产品名称

英文名称：LY364947

同义词

396129-53-6、LY-364947、LY364947、4-(3-PYRIDIN-2-YL-1H-PYRAZOL-4-YL)QUINOLINE、4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)quinoline、LY 364947、TGF-beta RI Kinase Inhibitor、HTS 466284、4-(5-pyridin-2-yl-1H-pyrazol-4-yl)quinoline、HTS-466284、HTS466284、4-[3-(pyridin-2-yl)

产品性质

CAS编号：396129-53-6

分子式：C17H12N4

分子量：272.3

MDL号：MFCD00800758

PubChem编号：447966

英文别名：396129-53-6|LY-364947|LY364947|4-(3-PYRIDIN-2-YL-1H-PYRAZOL-4-YL)QUINOLINE|4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)quinoline|LY 364947|TGF-beta RI Kinase Inhibitor|HTS 466284|4-(5-pyridin-2-yl-1H-pyrazol-4-yl)quinoline|HTS-466284|HTS466284|4-[3-(pyridin-2-yl)

规格或纯度：≥98%

英文名称：LY364947

生化机理：LY 364947 is a diheteroaryl-substituted pyrazole compound used as a selective, ATP-competitive inhibitor of TGF-βRI (TGF-β Receptor I kinase). Studies of mouse fibroblasts show that LY 364947 inhibits cellular growth and transcription activation via TGF-β Receptor I kinase inhibition. In addition, TGF-β Receptor I kinase is responsible for fibroblast proliferation and the accumulation of astrocytes around the fibrotic scar when injury occurs to cells. In vitro studies report that in the presence of LY 364947 the amount of reactive astrocytes at the lesion site is also reduced. Furthermore, studies show that LY 364947 strongly effects intraplμg vasculature by increasing the extravasation of Dextran . LY 364947 is an inhibitor of eIF2 alpha, MLTK, p38 alpha and TGF β RII.

储存温度：2-8°C储存

运输条件：冰袋运输

备注：如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。有毒，请参阅SDS以获取更多信息。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

产品介绍：LY364947是一种有效的，ATP竞争性的TGFβR-I抑制剂，IC50为59 nM，比作用于TGFβR-II选择性高7倍。A selective ATP-competitive inhibitor of TGF-β Receptor I kinase.LY364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, shows 7-fold selectivity over TGFβR-II.A selective ATP-competitive inhibitor of TGF-β Receptor I kinase.

IUPAC Name：4-(5-pyridin-2-yl-1H-pyrazol-4-yl)quinoline

INCHI：InChI=1S/C17H12N4/c1-2-6-15-13(5-1)12(8-10-19-15)14-11-20-21-17(14)16-7-3-4-9-18-16/h1-11H,(H,20,21)

InChi Key：IBCXZJCWDGCXQT-UHFFFAOYSA-N

Canonical SMILES：C1=CC=C2C(=C1)C(=CC=N2)C3=C(NN=C3)C4=CC=CC=N4

Isomeric SMILES：C1=CC=C2C(=C1)C(=CC=N2)C3=C(NN=C3)C4=CC=CC=N4

WGK Germany：3

PubChem CID：447966

DrugBank Ligand：DB03921

ChEMBL Ligand：CHEMBL261454

CAS Registry No.：396129-53-6

RCSB PDB Ligand：PY1

溶解性：Soluble in DMSO (100 mM), water (<1 mg/ml at 25 °C), ethanol (<1 mg/ml at 25 °C), DMF (~0.1 mg/ml), and 11 DMFPBS (pH 7.2) (~0.5 mg/ml).

熔点：230°C

象形图：

信号词：Danger

危险声明：H315 Causes skin irritationH319 Causes serious eye irritationH335 May cause respiratory irritationH301 Toxic if swallowedH400 Very toxic to aquatic life

预防措施声明：P261,P305+P351+P338,P273,P301+P310

个人防护装备：Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges

产品包装