SR210831C
SR210831C is a highly selective, orally active retinoic acid receptor α (RARα) inhibitor with an IC50 of 0.051 nM. SR210831C suppresses spermatogenesis by reducing sperm count in house mice via acting on the early stages of spermatogenesis, and it does not cross the blood-testis barrier. SR210831C can be used in male contraception research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C29H25NO3
- Peso molecular:435.51
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Actividad biológica
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RXR α 0.051 nM (IC50) |
SR210831C potently and selectively inhibits human RARα with an IC50 of 0.051 nM, showing >1647-fold selectivity over RARβ and >1960-fold selectivity over RARγ in GeneBLAzer reporter cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 (Plasma) | Cmax |
|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 12.0 h | 4992 ng/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD1 mice[1]
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Dosage:10 mg/kg/day; 1 mg/kg/day; 0.3 mg/kg/day; 0.1 mg/kg/day; 0.03 mg/kg/day
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Administration:p.o.; daily; 28 days
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Result:Reduced sperm counts to 2.6 × 106 per sample and testicular weight to 205 mg at 10 mg/kg/day.
Achieved complete inhibition of spermatogenesis 1 day post-treatment at 1 mg/kg/day and 0.3 mg/kg/day.
Showed reduced inhibitory effect on spermatogenesis 1 day post-treatment at 0.1 mg/kg/day.
Detected no inhibitory effect on spermatogenesis 1 day post-treatment at 0.03 mg/kg/day.
Recovered sperm counts to ~40% of control levels at 4 weeks post-treatment and fully recovered by 8 weeks post-treatment at 10 mg/kg/day.
Showed partial sperm count recovery at 4 weeks post-treatment and full recovery by 8 weeks post-treatment, with testicular weight returning to baseline by 4 weeks post-treatment at 1 mg/kg/day.
Chemical Information
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Peso molecular 435.51
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Fòrmula C29H25NO3
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SMILES
CC1=C2O[C@H](C(C3=CC=C(N3)C4=CC=C(C=C4)C(O)=O)=CC2=C(C=C1)C5=CC=C(C)C=C5)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SR210831C Related Classifications
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