SB273005

Alias: SB-273005; SB 273005; SB273005
Cat No.:V1600 Purity: ≥98%
SB273005 (SB 273005; SB-273005) is a novel and potent integrin inhibitor with potential usefulness in bone resorption, osteoporosis and arthritis.
SB273005 Chemical Structure CAS No.: 205678-31-5
Product category: Integrin
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
Other Sizes
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

SB273005 (SB 273005; SB-273005) is a novel and potent integrin inhibitor with potential usefulness in bone resorption, osteoporosis and arthritis. It inhibits integrin αvβ3 receptor and αvβ5 receptor with Ki values of 1.2 nM and 0.3 nM, respectively. 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.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: In vitro, SB273005 inhibits human osteoclast-mediated bone resorption with IC50 of 11 nM. In blood containing MDA-MB-231 cells, a combination of SB273005 and lamifiban inhibits tumor cell adhesion to vascular extracellular matrix (ECM).


Kinase Assay: 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.

ln Vivo
In rat models of bone resorption and osteoporosis, SB273005 (30 mg/kg, p.o.) inhibits the parathyroid hormone-stimulated calcemic response, and inhibits bone loss. In rat with adjuvant-induced arthritis, SB273005 (60 mg/kg, p.o.) significantly reduces the symptoms of adjuvant-induced arthritis. SB273005 (1000 mg/kg/day, p.o.) causes acute, transient necrosis of vascular smooth muscle cell (VSMC) in aorta and renal arteries of mice. In pregnant mice, SB273005 reverses the reduction of Th1 cell-produced IL-2 levels and the increase of Th2 cell-derived IL-10 levels.
Animal Protocol
Dissolved in 1% methylcellulose; 30 mg/kg; i.p. injection
Thyroidectomized parathyroidectomized (TPTx) rat model of bone resorption, and ovariectomized (Ovx) rat model of osteoporosis
References
J Med Chem.2000 Jan 13;43(1):22-6;Arthritis Rheum.2001 Jan;44(1):128-37.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H24F3N3O4
Molecular Weight
451.44
CAS #
205678-31-5
Related CAS #
205678-31-5
SMILES
FC(C([H])([H])N1C([C@]([H])(C([H])([H])C(=O)O[H])C([H])([H])C2C([H])=C([H])C(=C([H])C=2C1([H])[H])OC([H])([H])C([H])([H])C1C([H])=C([H])C([H])=C(N([H])C([H])([H])[H])N=1)=O)(F)F
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
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
Synonyms
SB-273005; SB 273005; SB273005
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 90 mg/mL (199.4 mM)
Water:<1 mg/mL
Ethanol:16 mg/mL (35.4 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2151 mL 11.0757 mL 22.1513 mL
5 mM 0.4430 mL 2.2151 mL 4.4303 mL
10 mM 0.2215 mL 1.1076 mL 2.2151 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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