| Hazard Information | Back Directory | [Uses]
M109S is a novel small molecule protecting cells from mitochondria-dependent apoptosis both in vitro and in vivo. M109S has the potential to become a research tool for studying cell death mechanisms and to develop therapeutics targeting mitochondria-dependent cell death pathway. M109S has orally bioactivity with excellent brain permeability[1]. | [in vivo]
M109S (10mg/kg p.o., three time in 48 h) protects the retina from the bright-light-induced photoreceptor death[1].
M109S (1 mg/kg, i.p., i.v., 5 mg/kg, o.p. 10 mg/kg 1 time) is an orally bioactive cell death inhibitor penetrating blood-brain/retina-barrier[1].
| Animal Model: | Abca4-/-Rdh8-/- mice | | Dosage: | 10 mg/kg | | Administration: | Oral Gavage (p.o.) | | Result: | Comparing to mice with M109S, the number of AF spots was similar to that detected in the dark-adapted mice. |
| Animal Model: | Mice and Rat | | Dosage: | Intraperitoneal injection (i.p., 1 mg/kg), Intravenous injection (i.v., 5 mg/kg), or Oral gavage (p.o., 10 mg/kg) | | Administration: | Intraperitoneal injection (i.p.), Intravenous injection (i.v.), or Oral gavage (p.o.). | | Result: | Showed plasma concentration reached 1.0 mg/mL (2.6 mM) within 30 min from p.o. in mice, and it remained at 596± 134 ng/mL (1.6±0.36 mM) after 24 h, the same as in rat. Plasmic M109S was 565.3±188.3 nM in rats, and 171.0±52.0 nM in retina, 222.7±74.7 nM in brain, respectively. |
| [IC 50]
caspase-3: 23.4 nM (EC50); Caspase 3: 23.4 nM (EC50) | [References]
[1] Mieko Matsuyama, et al. Development of novel cytoprotective small compounds inhibiting mitochondria-dependent cell death. Science 26, 107916, October 20, 2023 |
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