(Z)-Isbogrel
(Z)-Isbogrel ((Z)-CV-4151) is a potent thromboxane A2 (TxA2) synthase inhibitor with an IC50 of 0.9 nM. (Z)-Isbogrel inhibits serum TxB2 production, with an ED50 of 0.01 mg/kg upon intravenous administration and an ED50 of 0.05 mg/kg upon oral administration in rats, and it exhibits no PAF receptor antagonistic activity. (Z)-Isbogrel can be used in research related to cardiovascular and cerebrovascular diseases.
For research use only. We do not sell to patients.
- CAS No.: 89667-39-0
- Formula: C18H19NO2
- Molecular Weight:281.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
TXA2 0.9 nM (IC50) |
In Vitro
(Z)-Isbogrel potently inhibits thromboxane A2 synthase activity in human platelet microsomes. When TxB2 production is measured using PGH2 as the substrate, the IC50 value is 0.9 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 89667-39-0
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Molecular Weight 281.36
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Formula C18H19NO2
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SMILES
C(=C/CCCCC(O)=O)(\C1=CC=CC=C1)/C=2C=CC=NC2
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Synonyms
(Z)-CV-4151
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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.
Protocols
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How to Select the Route of Administration for Mammals
Route-of-administration selection in mammals is a pharmacokinetic, pharmacodynamic, formulation, animal-welfare, and translational decision, not a default technical choice. The selected route should match the study goal: intravenous dosing is most useful when complete systemic exposure and rapid onset are required, oral dosing is most translational for orally intended medicines but is affected by absorption and first-pass metabolism, subcutaneous or intramuscular dosing can provide slower systemic exposure, and intraperitoneal dosing can be useful in rodent proof-of-concept studies but may have limited clinical translation. Published route-comparison studies show that the same compound can produce different exposure, onset, bioavailability, tissue distribution, and tolerability depending on route; therefore, route choice should be supported by pilot pharmacokinetic or pharmacodynamic evidence when the literature is insufficient. Unresolved questions include how to standardize route sel
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)