1. NF-κB Apoptosis
  2. Keap1-Nrf2 Apoptosis Caspase
  3. Nrf2 activator-21

Nrf2 activator-21 is a Nrf2 activator with dual antioxidant and neuroprotective properties. Nrf2 activator-21 binds to Keap1 Kelch domain and disrupts Keap1-Nrf2 interactions and activate antioxidant defense mechanisms. Nrf2 activator-21 reduces apoptosis and decreases caspase-3 activity in the hippocampal neurons. Nrf2 activator-21 targets cerebral ischemia/reperfusion injury (CIRI) via Nrf2 pathway activation. Nrf2 activator-21 improves neurological function, alleviates anxiety-like behavior, enhances memory in rats with 2-vessel occlusion (2VO)-induced CIRI. Nrf2 activator-21 can be used for the study of cerebral ischemia/reperfusion injury.

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Nrf2 activator-21

Nrf2 activator-21 Chemical Structure

CAS No. : 1912404-14-8

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Description

Nrf2 activator-21 is a Nrf2 activator with dual antioxidant and neuroprotective properties. Nrf2 activator-21 binds to Keap1 Kelch domain and disrupts Keap1-Nrf2 interactions and activate antioxidant defense mechanisms. Nrf2 activator-21 reduces apoptosis and decreases caspase-3 activity in the hippocampal neurons. Nrf2 activator-21 targets cerebral ischemia/reperfusion injury (CIRI) via Nrf2 pathway activation. Nrf2 activator-21 improves neurological function, alleviates anxiety-like behavior, enhances memory in rats with 2-vessel occlusion (2VO)-induced CIRI. Nrf2 activator-21 can be used for the study of cerebral ischemia/reperfusion injury[1].

In Vitro

Nrf2 activator-21 (Compound 7I) (1-15 μM, 24 h) significantly improves the viability of hippocampal neuronal cells exposed to H2O2[1].
Nrf2 activator-21 (2.5 μM, 24 h) reduces apoptosis and decreases caspase-3 activity in the hippocampal neurons[1].

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

Apoptosis Analysis[1]

Cell Line: hippocampal neurons
Concentration: 2.5 μM
Incubation Time: 24 h
Result: Reduced apoptosis and decreased caspase-3 activity in the hippocampal neurons.
In Vivo

Nrf2 activator-21 (Compound 7I) (15 mg/kg, i.p., once, 15 min post-reperfusion) significantly improves neurological function in male adult Wistar rats with 2-vessel occlusion (2VO)-induced cerebral ischemia/reperfusion injury[1].

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

Animal Model: Male adult Wistar rats: a midline neck incision was made to isolate bilateral common carotid arteries, which were then clamped simultaneously for 15 min to induce cerebral ischemia, followed by 15 min of reperfusion to establish the 2-vessel occlusion (2VO) cerebral ischemia/reperfusion injury model[1]
Dosage: 15 mg/kg
Administration: i.p. once 15 min post-reperfusion
Result: Achieved significant improvements in motor function, sensory response, and wire cage climbing ability, with total neurological deficit scores notably reduced in 2VO model rats.
Showed alleviation of anxiety-like behavior.
Improved memory function, with the discrimination index significantly increased in the Novel Object Recognition Test, reversing memory deficits induced by cerebral ischemia/reperfusion injury .
Preserved hippocampal CA1 neuron morphology and reduced the number of degenerated dark neurons and decreased hippocampal caspase-3 activity.
Increased hippocampal Nrf2 protein expression, restored SOD and CAT activities to near-sham levels and reduced MDA levels .
Upregulated hippocampal BDNF and TrkB receptor levels and enhanced neuroprotective signaling.
Molecular Weight

322.31

Formula

C19H14O5

CAS No.
SMILES

COC1=CC=C2C(OC(C(C(/C=C/C3=CC=C(O)C=C3)=O)=C2)=O)=C1

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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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Nrf2 activator-21
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HY-175548
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