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CMPD101

رقم الكتالوجGC43286

CMPD101 هو مثبط جزيء صغير قوي وانتقائي للغاية ونفاذ الغشاء لـ GRK2 / 3 مع IC50 من 18 نانومتر و 5.4 نانومتر ، على التوالي

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CMPD101 التركيب الكيميائي

Cas No.: 865608-11-3

الحجم السعر المخزون الكميّة
1mg
44٫00
متوفر
5mg
146٫00
متوفر
10mg
245٫00
متوفر
25mg
556٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of CMPD101

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 of CMPD101

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
الذوبان 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 of CMPD101

Prepare stock solution
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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In vivo Formulation Calculator (Clear solution) of CMPD101

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 31 reference(s) in Google Scholar.)

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