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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2460353-87-9
- 分子式: C28H30Cl2N4O2
- 分子量:525.47
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
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
|
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 |
体外実験
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
化学情報
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CAS 番号 2460353-87-9
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分子量 525.47
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)