914389-14-3

914389-14-3 structure
914389-14-3 structure
  • Name: SMP-028
  • Chemical Name: SMP-028
  • CAS Number: 914389-14-3
  • Molecular Formula: C23H26FN5O2S
  • Molecular Weight: 455.55
  • Catalog: Research Areas Metabolic Disease
  • Create Date: 2019-03-03 15:24:03
  • Modify Date: 2024-01-09 19:39:37
  • SMP-028 is an inhibitor of neutral cholesterol esterase (CEase), with an IC50 of 1.01 μM.

Name SMP-028
Description SMP-028 is an inhibitor of neutral cholesterol esterase (CEase), with an IC50 of 1.01 μM.
Related Catalog
Target

IC50: 1.01 μM (CEase)[1].

In Vitro SMP-028 potently and concentration-dependently inhibits neutral cholesterol esterase (CEase) with an IC50 value of 1.01 μM. On the other hand, inhibition of other steroidogenic enzymes by SMP-028 is weak with IC50 values>10 μM. In particular, SMP-028 does not inhibit acid CEase and only weakly reduces the activity of CYP11A1 (IC50 values>100 μM and 49.8 μM respectively) [1]. SMP-028 at 10 μM or less does not affect the viability of male adrenal cells, female adrenal cells, testicular cells, and ovarian cells. On the other hand, SMP-028 at concentrations higher than 30 μM significantly reduce the viability of male adrenal cells, female adrenal cells [2].
Cell Assay Testicular and ovarian cells from Sprague–Dawley rats are cultured in medium containing SMP-028 dissolved in dimethyl sulfoxide (DMSO) is added to each well of the 96-well cell culture plates. The final concentration of DMSO is 0.1% (v/v) and that of SMP-028 is set between 0.1 μM to 50 μM. The cells with culture medium containing DMSO only (not containing SMP-028) are as a control. The plates are next incubated at 37°C, 5% CO2 in air atmosphere for 24 hours. SMP-028 cytotoxicity is estimated. The luminescence of each plate is measured[2].
References

[1]. Nishizato Y, et al. Translational research into species differences of endocrine toxicity via steroidogenesis inhibition by SMP-028--for human safety in clinical study. Toxicol Appl Pharmacol. 2014 May 1;276(3):213-9.

[2]. Nishizato Y, et al. Effect of SMP-028 on steroidogenesis in rats; mechanism of toxicological events on endocrine organs of rats. Toxicol In Vitro. 2014 Apr;28(3):397-402.

Molecular Formula C23H26FN5O2S
Molecular Weight 455.55