Synonym
SB-273005; SB 273005; SB273005;
IUPAC/Chemical Name
2-[(4S)-8-[2-[6-(Methylamino)pyridin-2-yl]ethoxy]-3-oxo-2-(2,2,2-trifluoroethyl)-4,5-dihydro-1H-2-benzazepin-4-yl]acetic acid
InChi Key
KSSPHFGIOASRDE-HNNXBMFYSA-N
InChi Code
InChI=1S/C22H24F3N3O4/c1-26-19-4-2-3-17(27-19)7-8-32-18-6-5-14-9-15(11-20(29)30)21(31)28(12-16(14)10-18)13-22(23,24)25/h2-6,10,15H,7-9,11-13H2,1H3,(H,26,27)(H,29,30)/t15-/m0/s1
SMILES Code
O=C(O)C[C@H]1C(N(CC(F)(F)F)CC2=CC(OCCC3=NC(NC)=CC=C3)=CC=C2C1)=O
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).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
451.44
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Wang S, Zhou X, Yang J. Integrin αvβ3 Is Essential for Maintenance of Decidua Tissue Homeostasis and of Natural Killer Cell Immune Tolerance During Pregnancy. Reprod Sci. 2018 Jan 1:1933719117746766. doi: 10.1177/1933719117746766. [Epub ahead of print] PubMed PMID: 29303057.
2: Wang S, Yang J, Wang C, Yang Q, Zhou X. 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. Epub 2014 Apr 7. PubMed PMID: 24926365; PubMed Central PMCID: PMC4043605.
3: Dalmas Wilk DA, Scicchitano MS, Morel D. In vitro investigation of integrin-receptor antagonist-induced vascular toxicity in the mouse. Toxicol In Vitro. 2013 Feb;27(1):272-81. doi: 10.1016/j.tiv.2012.08.028. Epub 2012 Sep 1. PubMed PMID: 22964516.
4: Rehm S, Thomas RA, Smith KS, Mirabile RC, Gales TL, Eustis SL, Boyce RW. Novel vascular lesions in mice given a non-peptide vitronectin receptor antagonist. Toxicol Pathol. 2007 Dec;35(7):958-71. PubMed PMID: 18098042.
5: Gomes N, Vassy J, Lebos C, Arbeille B, Legrand C, Fauvel-Lafeve F. Breast adenocarcinoma cell adhesion to the vascular subendothelium in whole blood and under flow conditions: effects of alphavbeta3 and alphaIIbbeta3 antagonists. Clin Exp Metastasis. 2004;21(6):553-61. PubMed PMID: 15679053.
6: Hoffman SJ, Vasko-Moser J, Miller WH, Lark MW, Gowen M, Stroup G. 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. PubMed PMID: 12065718.
7: Badger AM, Blake S, Kapadia R, Sarkar S, Levin J, Swift BA, Hoffman SJ, Stroup GB, Miller WH, Gowen M, Lark MW. 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. PubMed PMID: 11212150.
