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Merck
CN

SML3926

YM-53601 hydrochloride

≥98% (HPLC)

Synonym(s):

(E)-2-[2-fluoro-2-(quinuclidin-3-ylidene) ethxy]-9H-carbazole monohydrochloride, 2-[(2E)-2-(1-Azabicyclo[2.2.2]oct-3-ylidene)-2-fluoroethoxy]-9H-carbazole hydrochloride, YM 53601

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About This Item

Empirical Formula (Hill Notation):
C21H21FN2O·HCl
CAS Number:
Molecular Weight:
372.86
MDL number:
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Quality Level

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Biochem/physiol Actions

Squalene synthase inhibitor.


YM-53601 is a cell penetrant and potent squalene synthase inhibitor inhibits cholesterol biosynthesis in rodents. YM-53601 lowers cholesterol levels and triglyceride levels better than HMG-CoA reductase inhibitor (prevastatin) and fibrate (fenofibrate.).

Disclaimer

Hygroscopic

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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T Ugawa et al.
British journal of pharmacology, 131(1), 63-70 (2000-08-26)
The aim of this study was to evaluate the potency of YM-53601 ((E)-2-[2-fluoro-2-(quinuclidin-3-ylidene) ethoxy]-9H-carbazole monohydrochloride), a new inhibitor of squalene synthase, in reducing both plasma cholesterol and triglyceride levels, compared with 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor and fibrates, respectively.
Kyoko Saito et al.
Journal of virology, 89(4), 2220-2232 (2014-12-05)
Hepatitis C virus (HCV) exploits host membrane cholesterol and its metabolism for progeny virus production. Here, we examined the impact of targeting cellular squalene synthase (SQS), the first committed enzyme for cholesterol biosynthesis, on HCV production. By using the HCV
Yasushi Takemoto et al.
Journal of the American Chemical Society, 142(3), 1142-1146 (2020-01-04)
We accidentally found that YM-53601, a known small-molecule inhibitor of squalene synthase (SQS), selectively depletes SQS from mammalian cells upon UV irradiation. Further analyses indicated that the photodepletion of SQS requires its short peptide segment located at the COOH terminus.

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