Integrin Inhibitors

αvβ1

αvβ3

αvβ5

αvβ6

αvβ8

α5β1

α1β1

α2β1

α4β1

α9β1

αIIbβ3

α4β7

αLβ2

Integrin Inhibitors, Agonists & Antagonists

Product Name	αvβ1	αvβ3	αvβ5	αvβ6	αvβ8	α5β1	α1β1	α2β1	α4β1	α9β1	αIIbβ3	α4β7	αLβ2	Purity
Cilengitide		αvβ3, IC₅₀: 4 nM (αvβ3-Vitronectin interaction^[2]) αvβ3, IC₅₀: 0.61 nM (^[1])	αvβ5, IC₅₀: 79 nM (αvβ5-Vitronectin interaction^[2]) αvβ5, IC₅₀: 8.4 nM (^[1])			α5β1, IC₅₀: 14.9 nM (^[1])								99.80%
Cyclo(-RGDfK)		αvβ3, IC₅₀: 0.94 nM												≥98.0%
Volociximab						α5β1, EC₅₀: 0.2 nM
MK-0429	αvβ1, IC₅₀: 1.6 nM (inhibition of fibronectin-binding )	αvβ3, IC₅₀: 2.8 nM (inhibition of vitronectin-binding)	αvβ5, IC₅₀: 0.1 nM (inhibition of vitronectin-binding)	αvβ6, IC₅₀: 0.7 nM (inhibition of LAP-binding)	αvβ8, IC₅₀: 0.5 nM (inhibition of LAP-binding)	α5β1, IC₅₀: 12.2 nM (inhibition of fibronectin-binding)								99.08%
Lifitegrast													αLβ2	99.21%
Bexotegrast	αvβ1, Kd: 3.4 nM			αvβ6, Kd: 5.7 nM										98.09%
RGD peptide (GRGDNP) (TFA)						α5β1								99.41%
Natalizumab									α4β1					99.10%
Firategrast									α4β1			α4β7		99.62%
Etrolizumab												α4β7		99.56%
BIO5192								α2β1, IC₅₀: 1053 nM	α4β1, IC₅₀: 1.8 nM	α9β1, IC₅₀: 138 nM		α4β7, IC₅₀: >500 nM		99.96%
BTT-3033								α2β1, EC₅₀: 130 nM						99.22%
Integrin modulator 1									α4β1, IC₅₀: 9.8 nM					99.44%
Cyclo(Arg-Gly-Asp-D-Phe-Cys)		αvβ3												99.70%
TC-I 15							α1β1, IC₅₀: 23.6 (α1β1 μM α1β1, IC₅₀: 24.4 (α1β1 μM	α2β1, IC₅₀: 0.4 (α2β1 μM α2β1, IC₅₀: 26.8 (α2β1 μM						99.80%
TR-14035									α4β1, IC₅₀: 87 nM			α4β7, IC₅₀: 7 nM		98.06%
Cyclo(-RGDfK) TFA		αvβ3, IC₅₀: 0.94 nM												99.82%
RGD peptide (GRGDNP)						α5β1								99.63%
αvβ5 integrin-IN-1			αvβ5, pIC₅₀: 8.2											99.72%
BIO5192 hydrate								α2β1, IC₅₀: 1053 nM	α4β1, IC₅₀: 1.8 nM	α9β1, IC₅₀: 138 nM		α4β7, IC₅₀: >500 nM		99.78%
Lifitegrast sodium													αLβ2	99.33%
Cyclo(RGDyK)		αvβ3, IC₅₀: 20 nM												99.73%
EMD527040				αvβ6, IC₅₀: 6 nM										99.94%
HSDVHK-NH2		αvβ3, IC₅₀: 2.74 nM												98.41%
BIO-1211									α4β1, IC₅₀: 4 nM			α4β7, IC₅₀: 2 μM		99.94%
Echistatin TFA		αvβ3				α5β1					αIIbβ3			98.07%
RO0270608									α4β1			α4β7		98.69%
Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA		αvβ3												98.00%
BOP sodium									α4β1	α9β1				99.11%
Levocabastine									α4β1
Echistatin		αvβ3				α5β1					αIIbβ3
Nesvategrast		αvβ3, IC₅₀: 0.6 nM		αvβ6, IC₅₀: 8 nM	αvβ8, IC₅₀: 13 nM
Orbofiban											GPIIb/IIIa
Orbofiban acetate											GPIIb/IIIa			98.13%
R-BC154 acetate										α9β1
Tadocizumab											GPIIb/IIIa
Valategrast hydrochloride									α4β1			α4β7
JNJ-26076713		αvβ3, IC₅₀: 2.3 nM	αvβ5, IC₅₀: 6.3 nM
K34c						α5β1
αvβ6 integrin inhibitor 2				αvβ6, IC₅₀: 96.5 nM

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