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NPY Y2 antagonist 2

NPY Y2 antagonist 2 is a modulator targeting the neuropeptide Y (NPY) receptor Y2, with pK_i 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.

For research use only. We do not sell to patients.

CAS No.: 1262495-12-4
Formula: C₂₇H₃₃ClF₃N₅O
Molecular Weight:536.04

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

NPY Y2 antagonist 2 Chemical Structure

CAS No.: 1262495-12-4

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

human Y₂ receptor

6.8 nM (pKi)

rat Y₂ receptor

7.2 nM (pKi)

NPY Y₁ receptor

All Neuropeptide Y Receptor Isoforms :

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.

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 (C_max) in the brain was 73 ng/g, and the C_max in the blood was 32 ng/mL, demonstrating its ability to distribute into the central nervous system.

Chemical Information

CAS No. 1262495-12-4
Molecular Weight 536.04
Formula C₂₇H₃₃ClF₃N₅O
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Mittapalli GK, et al. Ligands of the neuropeptide Y Y2 receptor. Bioorg Med Chem Lett. 2014;24(2):430-441. [Content Brief]

Calculators

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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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