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Chemical Structure| 512177-83-2 Chemical Structure| 512177-83-2

Structure of CCR2-RA-[R]
CAS No.: 512177-83-2

Chemical Structure| 512177-83-2

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CCR2-RA-[R] is an allosteric antagonist that specifically inhibits the C-C chemokine receptor 2 (CCR2) with an IC50 of 103 nM, showing potential anti-inflammatory and antitumor activities.

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Product Details of CCR2-RA-[R]

CAS No. :512177-83-2
Formula : C18H19ClFNO3
M.W : 351.80
SMILES Code : O=C1N(C2=CC=C(Cl)C=C2F)[C@H](C3CCCCC3)C(C(C)=O)=C1O
MDL No. :MFCD11616183

Safety of CCR2-RA-[R]

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 CCR2-RA-[R]

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
U2OS-CCR2 cells 6 nM 120 min Determination of CCR2-RA-[R] binding affinity on CCR2, KD of 6.3 nM J Med Chem. 2018 Oct 25;61(20):9146-9161
U2OS-CCR1 cells 6 nM 120 min Determination of CCR2-RA-[R] binding affinity on CCR1, KD of 13.5 nM J Med Chem. 2018 Oct 25;61(20):9146-9161
CHO cells 7 nM 90 min To study the binding kinetics of CCR2-RA-[R] to CCR2, showing that BMS-681 enhanced [3H]-CCR2-RA binding Nature. 2016 Dec 15;540(7633):458-461

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice LPS-induced lung injury model Intraperitoneal injection 30 mg/kg Single dose, evaluated after 24 hours To evaluate the effect of CCR2 inhibitor on recruited macrophages, results showed PDX reduced macrophage infiltration by inhibiting CCR2 expression J Cell Mol Med. 2020 Sep;24(18):10604-10614

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.84mL

0.57mL

0.28mL

14.21mL

2.84mL

1.42mL

28.43mL

5.69mL

2.84mL

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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