MRS4608
MRS4608 (Compound 17) is a selective P2Y14 receptor antagonist with IC50 values of 20 (hP2Y14R) and 21.4 nM (mP2Y14R). MRS4608 has anti-inflammatory activity and can reduce the infiltration of eosinophils. MRS4608 can be used for the researches of inflammation and immunology, such as asthma.
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- CAS No.: 2370976-04-6
- Formule: C31H26F3NO2
- Masse moléculaire:501.54
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
|
hP2Y14R 20 nM (IC50) |
mP2Y14R 21.4 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.02 μM
Compound: 17
|
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
|
[PMID: 32787142] |
| CHO | IC50 |
38.1 nM
Compound: 17
|
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assay
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assay
|
[PMID: 32787142] |
| CHO | IC50 |
57 nM
Compound: 17
|
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assay
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assay
|
[PMID: 32787142] |
| CHO | IC50 |
84.5 nM
Compound: 17
|
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assay
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assay
|
[PMID: 32787142] |
| HEK293 | IC50 |
21.4 nM
Compound: 17
|
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
|
[PMID: 32787142] |
| HepG2 | IC50 |
>20 μM
Compound: 17
|
Toxicity in human HepG2 cells
Toxicity in human HepG2 cells
|
[PMID: 32787142] |
Chemical Information
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CAS No. 2370976-04-6
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Masse moléculaire 501.54
-
Formule C31H26F3NO2
-
SMILES
O=C(C1=CC2=C(C(C3=CC=C(C45CCN(CC5)CC4)C=C3)=C1)C=CC(C6=CC=C(C(F)(F)F)C=C6)=C2)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)