MK-0429

MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC50 values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively[1][2][3].

Product Specifications

CAS Number

[227963-15-7]

Product Name Alternative

L-000845704

UNSPSC

12352005

Hazard Statement

H360, H373

Target

Integrin

Type

Reference compound

Related Pathways

Cytoskeleton

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Cancer

Assay Protocol

https://www.medchemexpress.com/MK-0429.html

Purity

99.50

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : 2.78 mg/mL (ultrasonic)

Smiles

O=C1N([C@H](C2=CC=C(OC)N=C2)CC(O)=O)CCN1CCCC3=NC4=C(C=C3)CCCN4

Molecular Formula

C23H29N5O4

Molecular Weight

439.51

Precautions

H360, H373

References & Citations

[1]Hutchinson JH, et al. Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis. J Med Chem. 2003 Oct 23;46 (22) :4790-8.|[2]Pickarski M, et al. Orally active αvβ3 integrin inhibitor MK-0429 reduces melanoma metastasis. Oncol Rep. 2015 Jun;33 (6) :2737-45.|[3]Xiaoyan Zhou, et al. An integrin antagonist (MK-0429) decreases proteinuria and renal fibrosis in the ZSF1 rat diabetic nephropathy model. Pharmacol Res Perspect. 2017 Oct;5 (5) :e00354.