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Cat. No.: HY-175822

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5-HT2A inverse agonist-1

5-HT2A inverse agonist-1 is a 5-HT_2A receptor inverse agonist with a IC₅₀ of 5.5 nM. 5-HT2A inverse agonist-1 shows minimal hERG inhibition. 5-HT2A inverse agonist-1 can be used for the research of neurological disease, such as Parkinson’s disease.

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

CAS No.: 3028943-38-3
Formula: C₂₂H₂₅F₅N₄O₂
Molecular Weight:472.45

Storage:

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

Data Sheet (268 KB)

5-HT2A inverse agonist-1 Chemical Structure

CAS No.: 3028943-38-3

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Use of MCE Products

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

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

Biological Activity

Description

IC₅₀ & Target^[1]

5-HT_2A Receptor

5.5 nM (IC₅₀)

All 5-HT Receptor Isoforms :

Parmacokinetics

Species	Dose	Route	T_max	T_1/2	C_max	AUC_last	V_z	MRT	CL	F
Rat^[1]	23.3 μmol/Kg	i.g.	5.3 h	2.5 h	0.141 μM	1.346 μM/L·h	61.1 L/kg	6.5 h	17.5 L/h/kg	/
Rat^[1]	5.83 μmol/Kg	i.v.	/	1.5 h	0.3 μM	0.537 μM/L·h	23.4 L/kg	2 h	11.4 L/h/kg	62.6 %

In Vivo

5-HT2A inverse agonist-1 (Compound P25a) (0.47-4.27 μmol/kg, i.g.) attenuates head twitches in DOI-induced head twitches rats models^[1].
5-HT2A inverse agonist-1 (0.51-5.1 μmol/kg, i.g.) decreases activity distance in MK801 (HY-15084B)-induced hyperactivity rats models^[1].

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

Animal Model:

DOI-induced head twitches rats models^[1]
Dosage:

0.47, 1.41, 4.27 μmol/kg
Administration:

Orally gavage
Result:

Reduced numbers of head twitches.

Animal Model:

MK801-induced hyperactivity rats models^[1]
Dosage:

0.51, 1.7 and 5.1 μmol/kg
Administration:

Orally gavage
Result:

Decreases activity distance.

Chemical Information

CAS No. 3028943-38-3
Molecular Weight 472.45
Formula C₂₂H₂₅F₅N₄O₂
SMILES

FC(C=C1)=CC=C1CN([C@@H]2[C@@H](CN(CC2)C)F)C(NCC3=CN=C(OCC(F)(F)F)C=C3)=O
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 (268 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]. Ma M, et al. Synthesis and evaluation of novel 5-HT2A receptor inverse agonist with excellent in vivo antipsychotic efficacy and superior tissue distribution for treatment of Parkinson's disease psychosis. Eur J Med Chem. 2025 Nov 15;298:118044. [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.

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MOQ

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100 mg

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

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5-HT2A inverse agonist-1

All 5-HT Receptor Isoforms