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CMPD101

目录号: PL09899 纯度: ≥98%

CMPD101 是一种高效、高选择性、膜透性的 GRK2/3 小分子抑制剂，IC50 分别为 18 nM 和 5.4 nM。CMPD101 针对 GRK1、GRK5 ROCK-2 和 PKCα 的选择性较小，IC50 值分别为 3.1 μM，2.3 μM，1.4 μM 和 8.1 μM。CMPD101 可用于心衰疾病的研究。

CAS No. :865608-11-3

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中文名称	CMPD101
中文别名	化合物CMPD101
英文名称	CMPD101
英文别名	cmpd101;compound 101 [PMID: 21596927];Takeda compound 101;3-({[4-Methyl-5-(Pyridin-4-Yl)-4h-1,2,4-Triazol-3-Yl]methyl}amino)-N-[2-(Trifluoromethyl)benzyl]benzamide;3-[(4-methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide;3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide;compound 101;3pvu;QRW;CID 11677079;3-[(4-methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylam;CMPD101;Benzamide, 3-[[[4-methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]-;Takeda101
Cas No.	865608-11-3
分子式	C₂₄H₂₁F₃N₆O
分子量	466.46
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	CMPD101 是一种高效、高选择性、膜透性的 GRK2/3 小分子抑制剂，IC50 分别为 18 nM 和 5.4 nM。CMPD101 针对 GRK1、GRK5 ROCK-2 和 PKCα 的选择性较小，IC50 值分别为 3.1 μM，2.3 μM，1.4 μM 和 8.1 μM。CMPD101 可用于心衰疾病的研究。

产品详情	CMPD101 是一种高效、高选择性、膜透性的 GRK2/3 小分子抑制剂，IC₅₀ 分别为 18 nM 和 5.4 nM。CMPD101 针对 GRK1、GRK5 ROCK-2 和 PKCα 的选择性较小，IC₅₀ 值分别为 3.1 μM，2.3 μM，1.4 μM 和 8.1 μM。CMPD101 可用于心衰疾病的研究。
生物活性	CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC 50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC 50 s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.
性状	Solid
IC50 & Target[1][2]	GRK2 18 nM (IC50) GRK3 5.4 nM (IC50
体外研究(In Vitro)	CMPD101 (100 μM; pre-20 mins) inhibit the internalization of β2AR, remarkably decreases the isoproterenol-induced formation of clathrin-coated vesicles and the β2AR-GFP fusion protein remained on the plasma membrane in HEK-B2 cell line. CMPD101 (3-30 μM; pre-30 minutes) produced a robust phosphorylation of Ser375, which is partially inhibited by pretreatment of cells for 30 minutes with 3 μM Cmpd101 and fully blocked by pretreatment with 30 μM Cmpd101. It also inhibits phosphorylation of MOPr at Thr370, Thr376, and Thr379 residues. CMPD101 (3-30 μM; pre-30 minutes) does not affect the DAMGO-induced increase in ERK1/2 and Elk-1 phosphorylation, at 30 μM, this compound produces a small increase in basal ERK1/2 phosphorylation in HEK 293 cells expressing HA-MOPrs. has not independently confirmed the accura
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Okawa T, et al. 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. 2017 Aug 24;60(16):6942-6990. [2]. Yu Q, et al. Inhibition of prostatic smooth muscle contraction by the inhibitor of G protein-coupled receptor kinase 2/3, CMPD101.Eur J Pharmacol. 2018 Jul 15;831:9-19.

溶解度数据	In Vitro: DMSO : 250 mg/mL (535.95 mM; Need ultrasonic)配制储备液

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[1]. Okawa T, et al. 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. 2017 Aug 24;60(16):6942-6990.
[2]. Yu Q, et al. Inhibition of prostatic smooth muscle contraction by the inhibitor of G protein-coupled receptor kinase 2/3, CMPD101.Eur J Pharmacol. 2018 Jul 15;831:9-19.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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