2. GPCR/G Protein Immunology/Inflammation Metabolic Enzyme/Protease
  3. Adenosine Receptor Interleukin Related IFNAR Cytochrome P450
  4. Adenosine receptor antagonist 6

Adenosine receptor antagonist 6, a (S)-enantiomer compound, is an orally active and selective A2A adenosine receptor (A2AAR) antagonist. Adenosine receptor antagonist 6 binds to the A2A adenosine receptor with a Ki of 19.18 nM. Adenosine receptor antagonist 6 inhibits 5’-N-ethylcarboxamide adenosine (NECA) (HY-103173)-mediated cAMP production (IC50 = 0.089 μM) and immunosuppression, while promoting IL-2 and IFN-γ secretion. Adenosine receptor antagonist 6 abolishes the immunosuppressive effects of adenosine on T-cell activation and cytokine release. Adenosine receptor antagonist 6 inhibits tumor growth in a CT26/MC38 xenograft model. Adenosine receptor antagonist 6 can be used for the study of colon cancer.

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Adenosine receptor antagonist 6

Adenosine receptor antagonist 6 Chemical Structure

CAS No. : 2913578-04-6

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Adenosine receptor antagonist 6 Related Antibodies

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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Description

Adenosine receptor antagonist 6, a (S)-enantiomer compound, is an orally active and selective A2A adenosine receptor (A2AAR) antagonist. Adenosine receptor antagonist 6 binds to the A2A adenosine receptor with a Ki of 19.18 nM. Adenosine receptor antagonist 6 inhibits 5’-N-ethylcarboxamide adenosine (NECA) (HY-103173)-mediated cAMP production (IC50 = 0.089 μM) and immunosuppression, while promoting IL-2 and IFN-γ secretion. Adenosine receptor antagonist 6 abolishes the immunosuppressive effects of adenosine on T-cell activation and cytokine release. Adenosine receptor antagonist 6 inhibits tumor growth in a CT26/MC38 xenograft model. Adenosine receptor antagonist 6 can be used for the study of colon cancer[1].

In Vitro

Adenosine receptor antagonist 6 (Compound 11a) exhibits selective binding to A1, A2B and A3 adenosine receptors with Ki values of 392.23 nM, 2129 nM, and 9036 nM, respectively[1].
Adenosine receptor antagonist 6 (0.001-100 μM) exhibits dose-dependent inhibition of 5’-N-ethylcarboxamide adenosine (NECA) (HY-103173)-mediated cAMP production with an IC50 of 0.089 μM in activated primary human PBMCs[1].
Adenosine receptor antagonist 6 (0.1-10 μM) abolishes the immunosuppressive effects of adenosine on T-cell activation and cytokine release in activated primary human PBMCs [1].
Adenosine receptor antagonist 6 (0.03-3 μM) inhibits the NECA-mediated immunosuppression and restores the secretion of IL-2 and IFN-γ in activated primary human PBMCs [1].
Adenosine receptor antagonist 6 (0.8125-50 μM, 48 h) inhibits the proliferation of HCT116 cells (IC50 = 17.21 μM), MDA-MB-231 cells (IC50 = 53.77 μM), MC38 cells (IC50 = 18.91 μM), and CT26 cells (IC50 = 19.36 μM)[1].
Adenosine receptor antagonist 6 exhibits lower metabolic clearance by CYP450 enzymes, with CYP1A2 playing a major role in their stereoselective metabolism[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Adenosine receptor antagonist 6 Related Antibodies
In Vivo

Adenosine receptor antagonist 6 (Compound 11a) (15-25 mg/kg, p.o., once daily, 19-21 days) inhibits tumor growth in a CT26/MC38 xenograft model when used alone or combined with PD-L1 monoclonal antibody[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CT26 cancer cells (5 × 105 in 100 μL) were injected subcutaneously into both flanks of BALB/c mice[1]
Dosage: 25 mg/kg
Administration: p.o. once daily for 19 days
Result: Demonstrated a tumor growth inhibition rate (TGI) of 37%.
Exhibited significant enhancement of efficacy (TGI = 92%) when combined with PD-L1 monoclonal antibody (10 mg/kg, i.p., b.i.w.).
Animal Model: MC38 cancer cells (5 × 105 in 100 μL) were injected subcutaneously into both flanks of C57BL/6 mice[1]
Dosage: 15 mg/kg
Administration: p.o. once daily for 21 days
Result: Demonstrated a tumor growth inhibition rate (TGI) of 69.74%.
Exhibited significant enhancement of efficacy (TGI = 98.1%) when combined with PD-L1 monoclonal antibody (10 mg/kg, i.p., b.i.w.).
Molecular Weight

332.36

Formula

C18H16N6O
CAS No.
SMILES

O=C(C1=CN2C3=CC=CC=C3N=C2C(N)=N1)N[C@@H](C)C4=NC=CC=C4
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Adenosine receptor antagonist 6 Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Adenosine receptor antagonist 62913578-04-6Adenosine receptor antagonist6Adenosine receptor antagonist-6Adenosine ReceptorInterleukin RelatedIFNARCytochrome P450P1 receptorILInterferon-α/β receptorInterferon-alpha/beta receptor CYPsAdenosine receptorcolon cancerchiral compoundInhibitorinhibitorinhibit

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