SB-273005
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MedKoo CAT#: 562036

CAS#: 205678-31-5

Description: SB-273005 is an inhibitor of integrin αvβ3. SB-273005 reduces the production of Th2 cells and cytokine IL-10 in pregnant mice. SB-273005 causes direct chemical vascular toxicity in murine VSMC which involves apoptosis mediated through the intrinsic (mitochondrial) apoptotic pathway. SB-273005 may be useful for the treatment of metabolic bone diseases, including those resulting from hyperthyroidism.

Chemical Structure

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SB-273005
CAS# 205678-31-5
Instruction

Theoretical Analysis

MedKoo Cat#: 562036
Name: SB-273005
CAS#: 205678-31-5
Chemical Formula: C22H24F3N3O4
Exact Mass: 451.17
Molecular Weight: 451.440
Elemental Analysis: C, 58.53; H, 5.36; F, 12.63; N, 9.31; O, 14.18

Price and Availability

Size Price Availability Quantity
25mg USD 450 2 Weeks
50mg USD 750 2 Weeks
100mg USD 1350 2 Weeks
200mg USD 2050 2 Weeks
500mg USD 3650 2 Weeks
1g USD 4650 2 Weeks
2g USD 6950 2 Weeks
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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

Appearance: Solid powder

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

More Info:

Biological target:
In vitro activity:
In vivo activity:

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.

Recalculate based on batch purity %
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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.