DS37571084
DS37571084 is an orally active competitive antagonist of parathyroid hormone receptor 1 (PTH1R) with an IC50 value of 0.17 μM. DS37571084 is applicable to the research of bone diseases and calcium metabolism disorders associated with primary hyperparathyroidism.
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- CAS No.: 2460353-87-9
- Formule: C28H30Cl2N4O2
- Masse moléculaire:525.47
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[2]|
PTH1R 0.17 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
0.17 μM
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Inhibition of PTH-induced cAMP production in cAMP Hunter™ CHO-K1 PTHR1 Gs/Gq cells incubated for 30 min using a cAMP dynamic 2 kit.
Inhibition of PTH-induced cAMP production in cAMP Hunter™ CHO-K1 PTHR1 Gs/Gq cells incubated for 30 min using a cAMP dynamic 2 kit.
|
39519190 |
In Vitro
DS37571084 (10-100 μM; 30 min) potently inhibits PTHR1-induced cAMP production in cAMP Hunter™ CHO-K1 PTHR1 Gs/Gq cells with an IC50 of 0.17 μM[1].
DS37571084 exhibits metabolic stability in rat liver microsomes, with 65% of the compound remaining after 20 min of incubation at 1 μM[1].
DS37571084 shows no significant inhibitory activity against CYP 1A2, CYP 2C8, CYP 2C9, CYP 2C19, CYP 2D6, or CYP 3A4 at a concentration of 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
Chemical Information
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CAS No. 2460353-87-9
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Masse moléculaire 525.47
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Formule C28H30Cl2N4O2
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SMILES
O=C1N(C2=CC=C(NCCNC3CCOCC3)C=C2)C4=CC(Cl)=CC=C4C5=CC(Cl)=CN=C5C1(C)C
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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.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)