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Cat. No. M10957
MK-0429 Structure


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Biological Activity

MK-0429 (L-000845704) is an oral, highly effective, selective, non-peptide integrin ubiquitous antagonist for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1 IC5 0 The values are 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM, and 12.2 nM, respectively.

Chemical Information
Molecular Weight 439.52
Formula C23H29N5O4
CAS Number 227963-15-7
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Anya Gupta, et al. J Org Chem. Thermodynamic Understanding of an Aza-Michael Reaction Enables Five-Step Synthesis of the Potent Integrin Inhibitor MK-0429

[2] Ji Zhang, et al. Sci Rep. Discovery of a new class of integrin antibodies for fibrosis

[3] Izabela Łasiska, et al. Anticancer Agents Med Chem. Integrins as A New Target for Cancer Treatment

[4] Xiaoyan Zhou, et al. Pharmacol Res Perspect. An integrin antagonist (MK-0429) decreases proteinuria and renal fibrosis in the ZSF1 rat diabetic nephropathy model

[5] Maureen Pickarski, et al. Oncol Rep. Orally active αvβ3 integrin inhibitor MK-0429 reduces melanoma metastasis

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Keywords: MK-0429, L-000845704 supplier, Integrin, inhibitors, activators

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