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Umirolimus

Names

[ CAS No. ]:
851536-75-9

[ Name ]:
Umirolimus

[Synonym ]:
Umirolimus
Biolimus A9
23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone, 3-[(1R)-2-[(1S,3R,4R)-4-(2-ethoxyethoxy)-3-methoxycyclohexyl]-1-methylethyl]-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-hexadecahydro-9,27-dihydroxy-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-, (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,26R,27R,34aS)-
(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,35R)-12-{(2R)-1-[(1S,3R,4R)-4-(2-Ethoxyethoxy)-3-methoxycyclohexyl]-2-propanyl}-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dio ;xa-4-azatricyclo[30.3.1.0]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone
Biolimus
MFCD22124433

Biological Activity

[Description]:

Umirolimus, a macrocyclic triene lactone Rapamycin derivative, is powerful immunosuppressant and anti-inflammatory agent. Umirolimus has highly lipophilicity and can be used drug-eluting stent (DES) applications[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Inflammation/Immunology

[In Vitro]

Umirolimus is a macrocyclic triene lactone, developed with pharmacological properties specifically tailored for localized drug delivery. Umirolimus can be used drug-eluting stent (DES) applications. Owing to its enhanced lipophilicity,it is strongly attracted to binding sites within the vessel wall and small, tortuous vessels, and contributing to cellular absorption and sustained distribution in the vessel wall surrounding the stent[1]. Umirolimus prevents progression of the cell cycle in G1 phase by inhibiting IL-2/mTOR-mediated P70-KD S6 protein kinase activation. Umirolimus inhibits T-cell growth, as well as smooth muscle cell growth[1].

[In Vivo]

The elimination half-life of Umirolimus is approximately 25 h in whole blood[1].

[References]

[1]. Eberhard Grube, et al. BioMatrix Biolimus A9-eluting coronary stent: a next-generation drug-eluting stent for coronary artery disease. Expert Rev Med Devices. 2006 Nov;3(6):731-41.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
991.0±75.0 °C at 760 mmHg

[ Molecular Formula ]:
C55H87NO14

[ Molecular Weight ]:
986.278

[ Flash Point ]:
553.1±37.1 °C

[ Exact Mass ]:
985.612671

[ PSA ]:
193.66000

[ LogP ]:
4.24

[ Vapour Pressure ]:
0.0±0.6 mmHg at 25°C

[ Index of Refraction ]:
1.540

Related Compounds