1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  2. RAR/RXR
  3. 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.

For research use only. We do not sell to patients.

SR210831C

SR210831C Chemical Structure

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Description

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[1].

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.

Parmacokinetics
Species Dose Route T1/2 (Plasma) Cmax
Mice[1] 10 mg/kg p.o. 12.0 h 4992 ng/mL
In Vivo

SR210831C (Compound 23) (0.03-10 mg/kg/day; p.o.; daily; 28 days) produces a reversible, dose-dependent inhibition of spermatogenesis in CD1 mice, with a minimum effective dose between 0.3 and 1 mg/kg/day for full contraceptive effect[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD1 mice[1]
Dosage: 10 mg/kg/day; 1 mg/kg/day; 0.3 mg/kg/day; 0.1 mg/kg/day; 0.03 mg/kg/day
Administration: p.o.; daily; 28 days
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.
Molecular Weight

435.51

Formula

C29H25NO3

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
SR210831C
Cat. No.:
HY-183986
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