2. GPCR/G Protein Neuronal Signaling
  3. Neuropeptide Y Receptor
  4. NPY Y2 antagonist 2

NPY Y2 antagonist 2 is a modulator targeting the neuropeptide Y (NPY) receptor Y2, with pKi values of 6.8 nM and 7.2 nM in human and rat brains, respectively, and demonstrating blood-brain barrier penetration. NPY Y2 antagonist 2 shows selectivity for the Y1 and Y5 receptors. NPY Y2 antagonist 2 blocks the negative feedback regulation mediated by the NPY Y2 receptor, thereby increasing endogenous NPY release and enhancing Y1 receptor activation, resulting in the modulation of central neurotransmitter release. NPY Y2 antagonist 2 exhibits moderate in vivo clearance, high free fraction in rat brain, and a favorable brain/plasma ratio and brain exposure. NPY Y2 antagonist 2 is applicable for research in conditions such as mood disorders, anxiety induced by alcohol withdrawal, and social anxiety associated with nicotine withdrawal.

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NPY Y2 antagonist 2

NPY Y2 antagonist 2 Chemical Structure

CAS No. : 1262495-12-4

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NPY Y2 antagonist 2 Related Antibodies

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Description

NPY Y2 antagonist 2 is a modulator targeting the neuropeptide Y (NPY) receptor Y2, with pKi values of 6.8 nM and 7.2 nM in human and rat brains, respectively, and demonstrating blood-brain barrier penetration. NPY Y2 antagonist 2 shows selectivity for the Y1 and Y5 receptors. NPY Y2 antagonist 2 blocks the negative feedback regulation mediated by the NPY Y2 receptor, thereby increasing endogenous NPY release and enhancing Y1 receptor activation, resulting in the modulation of central neurotransmitter release. NPY Y2 antagonist 2 exhibits moderate in vivo clearance, high free fraction in rat brain, and a favorable brain/plasma ratio and brain exposure. NPY Y2 antagonist 2 is applicable for research in conditions such as mood disorders, anxiety induced by alcohol withdrawal, and social anxiety associated with nicotine withdrawal[1].

IC50 & Target

human Y2 receptor

6.8 nM (pKi)

rat Y2 receptor

7.2 nM (pKi)

NPY Y1 receptor

 

In Vitro

NPY Y2 antagonist 2 (compound 149) exhibits moderate hepatic microsomal clearance (rat: 1.8 mL/min/g, human: 0.8 mL/min/g) and 97.2% brain penetration in rat blood-brain barrier binding in in vitro physicochemical and metabolic stability studies[1].

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

NPY Y2 antagonist 2 Related Antibodies
Parmacokinetics
Species Dose Route Plasma Concentration Brain Concentration Brain-to-Plasma Ratio
Rat[1] 2 mg/kg s.c. 32 ng/g 73 ng/g 2.3
In Vivo

NPY Y2 antagonist 2 (compound 149) (2 mg/kg; s.c.; single dose) exhibits good brain penetration and exposure in rats after a single subcutaneous dose of 2 mg/kg, with a brain-to-blood ratio of 2.3 at 1 hour, a maximum brain concentration of 73 ng/g, and a maximum blood concentration of 32 ng/mL[1].

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

Animal Model: rats (specific strain not reported)[1]
Dosage: 2 mg/kg
Administration: s.c.; single dose
Result: Effectively penetrated the blood-brain barrier, with a brain/blood ratio of 2.3 at 1 hour post-administration.
The maximum concentration (Cmax) in the brain was 73 ng/g, and the Cmax in the blood was 32 ng/mL, demonstrating its ability to distribute into the central nervous system.
Molecular Weight

536.04

Formula

C27H33ClF3N5O
CAS No.
SMILES

O=C(NC1=CC=C(C(Cl)=C1)N2CCC3(CN(CC3)CC4CC4)CC2)C(C5=NC=CC(=N5)C(F)(F)F)(C)C
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NPY Y2 antagonist 2 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NPY Y2 antagonist 21262495-12-4Neuropeptide Y ReceptorNPY receptorratY2 receptorY5 receptorsblood-brain barrierCYP isoformsanimal modelsneurological diseaseNeuropeptide Y Y2 receptorY1 receptorshumanInhibitorinhibitorinhibit

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