K-134

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 528817

CAS#: 189362-06-9

Description: K-134 is a PDE3 inhibitor potentially for the treatment of anti-thrombotic and anti-hyperplastic activities.


Price and Availability

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K-134 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 528817
Name: K-134
CAS#: 189362-06-9
Chemical Formula: C22H29N3O4
Exact Mass:
Molecular Weight: 399.491
Elemental Analysis: C, 66.14; H, 7.32; N, 10.52; O, 16.02


Synonym: K-134; OPC-33509; K134; OPC33509; K 134; OPC 33509

IUPAC/Chemical Name: 1-cyclopropyl-1-((1R,2R)-2-hydroxycyclohexyl)-3-(3-((2-oxo-1,2-dihydroquinolin-6-yl)oxy)propyl)urea

InChi Key: ULGNGSQNNMKROG-WOJBJXKFSA-N

InChi Code: 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

SMILES Code: O=C(NCCCOC1=CC2=C(NC(C=C2)=O)C=C1)N(C3CC3)[C@H]4[C@H](O)CCCC4


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Sasaki Y, Suzuki H, Itoh S, Yoshida H, Kondo S, Inoue K, Tanabe S. K-134, a phosphodiesterase 3 inhibitor, improves gait disturbance and hindlimb blood flow impairment in rat peripheral artery disease models. Eur J Pharmacol. 2012 Aug 15;689(1-3):132-8. doi: 10.1016/j.ejphar.2012.05.014. Epub 2012 May 31. PubMed PMID: 22659587.

2: Yoshida H, Ashikawa Y, Itoh S, Nakagawa T, Asanuma A, Tanabe S, Inoue Y, Hidaka H. K-134, a phosphodiesterase 3 inhibitor, prevents brain damage by inhibiting thrombus formation in a rat cerebral infarction model. PLoS One. 2012;7(10):e46432. doi: 10.1371/journal.pone.0046432. Epub 2012 Oct 23. PubMed PMID: 23110051; PubMed Central PMCID: PMC3479105.

3: Yoshida H, Itoh S, Hara T, Sasaki Y, Kondo S, Nakagawa T, Asanuma A, Tanabe S. A phosphodiesterase 3 inhibitor, K-134, improves hindlimb skeletal muscle circulation in rat models of peripheral arterial disease. Atherosclerosis. 2012 Mar;221(1):84-90. doi: 10.1016/j.atherosclerosis.2011.12.044. Epub 2012 Jan 5. PubMed PMID: 22269153.

4: Brass EP, Cooper LT, Morgan RE, Hiatt WR. A phase II dose-ranging study of the phosphodiesterase inhibitor K-134 in patients with peripheral artery disease and claudication. J Vasc Surg. 2012 Feb;55(2):381-389.e1. doi: 10.1016/j.jvs.2011.09.004. Epub 2011 Nov 25. PubMed PMID: 22119244.

5: Inoue Y, Sugano N, Jibiki M, Kudo T, Iwai T. Effects of cilostazol and k-134 on reconstructive surgery using prosthetic grafts in the abdominal aorta of beagle dogs. Thromb Res. 2008;123(1):122-9. doi: 10.1016/j.thromres.2008.04.018. Epub 2008 Jun 16. PubMed PMID: 18558424.

6: Ikenoya M, Doi T, Miura T, Sawanobori K, Nishio M, Hidaka H. Investigation of binding proteins for anti-platelet agent K-134 by Drug-Western method. Biochem Biophys Res Commun. 2007 Feb 23;353(4):1111-4. Epub 2006 Dec 29. PubMed PMID: 17207464.

7: Kajimoto T, Endo S, Tanaka K, Okashiro Y, Kai H, Fujii S, Mishima A, Matsubara T, Yoshida S. Apparatus development for measurement of (134)Cs and (137)Cs radioactivity of soil contaminated by the Fukushima Daiichi Nuclear Power Plant accident. Appl Radiat Isot. 2016 Sep;115:4-7. doi: 10.1016/j.apradiso.2016.06.003. Epub 2016 Jun 4. PubMed PMID: 27289189.

8: Kuzubova EA, Bugaeva LI, Sergeeva SA, Petrov VI, Kataev VA, Kharlamov IV, Mal'tsev MV. Effects of a New Benzimidazole Derivative on Generative Function of Female Rats. Bull Exp Biol Med. 2015 Sep;159(5):635-7. doi: 10.1007/s10517-015-3034-2. Epub 2015 Oct 15. PubMed PMID: 26468030.

9: Lewis RJ, Connor JT, Teerlink JR, Murphy JR, Cooper LT, Hiatt WR, Brass EP. Application of adaptive design and decision making to a phase II trial of a phosphodiesterase inhibitor for the treatment of intermittent claudication. Trials. 2011 May 25;12:134. doi: 10.1186/1745-6215-12-134. PubMed PMID: 21612611; PubMed Central PMCID: PMC3126735.

10: Yoshida H, Okamura Y, Watanabe N, Ikeda Y, Handa M. Shear-dependent suppression of platelet thrombus formation by phosphodiesterase 3 inhibition requires low levels of concomitant Gs-coupled receptor stimulation. Thromb Haemost. 2011 Mar;105(3):487-95. doi: 10.1160/TH10-07-0439. Epub 2010 Dec 6. PubMed PMID: 21136009.

11: Altzitzoglou T, Bohnstedt A. Characterisation of the IAEA-375 Soil Reference Material for radioactivity. Appl Radiat Isot. 2016 Mar;109:118-21. doi: 10.1016/j.apradiso.2015.11.053. Epub 2015 Nov 22. PubMed PMID: 26651166.

12: Litchfield WR, Coolidge C, Silva P, Lifton RP, Fallo F, Williams GH, Dluhy RG. Impaired potassium-stimulated aldosterone production: a possible explanation for normokalemic glucocorticoid-remediable aldosteronism. J Clin Endocrinol Metab. 1997 May;82(5):1507-10. PubMed PMID: 9141541.

13: Firth SM, Clemmons DR, Baxter RC. Mutagenesis of basic amino acids in the carboxyl-terminal region of insulin-like growth factor binding protein-5 affects acid-labile subunit binding. Endocrinology. 2001 May;142(5):2147. PubMed PMID: 11316783.

14: Ateba JF, Ateba PO, Ben-Bolie GH, Abiama PE, Abega CR, Mvondo S. Natural background dose measurements in south Cameroon. Radiat Prot Dosimetry. 2010 Jun;140(1):81-8. doi: 10.1093/rpd/ncq035. Epub 2010 Feb 16. PubMed PMID: 20159924.

15: Girisha ST, Raju NS. Effect of sewage water on seed germination and vigour index of different varieties of groundnut (Arachis hypogaea L.). J Environ Biol. 2008 Nov;29(6):937-9. PubMed PMID: 19297996.

16: Farver O, Skov LK, van de Kamp M, Canters GW, Pecht I. The effect of driving force on intramolecular electron transfer in proteins. Studies on single-site mutated azurins. Eur J Biochem. 1992 Dec 1;210(2):399-403. PubMed PMID: 1459124.

17: Al Hamarneh I, Wreikat A, Toukan K. Radioactivity concentrations of 40K, 134Cs, 137Cs, 90Sr, 241Am, 238Pu and 239+240Pu radionuclides in Jordanian soil samples. J Environ Radioact. 2003;67(1):53-67. PubMed PMID: 12634001.

18: Dragović S, Onjia A. Classification of soil samples according to their geographic origin using gamma-ray spectrometry and principal component analysis. J Environ Radioact. 2006;89(2):150-8. Epub 2006 Jun 21. PubMed PMID: 16793182.