Home Cytoskeletal Signaling Integrin inhibitor SB273005 For research use only.

SB273005

SB273005 is a potent integrin inhibitor with Ki of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.

SB273005 Chemical Structure

SB273005 Chemical Structure

CAS No. 205678-31-5

Purity & Quality Control

SB273005 Related Products

Signaling Pathway

Integrin Signaling Pathways

Integrin Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK 293 cells Function assay Inhibition of Vitronectin receptor, integrin alphaV-beta3 expressed in HEK 293 cells, IC50=0.00015 μM 12477347
HEK Function assay HEK cell adhesion mediated by alpha v beta 3 integrin, IC50 = 0.003 μM. 10633035
Click to View More Cell Line Experimental Data

Biological Activity

Description SB273005 is a potent integrin inhibitor with Ki of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.
Targets
αvβ5 receptor [1]
(Cell-free assay)		 αvβ3 receptor [1]
(Cell-free assay)
0.3 nM 1.2 nM
In vitro
In vitro

In vitro, SB273005 inhibits human osteoclast-mediated bone resorption with IC50 of 11 nM. [1]

In blood containing MDA-MB-231 cells, a combination of SB273005 and lamifiban inhibits tumor cell adhesion to vascular extracellular matrix (ECM). [3]
Kinase Assay Binding assay
Binding affinity for human αvβ3 and αvβ5 is determined in a competitive binding assay employing 3H-SK&F 107260 as the displaced ligand. The Ki values represent the means of values determined in two to three separate experiments.
In Vivo
In 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. [1]

In rat with adjuvant-induced arthritis, SB273005 (60 mg/kg, p.o.) significantly reduces the symptoms of adjuvant-induced arthritis. [2]

SB273005 (1000 mg/kg/day, p.o.) causes acute, transient necrosis of vascular smooth muscle cell (VSMC) in aorta and renal arteries of mice. [4]

In pregnant mice, SB273005 reverses the reduction of Th1 cell-produced IL-2 levels and the increase of Th2 cell-derived IL-10 levels. [5]
Animal Research Animal Models Thyroidectomized−parathyroidectomized (TPTx) rat model of bone resorption, and ovariectomized (Ovx) rat model of osteoporosis
Dosages 30 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 451.44 Formula

C22H24F3N3O4
CAS No. 205678-31-5 SDF Download SB273005 SDF
Smiles CNC1=CC=CC(=N1)CCOC2=CC3=C(CC(C(=O)N(C3)CC(F)(F)F)CC(=O)O)C=C2
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 90 mg/mL ( (199.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 16 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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