YM17E |
Catalog No.GC31443
One-Click Copy Product Info
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YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 124900-72-7
Sample solution is provided at 25 µL, 10mM.
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YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro.
YM17E is as potent in inhibiting ACAT activity in the liver as in the intestine, with IC50 values of 45 and 34 nM, respectively[2].
YM17E (3, 10 and 30 mg/kg per day, p.o.) decreases total cholesterol, cholesteryl ester and non-HDL cholesterol in a dose-dependent manner. Total cholesterol and cholesteryl ester levels in liver do not decrease significantly after intravenous administration of YM17E, but do decrease significantly and in a dose-dependent manner after oral administration. YM17E (3, 5, 10 mg/kg, i.v.) significantly inhibits hepatic ACAT activities in a dose-dependent manner. YM17E produces a significant increase in 125I-LDL clearance in atherogenic diet-fed rats after both oral and intravenous administration[1]. YM17E inhibits production of [14C]cholesteryloleate from [14C]oleoyl CoA in a dose-dependent manner in both liver and intestinal microsomes used as enzyme sources[2].
[1]. Uchida T, et al. Relationship between bioavailability and hypocholesterolemic activity of YM17E, an inhibitor of ACAT, in cholesterol-fed rats. Atherosclerosis. 1998 Mar;137(1):97-106. [2]. Kashiwa M, et al. Pharmacological properties of YM17E, an acyl-CoA:cholesterol acyltransferase inhibitor, and diarrheal effect in beagle dogs. Jpn J Pharmacol. 1997 Jan;73(1):41-50.
Animal experiment: | YM17E is administered to rats fed an atherogenic diet at intravenous doses of 0, 3, 5 and 10 mg/kg per day for 5 days or oral doses of 0, 3, 10 and 30 mg/kg per day for 5 days. At 2 h after final administration, all the blood and liver are removed. Serum is obtained from the blood by centrifugation and serum total cholesterol and free cholesterol are measured by an enzymatic method. Serum HDL is prepared by the heparin-Mn method. |
References: [1]. Uchida T, et al. Relationship between bioavailability and hypocholesterolemic activity of YM17E, an inhibitor of ACAT, in cholesterol-fed rats. Atherosclerosis. 1998 Mar;137(1):97-106. | |
| Cas No. | 124900-72-7 | SDF | |
| Canonical SMILES | O=C(NC1=CC=C(N(C)C)C=C1)N(CC2=CC=CC(CN(C3CCCCCC3)C(NC4=CC=C(N(C)C)C=C4)=O)=C2)C5CCCCCC5 | ||
| Formula | C40H56N6O2 | M.Wt | 652.91 |
| Solubility | DMSO : ≥ 125 mg/mL (191.45 mM) | 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 | 1.5316 mL | 7.658 mL | 15.316 mL |
| 5 mM | 306.3 μL | 1.5316 mL | 3.0632 mL |
| 10 mM | 153.2 μL | 765.8 μL | 1.5316 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 19 reference(s) in Google Scholar.)