SB-273005

SB-273005 is an orally active non-peptide αvβ3 integrin antagonist with Ki values of 1.2 nM and 0.3 nM for αvβ3 and αvβ5, respectively. SB-273005 blocks the binding of integrins to the RGD sequence in the extracellular matrix. SB-273005 inhibits Rictor phosphorylation and reduces IL-10 secretion. SB-273005 inhibits inflammation, prevents bone loss, regulates vascular smooth muscle function, and reverses pregnancy-induced immune deviation. SB-273005 can be used in the study of rheumatoid arthritis, osteoporosis, and aneurysms. [1][2][3][4][5].

Product Specifications

CAS Number

[205678-31-5]

UNSPSC

12352005

Target

Integrin; Interleukin Related

Type

Reference compound

Related Pathways

Cytoskeleton; Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Endocrinology; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/sb-273005.html

Concentration

10mM

Purity

99.94

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(O)C[C@H]1C(N(CC(F)(F)F)CC2=CC(OCCC3=NC(NC)=CC=C3)=CC=C2C1)=O

Molecular Formula

C22H24F3N3O4

Molecular Weight

451.44

References & Citations

[1]Badger AM, et al. Disease-modifying activity of SB 273005, an orally active, nonpeptide alphavbeta3 (vitronectin receptor) antagonist, in rat adjuvant-induced arthritis. Arthritis Rheum. 2001 Jan;44 (1) :128-37. |[2]Rehm S, et al. Novel vascular lesions in mice given a non-peptide vitronectin receptor antagonist. Toxicol Pathol. 2007 Dec;35 (7) :958-71. |[3]Parker SJ, et al. Proteomics reveals Rictor as a noncanonical TGF-β signaling target during aneurysm progression in Marfan mice. Am J Physiol Heart Circ Physiol. 2018 Nov 1;315 (5) :H1112-H1126.|[4]Wang S, et al. SB-273005, an antagonist of αvβ3 integrin, reduces the production of Th2 cells and cytokine IL-10 in pregnant mice. Exp Ther Med. 2014 Jun;7 (6) :1677-1682. |[5]Hoffman SJ, et al. Rapid inhibition of thyroxine-induced bone resorption in the rat by an orally active vitronectin receptor antagonist. J Pharmacol Exp Ther. 2002 Jul;302 (1) :205-11.