Chemical Structure : Integrin α5β1 inhibitor MRT1
CAS No.:
3012561-21-3
Integrin α5β1 inhibitor MRT1
Catalog No.: PC-23935Not For Human Use, Lab Use Only.
Integrin α5β1 inhibitor MRT1 is a specific small molecule inhibitor of RGD (arginylglycylaspartic acid)-binding integrin α5β1 with IC50 of 40 nM in fluorescence polarization assays, and IC50 of 18 and 54 nM for other RGD binding β1 integrins αvβ1 and α8β1.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Integrin α5β1 inhibitor MRT1 is a specific small molecule inhibitor of RGD (arginylglycylaspartic acid)-binding integrin α5β1 with IC50 of 40 nM in fluorescence polarization assays, and IC50 of 18 and 54 nM for other RGD binding β1 integrins αvβ1 and α8β1.
MRT1 is inactive against members of the collagen- and laminin-binding integrinsubfamilies.
MRT1 inhibits integrin activityin cell-based ligand binding assays with similar IC50 values.
MRT1 (0.25-4 uM) treatment dose-dependently reduces the pro-proliferative and apoptosis-resistant phenotype of pulmonary arterialhypertension pulmonary artery smooth muscle cells.
MRT1 alone or combined with macitentan and tadalafil attenuates established pulmonary arterial hypertension in Sugen/hypoxia rats.
MRT1 reduces vascular remodeling in human precision-cut lung slices.
Physicochemical Properties
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M.Wt
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463.58
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Formula
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C26H33N5O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-(1,3-dimethyl-1H-indazol-7-yl)-2-(3-(4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)butoxy)azetidin-1-yl)acetic acid
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References
1. Lemay SE, et al. Circulation. 2025 Jan 20. doi: 10.1161/CIRCULATIONAHA.124.070693.
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