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CMPD101

カタログ番号GC43286

CMPD101 は、それぞれ 18 nM および 5.4 nM の IC50 を持つ、強力で高度に選択的で膜透過性の GRK2/3 の低分子阻害剤です。

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CMPD101 化学構造

Cas No.: 865608-11-3

サイズ 価格 在庫数 個数
1mg
$44.00
在庫あり
5mg
$146.00
在庫あり
10mg
$245.00
在庫あり
25mg
$556.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

CMPD101 is an inhibitor of G protein-coupled receptor kinase 2 (GRK2) and GRK3 (IC50s = 18 and 5.4 nM, respectively). [1] It is selective for GRK2 and GRK3 over GRK1, GRK5, GRK6, and GRK7 (IC50s = 3,100, 2,300, >30,000, and 25,000 nM, respectively), as well as Rho-associated kinase 2 (ROCK-2) and PKCα (IC50s = 1,400 and 8,100 nM, respectively). CMPD101 induces cAMP accumulation in HEK293 cells expressing human β2-adrenergic receptors (EC50 = 10 µM). In isolated human prostate strips, CMPD101 (50 µM) inhibits contractions induced by electrical field stimulation, norepinephrine, phenylephrine, endothelin-1 , and U-46619 . [2]

Reference:
[1]. Okawa, T., Aramaki, Y., Yamamoto, M., 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. 60(16), 6942-6990 (2017).
[2]. Yu, Q., Gratzke, C., Wang, Y., et al. Inhibition of prostatic smooth muscle contraction by the inhibitor of G protein-coupled receptor kinase 2/3, CMPD101. Eur. J. Pharmacol. 831, 9-19 (2018).

Chemical Properties

Cas No. 865608-11-3 SDF
Canonical SMILES O=C(C1=CC=CC(NCC2=NN=C(C3=CC=NC=C3)N2C)=C1)NCC4=CC=CC=C4C(F)(F)F
Formula C24H21F3N6O M.Wt 466.5
溶解度 10mg/mL in ethanol, 20mg/mL in DMSO, or in DMF Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.1436 mL 10.7181 mL 21.4362 mL
5 mM 0.4287 mL 2.1436 mL 4.2872 mL
10 mM 0.2144 mL 1.0718 mL 2.1436 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 31 reference(s) in Google Scholar.)

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