MK-7725
MK-7725 is a selective, orally active, and blood-brain barrier-permeable agonist of the subtype 3 of the frog skin peptide receptor (BRS-3). MK-7725 has a high affinity for the human BRS-3 (hBRS-3), with an IC50 of 3 nM, and its functional activity in the mouse-derived BRS-3 (mBRS-3) model with an EC50 of 22 nM (105% agonistic). MK-7725 significantly reduces the body weight of obese rats and obese dogs. MK-7725 can be used for the treatment of obesity.
For research use only. We do not sell to patients.
- CAS No.: 1034152-93-6
- Formula: C25H19F6N5O5S
- Molecular Weight:615.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
3.6 nM
Compound: 1, MK-7725
|
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
|
[PMID: 22494842] |
| CHO | IC50 |
3.6 nM
Compound: 14, MK-7725
|
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
|
[PMID: 24900461] |
| CHO-K1 | EC50 |
1.4 nM
Compound: 2, MK-7725
|
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
|
[PMID: 24412111] |
| CHO-K1 | EC50 |
130 nM
Compound: 1b, MK-7725
|
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
|
[PMID: 25497965] |
| CHO-K1 | EC50 |
22 nM
Compound: 2, MK-7725
|
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
|
[PMID: 24412111] |
| CHO-K1 | EC50 |
73 nM
Compound: 1b, MK-7725
|
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
|
[PMID: 25497965] |
Chemical Information
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CAS No. 1034152-93-6
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Molecular Weight 615.50
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Formula C25H19F6N5O5S
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SMILES
O=S(N1C2=C(C3=NOC(C(C)(O)C)=N3)C=CC=C2NC4=NC(C(F)(F)F)=CC=C4C1)(C5=CC=C(OC(F)(F)F)C=C5)=O
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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)