1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. nAChR
  3. 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.

nAChR antagonist 3

nAChR antagonist 3 Chemical Structure

CAS No. : 3114746-65-2

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Description

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[1].

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 T1/2 Tmax Cmax AUC0-t MRT Bioavailability CL Vss
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.
Molecular Weight

431.17

Formula

C16H21Br2N3O

CAS No.
SMILES

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

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Purity & Documentation
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    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.

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Product Name:
nAChR antagonist 3
Cat. No.:
HY-182010
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