Azalanstat dihydrochloride
Azalanstat dihydrochloride (RS-21607 dihydrochloride) is an inhibitor of heme oxygenase and lanosterol 14α-demethylase, with inhibitory activity against HO-1 (IC50 = 5.5 µM) and HO-2 (IC50 = 24.5 µM). Azalanstat dihydrochloride reduces the maturation rate of rat oocytes, increases rat oocyte degeneration, and partially inhibits progesterone production in preovulatory follicles of rats.
For research use only. We do not sell to patients.
- CAS No.: 143484-82-6
- Formula: C22H26Cl3N3O2S
- Molecular Weight:502.88
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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HO-1 |
HO-2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
13 μM
Compound: QC-1
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Cytotoxicity against CHO cell line
Cytotoxicity against CHO cell line
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[PMID: 16495054] |
Azalanstat dihydrochloride (Compound I) inhibits rat spleen microsomal HO-1 (IC50 = 5.8 μM) and rat brain microsomal HO-2 (IC50 = 28.0 μM) in vitro, with a selectivity index of 5 for HO-1 over HO-2[1].
Azalanstat dihydrochloride (0-100 μM) inhibits the activity of rat liver microsomal CYP3A1/3A2 in vitro, with an IC50 of 48.1 μM[1].
Azalanstat dihydrochloride (0-200 μM; 3-24 h, or 6 h + 24 h inhibitor-free culture) reduces GVBD in a dose- and time-dependent manner at high concentrations (≥50 μM for 6 h treatment, ≥10 μM for 24 h treatment), while increasing the degree of oocyte degeneration; notably, oocyte degeneration becomes irreversible after 6 h of treatment at 100 μM[2].
Azalanstat dihydrochloride (1-100 μM; 6-24 h with 5 μg/mL LH) reduces LH-induced GVBD in a dose-dependent manner, accompanied by increased degeneration of oocytes and follicles at 1-100 μM with a 24 h treatment[2].
Azalanstat dihydrochloride (1-100 μM; 6-24 h with 5 μg/mL LH) partially inhibits LH-induced progesterone synthesis in preovulatory rat follicles in vitro in a dose-dependent manner when applied at concentrations of 1, 50, and 100 μM for 6 or 24 h[2].
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:Wistar-derived rats (female, 23-24 days of age, injected with 10 IU eCG then 4 IU hCG to induce ovulatory dysfunction model)[2]
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Dosage:2.15-215 μg/bursa
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Administration:intrabursal injection; single dose
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Result:Caused statistically significant inhibition of ovulation.
Chemical Information
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CAS No. 143484-82-6
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Molecular Weight 502.88
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Formula C22H26Cl3N3O2S
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SMILES
ClC(C=C1)=CC=C1CC[C@]2(O[C@@H](CO2)CSC3=CC=C(C=C3)N)CN4C=CN=C4.Cl.Cl
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Synonyms
RS-21607 dihydrochloride
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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)