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Art. -Nr.: HY-P11291B

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NNC0165-1273 acetate

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NNC0165-1273 acetate is a selective NPY Y2 receptor agonist with a K_i of 2 nM and an EC₅₀ of 5.0 nM. NNC0165-1273 acetate blocks Ghrelin-induced cFos expression. NNC0165-1273 acetate reduces nocturnal food intake, attenuates feeding behavior, induces early satiety, and causes dose-dependent decreases in body weight and fat mass in diet-induced obese mice. When used in combination with Semaglutide (HY-114118), NNC0165-1273 acetate reduces preference for high-fat diet, promotes body weight loss, and produces sustained weight loss effects in diet-induced obese rats. NNC0165-1273 acetate can be used in studies related to diet-induced obesity.

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Formel: C₁₈₆H₂₈₀N₅₄O₅₄·xC₂H₄O₂
Molecular Weight:4136.54 (free base)

Speicherung:

Sealed storage, away from moisture.

Powder -80°C, 2 years , -20°C, 1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Kundenspezifische Peptidsynthese

NNC0165-1273 acetate Chemical Structure

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Menge

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[2]

NPY Y₂ receptor

2 nM (Ki)

Alle Neuropeptide Y Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

NNC0165-1273 acetate exhibits high selectivity for the Y2 receptor (>5000-fold over the Y1 receptor, 1250-fold over the Y4 receptor, and 650-fold over the Y5 receptor)^[1].
NNC0165-1273 acetate is a highly selective Y2 receptor agonist, with a binding K_i of 2.0 nM and a functional EC₅₀ of 5.0 nM for the Y2 receptor, and exhibits low activity against Y1, Y4 and Y5 receptors^[2].
The in vitro half-life of NNC0165-1273 acetate (570 min) is 2.85 times longer than that of PYY_3-36, indicating greater metabolic stability^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

NNC0165-1273 (0.03-1 μmol/kg/d; subcutaneous injection; continuous infusion; 14 days) acetate causes dose-dependent reductions in food intake, body weight, and fat mass in diet-induced obese male C57BL/6 mice, with the highest dose reducing fat mass by approximately 31%^[1].
NNC0165-1273 (0.04-1 μmol/kg; subcutaneous injection; single administration) acetate potently inhibits ghrelin-induced feeding behavior in healthy male C57BL/6 mice, with the 0.04 μmol/kg dose almost completely blocking the orexigenic effect of ghrelin at 1 and 2 hours^[1].
Combined administration of NNC0165-1273 (0.08 µmol/kg/d; osmotic minipump; continuous infusion) acetate and Semaglutide achieves a maximum body weight loss of 23.9% in diet-induced obese male Wistar rats, an effect superior to that observed with Roux-en-Y gastric bypass surgery in previous studies^[3].
Co-administration of NNC0165-1273 (0.04 µmol/kg/d; subcutaneous injection; continuous administration) acetate, NNC0165-0020 and Semaglutide (HY-114118) reduces the body weight of male Wistar rats with high-fat diet-induced obesity by a maximum of 20.5% and persistently decreases their preference for high-fat diet^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6 (male, adult, acclimated to handling for 2 weeks, singly housed)^[1]
Dosage:

0.0016 μmol/kg; 0.008 μmol/kg; 0.04 μmol/kg; 0.2 μmol/kg; 1 μmol/kg
Administration:

s.c.; single injection
Result:

Produced substantial reductions in food intake at 2 and 4 hours post-injection at doses of 0.04, 0.2, 1 μmol/kg.
Significantly reduced food intake at 2 hours at 0.008 μmol/kg dose, whereas PYY3-36 required a 0.04 μmol/kg dose to achieve a similar reduction.
Reduced food intake to ~2.7 g vs ~3.3 g in vehicle controls at 14 hours at 1 μmol/kg dose.

Animal Model:

Wistar rats (male, diet-induced obese via 8-week high-fat (45%) and high-fructose diet)^[3]
Dosage:

0.08 µmol/kg/d
Administration:

osmotic minipump; continuous delivery
Result:

Produced a maximum body weight loss of 23.9% when administered in combination with semaglutide, which was superior to semaglutide monotherapy and saline treatment, and more effective than Roux-en-Y gastric bypass surgery in a prior comparable study.
Led to a strong decrease in high-fat diet preference when administered in combination with semaglutide.

Chemical Information

Appearance Solid
Molecular Weight 4136.54 (free base)
Formel C₁₈₆H₂₈₀N₅₄O₅₄·xC₂H₄O₂
Sequence

Ile-Lys-Pro-Glu-Ala-Pro-Gly-Glu-Asp-Ala-Ser-Pro-Glu-Glu-Leu-Asn-Arg-Tyr-Tyr-Ala-Ser-Leu-Arg-His-Tyr-Leu-Asn-Trp-Val-Thr-Arg-Gln-{β-homoArg}-Tyr-NH2
Sequence Shortening

IKPEAPGEDASPEELNRYYASLRHYLNWVTRQ-{β-homoArg}-Y-NH2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 2 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Jones ES, et al. Modified Peptide YY Molecule Attenuates the Activity of NPY/AgRP Neurons and Reduces Food Intake in Male Mice. Endocrinology. 2019 Nov 01;160(11):2737-2747. [Content Brief]

[2]. Oertel M, et al. GLP-1 and PYY for the treatment of obesity: a pilot study on the use of agonists and antagonists in diet-induced rats. Endocrine connections. 2024 Mar 01;13(3):e230398.

[3]. Oertel M, et al. Effects of a combinatory treatment with semaglutide and a NPY Y2 receptor selective PYY 3-36 analogue in diet-induced obese rats: surpassing bariatric surgery?[C]//Endocrine Abstracts. Bioscientifica, 2023, 90.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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NNC0165-1273 acetate

Alle Neuropeptide Y Receptor Isoform-spezifische Produkte anzeigen