Chemical Structure : Integrin α5β1 inhibitor MRT1
CAS No.:
3012561-21-3
Integrin α5β1 inhibitor MRT1
货号: 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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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
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.
物理化学性质&存储条件
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分子量
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463.58
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分子式
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C26H33N5O3
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外观性状
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Solid
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CAS No.
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储存条件
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- 固体粉末
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-20°C 12 个月; 4°C 6 个月
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- 配置液
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-80°C 6 个月; -20°C 6 个月
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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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参考文献
1. Lemay SE, et al. Circulation. 2025 Jan 20. doi: 10.1161/CIRCULATIONAHA.124.070693.
