless steel guide cannula was implanted unilaterally into the right amygdala using coordinates: 2.3 mm posterior, 4.5 mm lateral to midline, and 8.0 mm ventral to bregma. The cannula was secured with dental cement and mounting screws. After 7 days of recovery, rats were habituated to handling. [Leu31,Pro34]Neuropeptide Y (porcine) was dissolved in artificial cerebrospinal fluid (aCSF, pH 7.4, with 0.1% bovine serum albumin) and administered in a volume of 1 μl over 1 min via a 33-gauge microinjection cannula extending 0.5 mm below the guide. The injection cannula was left in place for an additional minute to allow diffusion. Fifteen minutes after the last injection, rats were subjected to the elevated plus maze (EPM) test for 5 min, and the time spent and number of entries into open and closed arms were recorded. [2]
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| References | |
| Additional Infomation |
[Leu31,Pro34]Neuropeptide Y (porcine) is a synthetic NPY analog based on the PP-fold structure. The introduction of proline at position 34 (from pancreatic polypeptide) is considered the crucial structural change responsible for its differential receptor binding. It does not bind to Y2 receptors, unlike NPY-(13-36). This analog is useful for autoradiographic mapping of NPY receptor subtypes and for determining the relative importance of Y1 vs. Y2 receptors in biological effects of NPY. [1]
In the amygdala, [Leu31,Pro34]Neuropeptide Y (porcine) acts as a Y1 receptor agonist to produce anxiolytic-like effects, which are functionally antagonized by α-MSH acting via melanocortin-4 receptors (MC4-R). The anxiolytic action may be due to suppression of endogenous POMC derivative release. Co-administration of subeffective doses of this analog with the MC4-R antagonist HS014 produces synergistic anxiolysis, possibly via convergent inhibition of adenylyl cyclase activity. [2] |
| Molecular Formula |
C190H286N54O56
|
|---|---|
| Molecular Weight |
4222.63208246231
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| Exact Mass |
4222.125
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| CAS # |
125580-28-1
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| PubChem CID |
90479761
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| Appearance |
White to off-white solid powder
|
| LogP |
-14
|
| Hydrogen Bond Donor Count |
61
|
| Hydrogen Bond Acceptor Count |
63
|
| Rotatable Bond Count |
131
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| Heavy Atom Count |
300
|
| Complexity |
10500
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| Defined Atom Stereocenter Count |
37
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| SMILES |
O=C([C@H](CCCCN)NC([C@H](CO)NC([C@@H]1CCCN1C([C@H](CC1C=CC(=CC=1)O)N)=O)=O)=O)N1CCC[C@H]1C(N[C@@H](CC(=O)O)C(N[C@@H](CC(N)=O)C(N1CCC[C@H]1C(NCC(N[C@H](C(N[C@@H](CC(=O)O)C(N[C@@H](C)C(N1CCC[C@H]1C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](CO)C(N[C@@H](C)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(=N)N)C(N[C@@H](CC1=CNC=N1)C(N[C@@H](CC1C=CC(=CC=1)O)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CC(N)=O)C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H]([C@@H](C)O)C(N[C@@H](CCCNC(=N)N)C(N1CCC[C@H]1C(N[C@H](C(N[C@H](C(N)=O)CC1C=CC(=CC=1)O)=O)CCCNC(=N)N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CC1C=CC(=CC=1)O)=O)CC1C=CC(=CC=1)O)=O)CCCNC(=N)N)=O)C)=O)CC(C)C)=O)CC(=O)O)=O)CCC(=O)O)=O)C)=O)=O)=O)=O)CCC(=O)O)=O)=O)=O)=O)=O
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| InChi Key |
ZNBZLZXDILRJJT-CCPZSHQESA-N
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| InChi Code |
InChI=1S/C190H286N54O56/c1-16-96(10)150(180(294)234-130(82-142(193)253)168(282)225-124(74-94(6)7)164(278)226-125(75-95(8)9)171(285)239-151(101(15)247)181(295)221-120(32-22-66-208-190(202)203)185(299)243-70-26-36-140(243)177(291)219-116(31-21-65-207-189(200)201)156(270)222-121(152(195)266)77-103-40-50-109(249)51-41-103)238-172(286)128(80-106-46-56-112(252)57-47-106)229-167(281)129(81-107-87-204-91-210-107)230-158(272)115(30-20-64-206-188(198)199)218-163(277)123(73-93(4)5)223-155(269)98(12)212-173(287)135(89-245)236-166(280)127(79-105-44-54-111(251)55-45-105)228-165(279)126(78-104-42-52-110(250)53-43-104)227-157(271)114(29-19-63-205-187(196)197)216-153(267)97(11)211-161(275)122(72-92(2)3)224-169(283)132(85-148(262)263)232-160(274)118(59-61-146(258)259)217-154(268)99(13)213-176(290)138-34-24-67-240(138)182(296)100(14)214-162(276)131(84-147(260)261)231-159(273)117(58-60-145(256)257)215-144(255)88-209-175(289)137-33-23-69-242(137)186(300)134(83-143(194)254)235-170(284)133(86-149(264)265)233-178(292)141-37-27-71-244(141)184(298)119(28-17-18-62-191)220-174(288)136(90-246)237-179(293)139-35-25-68-241(139)183(297)113(192)76-102-38-48-108(248)49-39-102/h38-57,87,91-101,113-141,150-151,245-252H,16-37,58-86,88-90,191-192H2,1-15H3,(H2,193,253)(H2,194,254)(H2,195,266)(H,204,210)(H,209,289)(H,211,275)(H,212,287)(H,213,290)(H,214,276)(H,215,255)(H,216,267)(H,217,268)(H,218,277)(H,219,291)(H,220,288)(H,221,295)(H,222,270)(H,223,269)(H,224,283)(H,225,282)(H,226,278)(H,227,271)(H,228,279)(H,229,281)(H,230,272)(H,231,273)(H,232,274)(H,233,292)(H,234,294)(H,235,284)(H,236,280)(H,237,293)(H,238,286)(H,239,285)(H,256,257)(H,258,259)(H,260,261)(H,262,263)(H,264,265)(H4,196,197,205)(H4,198,199,206)(H4,200,201,207)(H4,202,203,208)/t96-,97-,98-,99-,100-,101+,113-,114-,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-,150-,151-/m0/s1
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| Chemical Name |
(4S)-4-[[2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-5-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-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-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]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, 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 : ≥ 100 mg/mL (~23.68 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 | 0.2368 mL | 1.1841 mL | 2.3682 mL | |
| 5 mM | 0.0474 mL | 0.2368 mL | 0.4736 mL | |
| 10 mM | 0.0237 mL | 0.1184 mL | 0.2368 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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