[CAS NO. 189060-13-7] Lapaquistatacetate

Name: Lapaquistatacetate
Brand: Arctom Scientific
SKU: HY-16274

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PRODUCTS SPECIFICATIONS [189060-13-7]

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Catalog

HY-16274

Brand

MCE

CAS

189060-13-7

DESCRIPTION [189060-13-7]

Overview

MDL	-
Molecular Weight	645.14
Molecular Formula	C33H41ClN2O9
SMILES	O=C(O)CC1CCN(C(C[C@@H]2C(N(CC(C)(C)COC(C)=O)C3=CC=C(Cl)C=C3[C@@H](C4=CC=CC(OC)=C4OC)O2)=O)=O)CC1

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

Summary

Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor, blocking the conversion of farnesyl diphosphate (FPP) to squalene in the cholesterol biosynthesis pathway ^[1] . Lapaquistat acetate is effective at lowering low-density lipoprotein cholesterol , but it might cause liver damage. Lapaquistat acetate is used for hypercholesterolemia and mevalonate kinase deficiency (MKD) research ^[2] .

IC50 & Target

Squalene synthase ^[1]

In Vivo

Lapaquistat acetate (diet supplemented; 100 or 200 mg/kg; 32 weeks) decreases plasma cholesterol and triglyceride levels. It delays progression of coronary atherosclerosis and changes coronary atheromatous plaques from unstable, macrophage/lipid accumulation-rich, lesions to stable fibromuscular lesions in vivo ^[3] .

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

Animal Model:	Male WHHLMI rabbits, aged 2 months ^[3]
Dosage:	100 or 200 mg/kg
Administration:	Diet supplemented; 100 or 200 mg/kg; 32 weeks
Result:	Increased collagen concentration and transformed coronary plaques into fibromuscular plaques. Suppressed the expression of MMP-1 and PAI-1 in the plaque and increased peripheral coenzyme Q10 levels.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00868127	Takeda	Hypercholesterolemia	December 2005	Phase 3
NCT00268697	Takeda	Hypercholesterolemia	October 2005	Phase 3
NCT00286481	Takeda	Hypercholesterolemia	March 2006	Phase 3
NCT00532311	Takeda	Hypercholesterolemia	July 2007	Phase 3
NCT00143663	Takeda	Dyslipidemia	September 2005	Phase 3
NCT00864643	Takeda	Hypercholesterolemia	September 2004	Phase 2
NCT00813527	Takeda	Hyperlipidemias	February 2006	Phase 2
NCT00249912	Takeda	Hypercholesterolemia	October 2005	Phase 3
NCT00865228	Takeda	Hypercholesterolemia	July 2007	Phase 2
NCT00251680	Takeda	Type 2 Diabetes	October 2005	Phase 3
NCT00532558	Takeda	Hypercholesterolemia	October 2007	Phase 3
NCT00263081	Takeda	Hypercholesterolemia	November 2005	Phase 3
NCT00256178	Takeda	Hypercholesterolemia	October 2005	Phase 3
NCT00487994	Takeda	Dyslipidemia	November 2004	Phase 3
NCT00143676	Takeda	Hypercholesterolemia	August 2005	Phase 3
NCT00249899	Takeda	Hypercholesterolemia	November 2005	Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 77.50 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5501 mL	7.7503 mL	15.5005 mL
5 mM	0.3100 mL	1.5501 mL	3.1001 mL
10 mM	0.1550 mL	0.7750 mL	1.5501 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (3.88 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

4-Piperidineacetic acid, 1-[2-[(3R,5S)-1-[3-(acetyloxy)-2,2-dimethylpropyl]-7-chloro-5-(2,3-dimethoxyphenyl)-1,2,3,5-tetrahydro-2-oxo-4,1-benzoxazepin-3-yl]acetyl]-

4-Piperidineacetic acid, 1-[[1-[3-(acetyloxy)-2,2-dimethylpropyl]-7-chloro-5-(2,3-dimethoxyphenyl)-1,2,3,5-tetrahydro-2-oxo-4,1-benzoxazepin-3-yl]acetyl]-, (3R-trans)-

4-Piperidineacetic acid, 1-[[(3R,5S)-1-[3-(acetyloxy)-2,2-dimethylpropyl]-7-chloro-5-(2,3-dimethoxyphenyl)-1,2,3,5-tetrahydro-2-oxo-4,1-benzoxazepin-3-yl]acetyl]-

1-[2-[(3R,5S)-1-[3-(Acetyloxy)-2,2-dimethylpropyl]-7-chloro-5-(2,3-dimethoxyphenyl)-1,2,3,5-tetrahydro-2-oxo-4,1-benzoxazepin-3-yl]acetyl]-4-piperidineacetic acid

TAK 475

Lapaquistat acetate