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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
α5β1; αvβ1; αvβ3; αvβ5; αvβ6; αvβ8
Available Sizes
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