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for ALS and Alzheimer's Disease Research

In recent reports, Glutamate released by activated microglia induces excitotoxic neuronal death, which likely contributes to non-cell autonomous neuronal death in neurodegenerative diseases, such as amyotrophic lateral sclerosis (ALSjand Alzheimer's disease.
INI-0602 is a novel blood-brain barrier permeable gap junction hemichannel blocker, that effectively inhibits neurotoxic microglial glutamate release.

C37H52INO5 = 717.72
Purity: ≥ 98.0%
Solubility: DMSO
CAS No.: 1204185-14-7

  1. Features
  2. Data1: Effects on INI-0602 on microglial glutamate release and neuronal death
  3. Data2: Amelioration effect on symptom in ALS mouse models
  4. Product List
  5. Related Product
  6. Reference
  7. Leaflet   (1.8 MB / 2P)

1. Features

  • Blood-brain barrier permeable.
  • Inhibits neurotoxic microglial glutamate release and excitotoxic neuronal death of cultured mouse primary neurons in microglia-conditioned media (in vitro).
  • Ameliorates disease symptoms in ALS and AD mouse models (in vivo).

2. Data 1: Effect of INI-0602 on microglial glutamate release and neuronal death

Fluorescent microscopic images
Fig.A: Fluorescent microscopic images of live/dead staining of mouse primary cortical neuron cultures in microglia-conditioned media.

Neurons in microglia-conditioned media containing 1 μg/mL LPS (LPS) underwent cell death with neuritic beading, whereas neurons in microglia-conditioned media containing PBS (PBS), 1 μg/ml LPS plus 100 μM CBX (100 μM CBX), or 1 μg/ml LPS plus 100 μM INI-0602 (100 μM INI-0602) appeared healthy. Green, neuron (MAP2); red, dead cell (PI); blue, nucleus (Hoechst). Scalebar, 20 μm.

Glutamate concentrations in media
Fig.B: Glutamate concentrations in media

StremSureTM Colonyformation
Fig.C: The percentages of dead neurons.
Data represent the means ±SD

(n = 6 per group)

Fig.A-C indicates INI-0602 significantly suppressed lipopolysaccharide (LPS)-induced glutamate release from microglia and subsequent excitotoxic neuronal death in a dose-dependent manner.
∗ CBX: Carbenoxolone is an existing gap junction blocker, but hardly penetrates blood-brain barrier.

Data is referred from Takeuchi, H. et al.: PLoS ONE., 6, e21108 (2011).

3. Data 2: Amelioration effect on symptom in ALS mouse models

20-week-old SOD1 F93A Tg mouse
Fig. D:
A representative photograph of 20-week-old SOD1 G93A Tg mice treated with PBS (left) or 10 mg/kg INI-0602 (right).

This showed obvious differences in body size, muscular atrophy, and kyphosis.
20-week-old SOD1 F93A Tg mouse
Fig. E: Survival rates of SOD1 G93A Tg mice (n=24 per group)
Treatment with INI-0602 significantly prolonged the lifespans of the SOD1 G93A Tg mice

Data is referred from Takeuchi, H. et al.: PLoS ONE., 6, e21108 (2011).

4. Product List
Product Name Grade Package Size Wako Catalog No. Storage Condition
INI-0602, 98.0+ % (HPLC) for Cellbiology 1 mg 097-06511
5 mg 093-06513
5. Related Products
Product Name Grade Package Size Wako Catalog No. Note
6-Diazo-5-oxo-L-norleucine, 98.0+ % (HPLC) for Cellbiology 5 mg 045-32441 an antibiotic with antitumor and enzyme inhibiting properties
25 mg 041-32443
Products listed in this page are for research use only.   Do not administer each to human.

6. Reference
Takeuchi, H. et al.: "Blockade of Gap Junction Hemichannel Suppresses Disease Progression in Mouse Models of Amyotrophic Lateral Sclerosis and Alzheimerfs Disease", PLoS ONE., 6, e21108 (2011)

7. Leaflet
Leaflet   (1.8 MB / 2P)

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