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Cat. No.: HY-182010

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nAChR antagonist 3

nAChR antagonist 3 is a selective α7 nAChR antagonist with an IC₅₀ of 0.86 μM. nAChR antagonist 3 exerts a protective effect against paraoxon-induced toxicity. nAChR antagonist 3 can be used for the research of organophosphate poisoning.

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

CAS No.: 3114746-65-2
Formula: C₁₆H₂₁Br₂N₃O
Molecular Weight:431.17

Storage:

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

nAChR antagonist 3 Chemical Structure

CAS No.: 3114746-65-2

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

Biological Activity

Description

In Vitro

nAChR antagonist 3 (Compound YZ4) (3-30 μM; 24 h) exerts significant dose-dependent cytoprotective effects on HT22 cells treated with the organophosphorus pesticide Paraoxon^[1].

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

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	MRT	Bioavailability	CL	V_ss
Mice^[1]	3 mg/kg	i.v.	2.63 h	0.08 h	120.35 ng/mL	443.85 ng·h/mL	3.80 h	/	7.63 L/h/kg	28.97 L/kg
Mice^[1]	10 mg/kg	i.g.	3.92 h	0.5 h	176.54 ng/mL	1372.77 ng·h/mL	5.96 h	92.77 %	/	/

In Vivo

nAChR antagonist 3 (Compound YZ4) (3 mg/kg; intravenous injection; single administration) exhibits a rescue effect against organophosphate poisoning in mice^[1].

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

Animal Model:

Male BALB/c mice, aged 6-8 weeks and weighing approximately 20 g^[1]
Dosage:

3 mg/kg
Administration:

i.v., single dose
Result:

Significantly reduced the epilepsy score and improve neurological symptoms.
Significantly alleviated the pathological damage of the liver, lungs and brain tissues, reduce the injury score, and restore the tissue structure.

Chemical Information

CAS No. 3114746-65-2
Molecular Weight 431.17
Formula C₁₆H₂₁Br₂N₃O
SMILES

CC(C)(N1CCC2(CC1)NC(C3=CC(Br)=CC(Br)=C3)=NO2)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

Handling Instructions (2659 KB)

References

[1]. Zhang H, et al. Discovery of Potent and Subtype-Selective α7 nAChR Antagonists for Organophosphate Poisoning Protection. J Med Chem. 2026;69(5):6138-6157. [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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