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.
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- 화학식: C29H25NO3
- 분자량:435.51
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보관:
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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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
RXR α 0.051 nM (IC50) |
In Vitro
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. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | T1/2 (Plasma) | Cmax |
|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 12.0 h | 4992 ng/mL |
In Vivo
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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분자량 435.51
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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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.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SR210831C Related Classifications
HY-183986 Related Classifications
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