FR173657
FR173657 is an orally active bradykinin B2 receptor antagonist (IC50: 0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively). FR173657 (p.o.) inhibits BK-induced bronchoconstriction in guinea-pigs (ED50: 0.075 mg/kg). FR173657 (p.o.) also inhibits Carrageenin-induced paw oedema in mice (ED50: 6.8 mg/kg). FR173657 can be used for research of inflammatory disease.
For research use only. We do not sell to patients.
- CAS No.: 167838-64-4
- Formula: C30H27Cl2N5O4
- Molecular Weight:592.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Bradykinin Receptor Isoforms
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Biological Activity
0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1.4 nM
Compound: 87b
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Inhibition specific binding of [3H]BK (1.0 nM) to human Bradykinin receptor B2 which was expressed in CHO (Chinese hamster ovary) cells by 50%.
Inhibition specific binding of [3H]BK (1.0 nM) to human Bradykinin receptor B2 which was expressed in CHO (Chinese hamster ovary) cells by 50%.
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[PMID: 9767643] |
| CHO | IC50 |
1.4 nM
Compound: 5
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Inhibition of the specific binding of [3H]BK to human recombinant Bradykinin receptor B2 expressed in CHO cells.
Inhibition of the specific binding of [3H]BK to human recombinant Bradykinin receptor B2 expressed in CHO cells.
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[PMID: 9804698] |
| HEK293 | IC50 |
1.4 nM
Compound: 1, FK-3657
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Displacement of [3H]bradykinin from human recombinant B2 receptor expressed in HEK293 cells
Displacement of [3H]bradykinin from human recombinant B2 receptor expressed in HEK293 cells
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[PMID: 19552431] |
| MDA-MB-231 | IC50 |
20 μM
Compound: FR-173657
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Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs
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[PMID: 33139111] |
Chemical Information
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CAS No. 167838-64-4
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Molecular Weight 592.47
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Formula C30H27Cl2N5O4
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SMILES
O=C(NCC(N(C1=CC=C(Cl)C(COC2=C3N=C(C)C=CC3=CC=C2)=C1Cl)C)=O)/C=C/C4=CC=C(NC(C)=O)N=C4
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Synonyms
FK-3657
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)