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Chemical Structure| 2437547-04-9 Chemical Structure| 2437547-04-9

Structure of CCR6 inhibitor 1
CAS No.: 2437547-04-9

Chemical Structure| 2437547-04-9

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CCR6 inhibitor 1 is a highly efficient and selective CCR6 inhibitor, with IC50 values of 0.45 and 6 nM for monkey and human CCR6, respectively, showing significantly higher selectivity for CCR1 and CCR7 (IC50 values of > 30000 nM and 9400 nM, respectively), and can significantly inhibit ERK phosphorylation, suitable for research on autoimmune diseases and cancer.

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Product Details of CCR6 inhibitor 1

CAS No. :2437547-04-9
Formula : C24H23F3N4O3S
M.W : 504.52
SMILES Code : O=S([C@@H]1CC[C@@H](NC2=NC=C(C=C2)C(F)(F)F)CC1)(C3=CC=C(C=C3)C4=CC=NC(C(N)=O)=C4)=O
MDL No. :N/A

Safety of CCR6 inhibitor 1

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 CCR6 inhibitor 1

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human peripheral blood mononuclear cells (PBMC) 150 μg/mL 24 hours EPS-R1 increased the CCR6+ population among CD8+ T cells in human PBMCs PMC9662940
Mouse splenocytes 150 μg/mL 24 hours EPS-R1 significantly increased the CCR6+ population among CD8+ T cells but not among CD4+ T cells PMC9662940
Splenic B cells 500 ng/ml CCL20 or 1000 ng/ml CXCL13 6 hours To study the migration ability of Id3−/− Apoe−/− B cells in response to CCL20 and CXCL13 PMC3253259
T lymphocytes 200 nM 1-90 minutes To study the effect of LARC on protein kinase B activation, results showed that LARC did not activate protein kinase B. PMC2193218

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Colon26 colon adenocarcinoma and 4T1 mammary tumor models Oral 25 μg/mL Continuous ingestion starting from day 0 EPS-R1 ingestion enhanced the antitumor effects of anti-CTLA-4 or anti-PD-1 monoclonal antibodies against CCL20-expressing tumors, increasing infiltrating CCR6+ CD8+ T cells and accompanied by a substantial immune response gene expression signature PMC9662940
C57BL/6 mice Hepatocellular carcinoma (HCC) model Intraperitoneal injection 25 mg/kg Daily Evaluate the effect of TREM-1 inhibitor GF9 on tumor growth and immunosuppression, showing that GF9 significantly inhibits tumor growth and improves CD8+ T cell function. PMC6618281
Mice SKG mouse model Intravenous injection 100 μg Once a week for 5 weeks Suppressed the onset and severity of arthritis PMC2118525

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.91mL

1.98mL

0.99mL

19.82mL

3.96mL

1.98mL

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
 

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