CMPD101

Cat. No. 5642 7 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent and selective GRK2/3 inhibitor

化学名： 3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide

纯度： ≥98% (HPLC)

引用文献 (7)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for CMPD101

CMPD101 is a potent and selective GRK2/3 inhibitor (IC₅₀ values are 32 and 54 nM for GRK3 and GRK2, respectively). Exhibits selectivity for GRK2/3 over GRK1/5. Reduces DAMGO-induced desensitization and internalization of μ-opioid receptors.

技术数据 for CMPD101

分子量	466.46
公式	C₂₄H₂₁F₃N₆O
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	865608-11-3
PubChem ID	11677079
InChI Key	WFOVEDJTASPCIR-UHFFFAOYSA-N
Smiles	CN1C(CNC2=CC(C(NCC3=CC=CC=C3C(F)(F)F)=O)=CC=C2)=NN=C1C4=CC=NC=C4

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for CMPD101

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	46.65	100
	ethanol	46.65	100

制备储备液 for CMPD101

以下数据基于产品分子量 466.46。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	2.14 mL	10.72 mL	21.44 mL
5 mM	0.43 mL	2.14 mL	4.29 mL
10 mM	0.21 mL	1.07 mL	2.14 mL
50 mM	0.04 mL	0.21 mL	0.43 mL

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产品说明书 for CMPD101

分析证书/产品说明书

化学品安全技术说明书

参考文献 for CMPD101

参考文献是支持产品生物活性的出版物。

Lowe et al (2015) Role of G protein-coupled receptor kinases 2 and 3 in μ-opioid receptor desensitization and internalization. Mol.Pharmacol. 88 347 PMID: 26013542

Thal et al (2011) Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors. Mol.Pharmacol. 80 294 PMID: 21596927

Okawa et al (2017) Design, synthesis, and evaluation of the highly selective and potent G-protein-coupled receptor kinase 2 (GRK2) inhibitor for the potential treatment of heart failure. J.Med.Chem. 60 6942 PMID: 28699740

If you know of a relevant reference for CMPD101, please let us know.

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关键词: CMPD101, CMPD101 supplier, potent, selective, GRK2, GRK3, inhibitors, inhibits, receptors, GPCRs, desensitization, kinases, Heterotrimeric, G-protein, GTPases, 5642, Tocris Bioscience