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Chemical Structure| 865608-11-3 Chemical Structure| 865608-11-3

Structure of CMPD101
CAS No.: 865608-11-3

Chemical Structure| 865608-11-3

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CMPD101 is a selective GRK2/3 inhibitor with IC50 values of 32 and 54 nM for GRK3 and GRK2, respectively.

Synonyms: CMPD101

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Product Details of CMPD101

CAS No. :865608-11-3
Formula : C24H21F3N6O
M.W : 466.46
SMILES Code : CN1C(CNC2=CC(C(NCC3=C(C(F)(F)F)C=CC=C3)=O)=CC=C2)=NN=C1C4=CC=NC=C4
Synonyms :
CMPD101
MDL No. :MFCD30182336

Safety of CMPD101

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of CMPD101

epigenetics
GPCR
cytoskeleton

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
3T3-L1 fibroblasts 3 µM 12 h CMPD101 significantly attenuated the detrimental effects of aldosterone on βAR signaling, as evidenced by restored ERK activation and cAMP production. Front Pharmacol. 2019 Aug 9;10:888
3T3-L1 fibroblasts 3 µM 12 h CMPD101 significantly attenuated the detrimental effects of aldosterone on insulin signaling, as evidenced by reduced phosphorylation of IRS1 (ser307pIRS1) and restored Akt activity. Front Pharmacol. 2019 Aug 9;10:888
HEK293A cells 10 µM CMPD101 at concentrations ≤10 µM showed high similarity to genetic knockout approaches, validating its specificity. However, off-target effects were observed at high concentrations (≥30 µM). Sci Rep. 2020 Oct 15;10(1):17395
HEK 293 cells 3 μM and 30 μM 30 min To assess the effect of Cmpd101 on DAMGO-induced MOPr phosphorylation, internalization, and arrestin translocation. Results showed that Cmpd101 concentration-dependently inhibited DAMGO-induced phosphorylation of MOPr at Ser375, arrestin-3 recruitment, and MOPr internalization. Mol Pharmacol. 2015 Aug;88(2):347-56
H295R cells 30 µM 6 h GRK2 blockade abolished isoproterenol’s effects on AngII-induced aldosterone synthesis/secretion Int J Mol Sci. 2020 Jan 16;21(2):574

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6N mice Female mice Intraperitoneal injection 15 mg/kg Single administration Enhanced κ-opioid receptor-mediated analgesia in female mice J Neurosci. 2018 Sep 12;38(37):8031-8043

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.72mL

2.14mL

1.07mL

21.44mL

4.29mL

2.14mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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