205678-31-5
Chemical Structure
SB-273005
- CAS. Nr.: 205678-31-5
- Formula:C22H24F3N3O4
- Molecular Weight:451.44
IUPAC Name: (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
InChIKey: KSSPHFGIOASRDE-HNNXBMFYSA-N
SMILES: O=C(O)C[C@H]1C(N(CC(F)(F)F)CC2=CC(OCCC3=NC(NC)=CC=C3)=CC=C2C1)=O
Biological Activity: 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].
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SB-273005 | 99.94% | 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. . | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
