YM-53601

Name: YM-53601
Brand: MedChemExpress
SKU: HY-100313A
Rating: 5.0 (3 reviews)

Cat. No.: HY-100313A Purity: 99.26%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

YM-53601, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo. YM-53601 inhibits squalene synthase derived from human hepatoma cells with an IC₅₀ of 79 nM. Lipid-lowering agent. YM-53601 is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation.

For research use only. We do not sell to patients.

YM-53601 Chemical Structure

CAS No. : 182959-33-7

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of YM-53601:

YM-53601 free base Get quote

3 Publications Citing Use of MCE YM-53601

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Purity & Documentation
References
Customer Review

Description

YM-53601, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo^[1]. YM-53601 inhibits squalene synthase derived from human hepatoma cells with an IC₅₀ of 79 nM. Lipid-lowering agent^[2]. YM-53601 is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation^[3].

In Vitro

YM-53601 inhibits squalene synthase activities in hepatic microsomes from several species of rat, hamster, guinea-pig, rhesus monkey, and human-derived HepG2 cell with IC₅₀s of 90, 170, 46, 45, and 79 nM, respectively^[1].
YM-53601 inhibits conversion of [3H]farnesyl diphosphate to [³H]squalene by hamster liver squalene synthase with the IC₅₀?of 170 nM^[2].
YM-53601 (1 μM) potentiates the susceptibility of H35 cells to thapsigargin, lonidamine, and doxorubicin. YM-53601 (1 μM) reduces the mitochondrial cholesterol levels in both H35 and HepG2 cells^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[4]

Cell Line:	H35 and HepG2 cells
Concentration:	1 μM
Incubation Time:	24 hours
Result:	Reduced the mitochondrial cholesterol levels in both H35 and HepG2 cells.

In Vivo

YM-53601 suppresses cholesterol biosynthesis in rats (ED₅₀, 32?mg/kg)^[1].
YM-53601 also reduces plasma non-HDL cholesterol levels in hamsters by approximately 70% at an oral dose of 50 mg/kg/day for 5 days^[2].
YM-53601 potentiates Doxorubicin-mediated hepatocellular carcinoma cells (HCC) growth arrest and cell death in vivo^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Sprague-Dawley (SD) rats weighing 150-170 g^[1]
Dosage:	6.25, 12.5, 25 or 50 mg/kg
Administration:	Given a single p.o.
Result:	Inhibited cholesterol biosynthesis from acetate in a dose-dependent manner in rats. The ED₅₀ value for YM-53601 cholesterol biosynthesis inhibition is 32 mg/kg.

Animal Model:	Five- to six-week-old male BALB/c athymic (nu/nu) nude mice^[4]
Dosage:	15 mg/kg
Administration:	2 wk of daily treatment by p.o. gavage
Result:	Significantly decreased the intratumor cholesterol levels.

Molecular Weight

372.86

Formula

C₂₁H₂₂ClFN₂O

CAS No.

182959-33-7

Appearance

Solid

Color

White to light brown

SMILES

F/C(COC1=CC(NC2=C3C=CC=C2)=C3C=C1)=C4CN5CCC/4CC5.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (268.20 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6820 mL	13.4099 mL	26.8197 mL
5 mM	0.5364 mL	2.6820 mL	5.3639 mL
10 mM	0.2682 mL	1.3410 mL	2.6820 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.26%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (252 KB) HNMR (121 KB) RP-HPLC (169 KB) MS (357 KB)

Handling Instructions (2659 KB)

References

[1]. T Ugawa, et al. YM-53601, a novel squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in several animal species. Br J Pharmacol. 2000 Sep;131(1):63-70. [Content Brief]

[2]. Tsukasa Ishihara, et al. Syntheses of 3-ethylidenequinuclidine derivatives as squalene synthase inhibitors. Part 2: enzyme inhibition and effects on plasma lipid levels. Bioorg Med Chem. 2003 Aug 15;11(17):3735-45. [Content Brief]

[3]. Eun-Mee Park, et al. Farnesyl-diphosphate farnesyltransferase 1 regulates hepatitis C virus propagation. FEBS Lett. 2014 May 2;588(9):1813-20. [Content Brief]

[4]. Joan Montero,et al.Mitochondrial cholesterol contributes to chemotherapy resistance in hepatocellular carcinoma. Cancer Res. 2008 Jul 1;68(13):5246-56. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6820 mL	13.4099 mL	26.8197 mL	67.0493 mL
	5 mM	0.5364 mL	2.6820 mL	5.3639 mL	13.4099 mL
	10 mM	0.2682 mL	1.3410 mL	2.6820 mL	6.7049 mL
	15 mM	0.1788 mL	0.8940 mL	1.7880 mL	4.4700 mL
	20 mM	0.1341 mL	0.6705 mL	1.3410 mL	3.3525 mL
	25 mM	0.1073 mL	0.5364 mL	1.0728 mL	2.6820 mL
	30 mM	0.0894 mL	0.4470 mL	0.8940 mL	2.2350 mL
	40 mM	0.0670 mL	0.3352 mL	0.6705 mL	1.6762 mL
	50 mM	0.0536 mL	0.2682 mL	0.5364 mL	1.3410 mL
	60 mM	0.0447 mL	0.2235 mL	0.4470 mL	1.1175 mL
	80 mM	0.0335 mL	0.1676 mL	0.3352 mL	0.8381 mL
	100 mM	0.0268 mL	0.1341 mL	0.2682 mL	0.6705 mL

YM-53601 Related Classifications

Metabolic Disease Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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YM-53601

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Other Forms of YM-53601:

YM-53601 Related Antibodies

3 Publications Citing Use of MCE YM-53601

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•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

YM-53601 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

YM-53601 Related Classifications

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