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Cat. No.: HY-182389

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NLX-219

NLX-219 is a selective agonist of the 5-HT_1A with a pK_i of 10.21. NLX-219 activates ERK1/2 phosphorylation, inhibits adenylyl cyclase activity, promotes β-arrestin recruitment. NLX-219 can be used for the research of neurological disease.

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

CAS No.: 2170404-93-8
Formula: C₂₁H₂₃ClF₂N₂O₂
Molecular Weight:408.87

Storage:

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

NLX-219 Chemical Structure

CAS No.: 2170404-93-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
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Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

5-HT_1A Receptor

10.21 (pKi)

α1-adrenergic receptor

6.29 (pKi)

ERK1

ERK2

All 5-HT Receptor Isoforms :

All Adrenergic Receptor Isoforms :

All ERK Isoforms :

All Arrestin Isoforms :

In Vitro

NLX-219 (Compound 3) binds with high affinity to CHO-K1 cell-expressed human 5-HT₁A receptors (pK_i = 10.21) and α₁ adrenergic receptors (pK_i = 6.29), with no significant D₂ dopamine receptor affinity^[1].
NLX-219 fully activates ERK1/2 phosphorylation in CHO-K1 cell-expressed human 5-HT₁A receptors with a pEC₅₀ of 9.10^[1].
NLX-219 fully inhibits adenylyl cyclase activity via CHO-K1 cell-expressed human 5-HT₁A receptors with a pEC₅₀ of 8.09^[1].
NLX-219 fully promotes β-arrestin recruitment to U2OS cell-expressed human 5-HT₁A receptors with a pEC₅₀ of 7.98^[1].
NLX-219 fully triggers calcium mobilization in CHO-K1 cell-expressed human 5-HT₁A receptors with a pEC₅₀ of 7.20^[1].

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

Chemical Information

CAS No. 2170404-93-8
Molecular Weight 408.87
Formula C₂₁H₂₃ClF₂N₂O₂
SMILES

O=C(N1CCC(CNCCOC2=CC=CC=C2)(CC1)F)C3=CC=C(C(Cl)=C3)F
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

Handling Instructions (2659 KB)

References

[1]. Sniecikowska J, et al. Discovery of Novel pERK1/2- or β-Arrestin-Preferring 5-HT_1A Receptor-Biased Agonists: Diversified Therapeutic-like versus Side Effect Profile. J Med Chem. 2020;63(19):10946-10971. [Content Brief]

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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.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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NLX-219

All 5-HT Receptor Isoforms

All Adrenergic Receptor Isoforms

All ERK Isoforms

All Arrestin Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

NLX-219 Related Classifications

HY-182389 Related Classifications