IPR agonist-1
IPR agonist-1 is a prostaglandin-based IP receptor agonist. IPR agonist-1 binds to the IP receptor, forms hydrogen bonds with Tyr75-Ser168-Arg279, and undergoes π-π stacking with Tyr281, thereby triggering downstream signaling pathways. IPR agonist-1 inhibits ADP (Adenosine 5'-diphosphate) (HY-W010918)-induced platelet aggregation in rabbit platelet-rich plasma. IPR agonist-1 can be used in the research of pulmonary arterial hypertension.
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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: 3085716-86-2
- 分子式: C25H24D3N3O3
- 分子量:420.52
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
体外実験
IPR agonist-1 (7a-19) potently inhibits ADP-induced platelet aggregation in rabbit platelet-rich plasma with an IC50 of 0.97 μM[1].
IPR agonist-1 (7a-19) binds robustly to the prostanoid IP receptor, forming critical hydrogen-bonding and π-π stacking interactions that align with its potent agonist activity[1].
IPR agonist-1 (4 h) shows exceptional metabolic stability in rat liver microsomes, with 96.7% of the parent compound remaining after 4 h of incubation and minimal M1 metabolite formation[1].
IPR agonist-1 does not exert significant hERG potassium channel inhibition in stably transfected HEK293 cells, with an IC50 of 143.1 μM[1].
IPR agonist-1 is nonmutagenic in the Mini-Ames assay across multiple bacterial strains, with or without metabolic activation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) rats[1]
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Dosage:1.0 mg/kg (i.v.); 5.0 mg/kg (p.o.)
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Administration:i.v.; single dose; p.o.; single dose
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Result:Exhibited a terminal half-life of 12.0 h, an initial plasma concentration of 6.20 μg/mL, and a systemic exposure of 26.7 h·μg/mL after intravenous administration of 1.0 mg/kg.
Exhibited a terminal half-life of 10.5 h, a maximum plasma concentration of 2.29 μg/mL reached at 3.0 h, a systemic exposure of 63.1 h·μg/mL, and an oral bioavailability of 47.3% after oral administration of 5.0 mg/kg.
化学情報
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CAS 番号 3085716-86-2
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分子量 420.52
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分子式 C25H24D3N3O3
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SMILES
[2H]C([2H])([2H])N([C@@H]1CC[C@H](OCC(O)=O)CC1)C2=NC(C3=CC=CC=C3)=C(C4=CC=CC=C4)N=C2
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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.
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)
IPR agonist-1 関連分類
HY-187539S 関連分類
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Keywords
- IPR agonist-1
- 3085716-86-2
- IPR agonist1
- IPR agonist 1
- Prostaglandin Receptor
- Mini-Ames assay
- HEK293 cells
- bacterial strains
- platelet aggregation
- pulmonary arterial hypertension
- Sprague-Dawley rats
- rabbit platelet-rich plasma
- prostanoid IP receptor
- hERG potassium channel
- rat liver microsomes
- Inhibitor
- inhibitor
- inhibit