NNC0165-1273 TFA
NNC0165-1273 TFA is a selective NPY Y2 receptor agonist with a Ki of 2 nM and an EC50 of 5.0 nM. NNC0165-1273 TFA blocks Ghrelin-induced cFos expression. NNC0165-1273 TFA 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 TFA reduces preference for high-fat diet, promotes body weight loss, and produces sustained weight loss effects in diet-induced obese rats. NNC0165-1273 TFA can be used in studies related to diet-induced obesity.
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- Formule: C186H280N54O54·xC2HF3O2
- Masse moléculaire:4136.54 (free base)
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Stockage:
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)
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Activité biologique
Description
IC50 & Target
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NPY Y2 receptor 2 nM (Ki) |
In Vitro
NNC0165-1273 TFA 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 TFA is a highly selective Y2 receptor agonist, with a binding Ki 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 TFA (570 min) is 2.85 times longer than that of PYY3-36, indicating greater metabolic stability[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
NNC0165-1273 (0.04-1 μmol/kg; subcutaneous injection; single administration) TFA 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) TFA 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) TFA, 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.
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Animal Model:C57BL/6 (male, adult, acclimated to handling for 2 weeks, singly housed)[1]
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Dosage:0.0016 μmol/kg; 0.008 μmol/kg; 0.04 μmol/kg; 0.2 μmol/kg; 1 μmol/kg
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Administration:s.c.; single injection
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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.
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Animal Model:Wistar rats (male, diet-induced obese via 8-week high-fat (45%) and high-fructose diet)[3]
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Dosage:0.08 µmol/kg/d
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Administration:osmotic minipump; continuous delivery
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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
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Appearance Solid
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Masse moléculaire 4136.54 (free base)
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Formule C186H280N54O54·xC2HF3O2
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Color White to off-white
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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
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Sequence Shortening
IKPEAPGEDASPEELNRYYASLRHYLNWVTRQ-{β-homoArg}-Y-NH2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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)
Protocole
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Pureté et documentation
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Fiche technique (305 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)