SMP-028 |
カタログ番号GC31543
One-Click Copy Product Info
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SMP-028 は中性コレステロールエステラーゼ (CEase) の阻害剤で、IC50 は 1.01 μM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 914389-14-3
Sample solution is provided at 25 µL, 10mM.
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SMP-028 is an inhibitor of neutral cholesterol esterase (CEase), with an IC50 of 1.01 μM.
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].
[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.
Cell experiment: | 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. | |
| Cas No. | 914389-14-3 | SDF | |
| Canonical SMILES | O=C(NC)NCCN1/C(SC=C1C2=CC=C(N3CCOCC3)C=C2)=N/C4=CC=CC(F)=C4 | ||
| Formula | C23H26FN5O2S | M.Wt | 455.55 |
| 溶解度 | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1951 mL | 10.9757 mL | 21.9515 mL |
| 5 mM | 439 μL | 2.1951 mL | 4.3903 mL |
| 10 mM | 219.5 μL | 1.0976 mL | 2.1951 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)