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.
For research use only. We do not sell to patients.
- CAS No.: 3085716-86-2
- Formula: C25H24D3N3O3
- Molecular Weight:420.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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.
Chemical Information
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CAS No. 3085716-86-2
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Molecular Weight 420.52
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Formula 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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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)
IPR agonist-1 Related Classifications
HY-187539S Related Classifications
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- 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