Lapaquistat , CAS No.189059-71-0

Item Number
L648651
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L648651-1mg
1mg
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$280.90
L648651-5mg
5mg
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L648651-10mg
10mg
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L648651-25mg
25mg
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Basic Description

SynonymsLapaquistat | 189059-71-0 | Lapaquistat [INN] | PEZ79BV72X | CHEMBL341976 | 2-(1-(2-((3R,5S)-1-(3-hydroxy-2,2-dimethylpropyl)-7-chloro-5-(2,3- dimethoxyphenyl)-2-oxo-1,2,3,5-tetrahydrobenzo(E)(1,4)oxazepin-3-yl)acetyl)piperidin-4-yl)acetic acid | 4-Piperidineacetic a
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Product Description

Lapaquistat (T-91485), a cholesterol biosynthesis inhibitor, is the active metabolite of Lapaquistat acetate ( HY-16274 ). Lapaquistat can decrease statin-induced myotoxicity in lipid-lowering therapy

In Vitro

Lapaquistat inhibits cholesterol biosynthesis in differentiated RD (rhabdomyosarcoma) cells, with an IC 50 of 36 nM. Lapaquistat potently inhibits cholesterol synthesis in RD cells, with an IC 25 exceeded 100 μM. Lapaquistat concentration-dependently inhibits cholesterol biosynthesis in human skeletal myocytes, with an IC 50 of 45 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

After oral administration to rats, Lapaquistat acetate (HY-16274) is absorbed and rapidly hydrolyzed into a pharmacological active metabolite, Lapaquistat . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:Cholesterol biosynthesis

Associated Targets(Human)

FDFT1 Tchem Squalene synthase (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
Liver microsomes (16955 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Fdft1 Squalene synthetase (34 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Names and Identifiers

IUPAC Name 2-[1-[2-[(3R,5S)-7-chloro-5-(2,3-dimethoxyphenyl)-1-(3-hydroxy-2,2-dimethylpropyl)-2-oxo-5H-4,1-benzoxazepin-3-yl]acetyl]piperidin-4-yl]acetic acid
INCHI InChI=1S/C31H39ClN2O8/c1-31(2,18-35)17-34-23-9-8-20(32)15-22(23)28(21-6-5-7-24(40-3)29(21)41-4)42-25(30(34)39)16-26(36)33-12-10-19(11-13-33)14-27(37)38/h5-9,15,19,25,28,35H,10-14,16-18H2,1-4H3,(H,37,38)/t25-,28-/m1/s1
InChi Key HDGUKVZPMPJBFK-LEAFIULHSA-N
Canonical SMILES CC(C)(CN1C2=C(C=C(C=C2)Cl)C(OC(C1=O)CC(=O)N3CCC(CC3)CC(=O)O)C4=C(C(=CC=C4)OC)OC)CO
Isomeric SMILES CC(C)(CN1C2=C(C=C(C=C2)Cl)[C@H](O[C@@H](C1=O)CC(=O)N3CCC(CC3)CC(=O)O)C4=C(C(=CC=C4)OC)OC)CO
Alternate CAS 189059-71-0
PubChem CID 9960389
MeSH Entry Terms (1-(2-(1-(2-carboxyoxy-1,1-dimethylethyl)-7-chloro-5-(2,3-dimethoxyphenyl)-2-oxo-1,2,3,5-tetrahydrobenzo(e)(1,4)oxazepin-3-yl)acetyl)piperidin-4-yl)acetic acid;1-((1-(3-acetoxy-2,2-dimethylpropyl)-7-chloro-5-(2,3-dimethoxyphenyl)-2-oxo-1,2,3,5-tetrahydro-
Molecular Weight 603.10

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilityDMSO : 25 mg/mL (41.45 mM; Need ultrasonic)

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Solution Calculators