SMP-028
SMP-028 is an inhibitor of neutral cholesterol esterase (CEase), with an IC50 of 1.01 μM.
For research use only. We do not sell to patients.
- CAS No.: 914389-14-3
- Formula: C23H26FN5O2S
- Molecular Weight:455.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 1.01 μM (CEase)[1].
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 914389-14-3
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Molecular Weight 455.55
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Formula C23H26FN5O2S
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SMILES
O=C(NC)NCCN1/C(SC=C1C2=CC=C(N3CCOCC3)C=C2)=N/C4=CC=CC(F)=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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