Etoprine
Etoprine is a potent orally active dihydrofolate reductase (DHFR) inhibitor. Etoprine competitively inhibits testicular DHFR to disrupt tetrahydrofolate and DNA synthesis in rapidly dividing cells. Etoprine acts as an antifertility agent in male mice and reduces fecundity in male rats.
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- No. CAS: 18588-57-3
- Fòrmula: C12H12Cl2N4
- Peso molecular:283.16
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
In Vitro
Etoprine (6 h) potently inhibits growth of E. coli BL21(DE3)pLysS expressing wild-type PvDHFR-TS with an IC50 of 0.07 μM[2].
Etoprine (6 h) moderately inhibits growth of E. coli BL21(DE3)pLysS expressing SP21 mutant PvDHFR-TS with an IC50 of 10.45 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Etoprine (5 mg/kg/day; p.o.; daily; 65 days) reduces male rat fecundity via spermatogenesis inhibition[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male mice (65 days old)[1]
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Dosage:0.1; 0.5; 1; 5; 10; 25; 50 mg/kg
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Administration:p.o.; daily; 55 days
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Result:Reduced percent fertile males and percent pregnant females significantly at doses ≥5 mg/kg/day, with complete infertility observed.
Reduced epididymal sperm reserves significantly.
Rendered sperm motility unassessable.
Reduced seminiferous tubule diameter significantly.
Reduced testicular and epididymal weights significantly.
Maintained normal serum testosterone levels at all doses.
Reduced body weights significantly, with no dose-dependency observed.
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Animal Model:Rats (65 days old)[1]
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Dosage:5 mg/kg
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Administration:p.o.; daily; 65 days
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Result:Reduced percentage of pregnant female rats significantly, while all treated male rats remained fertile.
Reduced embryo number, size, and embryo score significantly.
Reduced testis weight, epididymis weigh, testis weight per 100g body weight, and epididymis weight per 100g body weight significantly.
Reduced epididymal sperm reserves significantly, with an estimated ED50 of 2.9 mg/kg/day for 50% reduction of sperm reserves.
Reduced seminiferous tubule diameter significantly, with no sperm sample obtainable for motility assessment.
Maintained body weight and serum testosterone levels not significantly different from controls.
Chemical Information
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No. CAS 18588-57-3
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Peso molecular 283.16
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Fòrmula C12H12Cl2N4
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SMILES
ClC1=CC=C(C=C1Cl)C=2C(=NC(=NC2CC)N)N
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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
[1]. Malik NS, et al. The contraceptive effects of etoprine on male mice and rats. J Androl. 1995;16(2):169-174. [Content Brief]
[2]. Bunyarataphan S, et al. Evaluation of the activities of pyrimethamine analogs against Plasmodium vivax and Plasmodium falciparum dihydrofolate reductase-thymidylate synthase using in vitro enzyme inhibition and bacterial complementation assays. Antimicrob Agents Chemother. 2006;50(11):3631-3637. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Etoprine Related Classifications
HY-105714 Related Classifications
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