K-134

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C22H29N3O4
Molecular Weight	399.4834
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O[C@@H]1CCCC[C@H]1N(C2CC2)C(=O)NCCCOC3=CC4=C(NC(=O)C=C4)C=C3

InChI

InChIKey=ULGNGSQNNMKROG-WOJBJXKFSA-N

InChI=1S/C22H29N3O4/c26-20-5-2-1-4-19(20)25(16-7-8-16)22(28)23-12-3-13-29-17-9-10-18-15(14-17)6-11-21(27)24-18/h6,9-11,14,16,19-20,26H,1-5,7-8,12-13H2,(H,23,28)(H,24,27)/t19-,20-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C22H29N3O4
Molecular Weight	399.4834
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/mesh/67116725 | https://www.ncbi.nlm.nih.gov/pubmed/10644042 | https://www.ncbi.nlm.nih.gov/pubmed/22119244

K-134, a 2(1H)-quinolinone derivative, is a phosphodiesterase 3 inhibitor. It has both anti-thrombotic and anti-hyperplastic activities. It was evaluated in a phase II trial in patients with peripheral artery disease and claudication.

Originator

Approval Year

PubMed

Title	Date	PubMed
2(1H)-quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activities.	1998 Jun 16	9873372
Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phosphodiesterase isozyme activity.	2000 Feb 15	10644042
Investigation of binding proteins for anti-platelet agent K-134 by Drug-Western method.	2007 Feb 23	17207464
Effects of cilostazol and k-134 on reconstructive surgery using prosthetic grafts in the abdominal aorta of beagle dogs.	2008	18558424
K-134, a phosphodiesterase 3 inhibitor, prevents brain damage by inhibiting thrombus formation in a rat cerebral infarction model.	2012	23110051
A phase II dose-ranging study of the phosphodiesterase inhibitor K-134 in patients with peripheral artery disease and claudication.	2012 Feb	22119244

Patents

Sample Use Guides

In Vitro Use Guide

K-134 (OPC-33509) inhibited recombinant PDE3A (IC50 = 0.10 uM) and PDE3B (IC50 = 0.28 uM).

Substance Class	Chemical Created by `admin` on `Fri Dec 15 15:55:13 GMT 2023` Edited by `admin` on `Fri Dec 15 15:55:13 GMT 2023`
Record UNII	J9J6NK6W4U
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

K-134

Common Name

English

OPC-33509

Code

English

UREA, N-CYCLOPROPYL-N'-(3-((1,2-DIHYDRO-2-OXO-6-QUINOLINYL)OXY)PROPYL)-N-((1R,2R)-2-HYDROXYCYCLOHEXYL)-

Systematic Name

English

Code System Code Type Description

DRUG BANK

DB12685