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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- Fòrmula: C186H280N54O54·xC2HF3O2
- Peso molecular:4136.54 (free base)
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Almacenamiento:
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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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
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.
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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Peso molecular 4136.54 (free base)
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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)
Pureza y Documentación
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Ficha de datos (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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- Español - ES (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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)
NNC0165-1273 TFA Related Classifications
HY-P11291A Related Classifications
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