2. Metabolic Enzyme/Protease
  3. Dihydrofolate reductase (DHFR)
  4. 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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Etoprine

Etoprine Chemical Structure

CAS No. : 18588-57-3

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Etoprine Related Antibodies

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Description

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[1][2].

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.

Etoprine Related Antibodies
In Vivo

Etoprine (0.1-50 mg/kg; p.o.; daily; 55 days) acts as a potent male antifertility agent in mice[1].
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.

Animal Model: Male mice (65 days old)[1]
Dosage: 0.1; 0.5; 1; 5; 10; 25; 50 mg/kg
Administration: p.o.; daily; 55 days
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.
Animal Model: Rats (65 days old)[1]
Dosage: 5 mg/kg
Administration: p.o.; daily; 65 days
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.
Molecular Weight

283.16

Formula

C12H12Cl2N4
CAS No.
SMILES

ClC1=CC=C(C=C1Cl)C=2C(=NC(=NC2CC)N)N
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Purity & Documentation
References
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Etoprine Related Classifications

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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.

Keywords:

Etoprine18588-57-3Dihydrofolate reductase (DHFR)DNA synthesisdihydrofolate reductasetetrahydrofolatevivax malariawild-type Plasmodium vivax DHFR-TSseminiferous tubulespermatogenic arrestmale miceSP21 mutant PvDHFR-TSmale ratsInhibitorinhibitorinhibit

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