(S)-2-(8-(2-(6-(methylamino)pyridin-2-yl)ethoxy)-3-oxo-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl)acetic acid

Biological Activity

sb 273005 is a potent nonpeptide antagonist of αvβ3 (vitronectin receptor), with ki values of 1.2 nm and 0.3 nm to two closely related integrins, αvβ3 and αvβ5, respectively [1].αvβ3 belongs to the integrin family of adhesion molecules. it is a heterodimer. it mediates cell adhesion to serum proteins and extracellular matrix via the recognition of the arg-gly-asp (rgd) sequence [1].sb 273005 binds αvβ3 and αvβ5 with low nm affinity, but binds weakly to integrins αiibβ3 and α5β1. sb 273005 inhibits αvβ3-mediated cell adhesion with an ic50 value of 3 nm, endothelial cell migration with an ic50 of 1.8 nm, and osteoclast-mediated bone resorption with an ic50 of 11 nm in vitro [1].the αvβ3 integrin is pivotal in bone resorption [2]. in the chronic ovx and thyroparathyroidectomized bone resorption rat models, sb 273005 as well as other similar vitronectin receptor antagonists, inhibit bone loss. in aia rats, prophylactical treatment with sb 273005 at doses of 60, 30, and 10 mg/kg twice daily significantly normalized bone mineral density (bmd). normalization values of bmd were 69%, 42%, and 44% for doses of 60, 30, and 10 mg/kg twice daily, respectively. a single daily dose of sb 273005 significantly improved bmd (24% normalization) only when sb 273005 was prophylactically administered at 60 mg/kg [1].

in vitro

SB273005 inhibits human osteoclast-mediated bone resorption in vitro with IC50 of 11 nM. In blood containing MDA-MB-231 cells, binding of SB273005 to lamifiban inhibited tumor cell adhesion to the vascular extracellular matrix (ECM).

in vitro

In rat models of bone resorption and osteoporosis, SB273005 (30 mg/kg, po) inhibits parathyroid hormone-stimulated calcium responses and inhibits bone loss. In adjuvant arthritis rats, it significantly reduced adjuvant-induced arthritis symptoms.

target

< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> 0.3 nM

Target	Value
αvβ5 receptor (Cell-free assay)
αvβ3 receptor (Cell-free assay)	1.2 nM

Supplier	Tel	Email	Country	ProdList	Advantage
Hubei Jusheng Technology Co.,Ltd.	18871490254	linda@hubeijusheng.com	CHINA	28172	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	32161	58
Dideu Industries Group Limited	+86-29-89586680 +86-15129568250	1026@dideu.com	China	22784	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6391	58
TargetMol Chemicals Inc.		support@targetmol.com	United States	38631	58
Wuhan Topule Biopharmaceutical Co., Ltd	+8618327326525	masar@topule.com	China	8467	58
Amadis Chemical Company Limited	571-89925085	sales@amadischem.com	China	131957	58
Suzhou Flokoo Pharmaceutical Co., Ltd.	0512-62706796	market@flokoo.com	China	112	55
ShangHai Angti Biotechnology Co., Ltd.	13764913901	info@angtibio.com	China	5003	55
Target molecule Corp.	857-239-0968	service1@targetmol.com	United States	2559	60