CMPD101 |
| Catalog No.GC43286 |
CMPD101 est une petite molécule inhibitrice puissante, hautement sélective et perméable À la membrane de GRK2/3 avec une IC50 de 18 nM et 5,4 nM, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 865608-11-3
Sample solution is provided at 25 µL, 10mM.
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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).
| 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 |
| Solubility | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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