Art. -Nr.: HY-182485

U-11634

U-11634 is an orally active dopamine β-hydroxylase noncompetitive inhibitor, with rat LD₅₀ values of 1197 mg/kg (subcutaneous) and 524 mg/kg (oral). U-11634 blocks conversion of dopamine to norepinephrine and reduces norepinephrine levels in brain. U-11634 decreases food intake and spontaneous motor activity via dietary inclusion. U-11634 induces thyroid toxicity and inhibits pregnancy. U-11634 inhibits deciduomata formation in intact and steroid-treated rats, with no reversal by progesterone or oestradiol. U-11634 can be used for pregnancy.

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CAS. Nr.: 3414-47-9
Formel: C₁₁H₁₀F₃NO₂S
Molecular Weight:277.26

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

U-11634 Chemical Structure

CAS. Nr.: 3414-47-9

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
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Verweise
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Biologische Aktivität

Beschreibung

In Vitro

U-11634 (compound 12) (1×10^-4 M) moderately inhibits purified bovine adrenal dopamine β-hydroxylase in vitro, reducing enzyme activity to 52% of control levels via noncompetitive inhibition^[1].

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

Parmacokinetics

Species	Dose	Route	Serum Concentration
Rat^[3]	100 mg/kg	p.o.	10.0 μg/mL
Cynomolgus Monkey^[3]	200 mg/kg	p.o.	10.4 μg/mL

In Vivo

U-11634 (compound 12) (200 mg/kg; i.p.; single dose) reduces rat brain norepinephrine levels to 82% of control at 4 hours and 72% of control at 16 hours following a single 200 mg/kg intraperitoneal dose^[1].
U-11634 (616 mg/kg per 24 h; p.o.; single application for 24 h) reduces spontaneous motor activity in mice to 67% of control when administered^[1].
U-11634 (5-10 mg/day; s.c.; daily; for 20 days) does not alter vaginal cytology, body weight gain, post-treatment mating interval, or litter outcomes in cyclic mature female Sprague-Dawley rats^[2].
U-11634 (5-10 mg/day; s.c.; once daily; days 4, 5, 6 of pseudopregnancy) does not significantly alter the interval from the start of pseudopregnancy to the first post-treatment oestrous-like smear in Sprague-Dawley rats^[2].
U-11634 (25 mg; p.o.; single dose) administered orally to female Sprague-Dawley rats results in rapid absorption, peak serum levels of 13.3 μg/mL (normalized to 100 mg/kg) at 2 hours, and stable serum retention for up to 24 hours^[3].
U-11634 (200 mg/kg; p.o.; single dose) administered orally to male cynomologous monkeys results in slower absorption, with peak serum levels of 33.0 μg/mL and 49.4 μg/mL at 12 hours for the two animals, and slow metabolism/excretion over 24 hours^[3].
U-11634 (0.25-10 mg; s.c.; daily from pro-oestrus to day 6; single dose on day 2, 4, 6, 12, or 16; daily from day 1 to day 3; daily from day 3 to day 6) completely inhibits pregnancy in Sprague-Dawley rats when given during the early pre-implantation period, with no observed foetal toxicity at therapeutic doses^[4].
U-11634 (3-12 mg/rat; dietary; average daily intake from pro-oestrus to Day 6) completely inhibits pregnancy in Sprague-Dawley rats when given during the early pre-implantation period, with no observed foetal toxicity at therapeutic doses^[4].
U-11634 (1.0-5.0 mg/rat; p.o.; daily from pro-oestrus for 7 or 13 days) completely inhibits pregnancy in Sprague-Dawley rats when given during the early pre-implantation period, with no observed foetal toxicity at therapeutic doses^[4].
U-11634 (1.0-5.0 mg; s.c.; daily for 8 days) inhibits pregnancy in Swiss-Webster mice^[4].
U-11634 (0.25 mg/mouse; p.o.; daily for 8 days) inhibits pregnancy significantly in Swiss-Webster mice^[4].
U-11634 (0.05-6.4 mg/rat; s.c.; daily for 10 days) does not exhibit gonadotrophic-inhibiting activity in immature male Sprague-Dawley rats at anti-fertility doses, with only mild effects on reproductive tissues observed at four times the therapeutic dose^[4].
U-11634 (0.05-2.0 mg; p.o.; daily for 10 days) does not exhibit uterotrophic or anti-oestrogenic activity in immature bilaterally ovariectomized Sprague-Dawley rats at oral doses up to 2.0 mg/rat daily^[4].
U-11634 (0.5-8.0 mg/rat; p.o.; daily for 10 days) does not exhibit androgenic activity in immature castrated male Sprague-Dawley rats at oral doses up to 8.0 mg/rat daily^[4].
U-11634 (10 mg/rat; p.o.; daily from Day 5 to Day 8) inhibits deciduomata formation in both intact and hormone-treated ovariectomized pseudopregnant Sprague-Dawley rats, supporting interference with uterine decidualization as a mechanism of pregnancy inhibition^[4].
U-11634 (12.5-50 mg/kg; p.o.; daily from day 9 to day 15 of pregnancy) does not cause significant foetal toxicity, death, or developmental abnormalities in pregnant Sprague-Dawley rats at oral doses up to 50 mg/kg daily during mid-pregnancy^[4].

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

Animal Model:

Sprague-Dawley (male, 140-200 g)^[1]
Dosage:

200 mg/kg
Administration:

i.p.; single dose
Result:

Remained at 100% of control values at 2 hours post-dose.
Reduced to 82% of control values at 4 hours post-dose.
Reduced to 72% of control values at 16 hours post-dose.

Animal Model:

CF-1 (male)^[1]
Dosage:

616 mg/kg
Administration:

p.o.; single application for 24 h
Result:

Reduced spontaneous motor activity to 67% of control values.

Animal Model:

Sprague-Dawley (mature female, cyclic)^[2]
Dosage:

5 mg/day; 10 mg/day
Administration:

s.c.; daily; 20 days
Result:

Showed no effect on vaginal cytology relative to vehicle controls.
Did not significantly differ from controls in body-weight gain (5 mg/day group: +25 g; 10 mg/day group: +23 g), days from end of treatment to mating (5 mg/day group: 2.0 days; 10 mg/day group: 3.6 days), litter size (5 mg/day group: 11.6 foetuses; 10 mg/day group: 11.2 foetuses), average foetal weight (5 mg/day group: 2.9 g; 10 mg/day group: 2.6 g), and foetal gross condition.

Animal Model:

Sprague-Dawley (lactating, litters reduced to 8 pups)^[2]
Dosage:

10 mg/day
Administration:

s.c.; once daily; days 5, 6, 7 of lactation
Result:

Showed no effect on pup weight (pups gained an average of 1.5 g body weight daily) or pup survival (no pup deaths) relative to controls.
Showed no effect on vaginal cytology timing (cornified oestrous smears observed on day 18 or 19, matching control timing) relative to controls.

Animal Model:

Sprague-Dawley (female, 219-231 g)^[3]
Dosage:

100 mg/kg
Administration:

p.o.; single dose
Result:

Reached normalized serum level of 10.0 μg/mL at 1 hour.
Reached normalized serum level of 13.3 μg/mL at 2 hours.
Reached normalized serum level of 14.2 μg/mL at 4 hours.
Reached normalized serum level of 12.8 μg/mL at 6 hours.
Reached normalized serum level of 14.4 μg/mL at 8 hours.
Reached normalized serum level of 15.8 μg/mL at 12 hours.
Reached normalized serum level of 10.0 μg/mL at 18 hours.
Reached normalized serum level of 15.3 μg/mL at 24 hours.
Observed peak levels 1-2 hours post-administration.
Maintained relatively stable serum levels from 2-24 hours.

Animal Model:

Two Macaca irus (male, weighing 4 kg and 5 kg, respectively)^[3]
Dosage:

200 mg/kg
Administration:

p.o.; single dose
Result:

Reached serum level of 10.4 μg/mL at 2 hours in monkey No. 635.
Reached serum level of 20.0 μg/mL at 4 hours in monkey No. 635.
Reached serum level of 29.2 μg/mL at 6 hours in monkey No. 635.
Reached serum level of 32.6 μg/mL at 8 hours in monkey No. 635.
Reached serum level of 33.0 μg/mL at 12 hours in monkey No. 635.
Reached serum level of 14.7 μg/mL at 24 hours in monkey No. 635.
Reached serum level of 12.7 μg/mL at 2 hours in monkey No. 636.
Reached serum level of 24.6 μg/mL at 4 hours in monkey No. 636.
Reached serum level of 32.7 μg/mL at 6 hours in monkey No. 636.
Reached serum level of 42.4 μg/mL at 8 hours in monkey No. 636.
Reached serum level of 49.4 μg/mL at 12 hours in monkey No. 636.
Reached serum level of 50.4 μg/mL at 24 hours in monkey No. 636.
Observed peak levels at 12 hours or later post-administration.

Animal Model:

Sprague-Dawley (mature nulliparous, 200 to 250 g body weight, pregnancy model via mating with fertile males)^[4]
Dosage:

0.25 mg/rat; 1 mg/rat; 2.5 mg/rat; 5 mg/rat; 10 mg/rat
Administration:

s.c.; daily from pro-oestrus to Day 6
Result:

Completely inhibited pregnancy (0 decidual sites per rat) at subcutaneous doses of 2.5, 5.0, and 10 mg/rat daily from pro-oestrus to Day 6.

Animal Model:

Mice (25-28 g body weight, pregnancy model)^[4]
Dosage:

1.0 mg/mouse; 2.5 mg/,ouse; 5.0 mg/mouse
Administration:

s.c.; daily from Day 1 to Day 8
Result:

Inhibited pregnancy at subcutaneous doses of 1.0, 2.5, and 5.0 mg/mouse daily from Day 1 to Day 8, with only 1/5 mice showing reduced, non-progressing decidual sites at the 1.0 and 5.0 mg/mouse doses.

Animal Model:

Mice (25-28 g body weight, pregnancy model)
^[4]
Dosage:

0.05 mg/mouse; 0.10 mg/mouse; 0.25 mg/mouse; 1 mg/mouse; 5.0 mg/mouse
Administration:

p.o.; daily from Day 1 to Day 8
Result:

Significantly inhibited pregnancy at the minimal effective oral dose of 0.25 mg/mouse daily; complete pregnancy inhibition was not achieved with any tested oral dose.

Animal Model:

Sprague-Dawley (immature male, 26 to 28 days of age)^[4]
Dosage:

0.05 mg/rat; 0.8 mg/rat; 1.6 mg/rat; 3.2 mg/rat; 6.4 mg/rat
Administration:

s.c.; daily for 10 days
Result:

Observed no significant changes in testes, seminal vesicle, or levator ani weights, or body weight gain at 1.6 mg/rat (equivalent to minimal 100% effective anti-fertility dose) compared to controls.
Observed slight reductions in testes (1.10 g vs. 1.34 g control), seminal vesicle (12 mg vs. 17 mg control), and levator ani (25 mg vs. 33 mg control) weights, plus reduced body weight gain (42 g vs. 50 g control) at 6.4 mg/rat (four times the anti-fertility dose).

Animal Model:

Sprague-Dawley (immature bilaterally ovariectomized, ~70 g body weight)^[4]
Dosage:

0.05 mg/rat; 0.20 mg/rat; 0.40 mg/rat; 1.0 mg/rat; 2.0 mg/rat
Administration:

p.o.; daily for 10 days
Result:

Did not increase uterine weight compared to vehicle controls (average uterine weight 25.2 mg, not significantly different from controls) at any tested oral dose.
Did not significantly reduce the uterine weight increase induced by concomitant oestradiol administration (122 mg in oestradiol-only group, no significant difference with U-11634 co-administration) at any tested dose.

Animal Model:

Sprague-Dawley (immature castrated male, ~100 g body weight)^[4]
Dosage:

0.5 mg/rat; 8.0 mg/rat
Administration:

p.o.; daily for 10 days
Result:

Did not significantly increase seminal vesicle (control 6.0 mg) or prostate (control 32.2 mg) weights compared to vehicle controls at any tested oral dose.

Animal Model:

Sprague-Dawley (pregnant females)^[4]
Dosage:

12.5 mg/kg; 25 mg/kg; 50 mg/kg
Administration:

p.o.; daily from Day 9 to Day 15 of pregnancy
Result:

No significant differences between treated and control groups in average number of foetuses per litter, average foetal weight, crown-rump distance, number of implantation sites, or number of resorption sites.
No foetal deaths, and only one isolated foetal abnormality (no tail) in the 50 mg/kg group.

Chemical Information

CAS. Nr. 3414-47-9
Molecular Weight 277.26
Formel C₁₁H₁₀F₃NO₂S
SMILES

FC(F)(C1=CC(OCC2OC(NC2)=S)=CC=C1)F
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Johnson GA, et al. Inhibition of dopamine -hydroxylase by 5-phenoxymethyl-2-oxazolidinethiones. J Med Chem. 1972 Mar;15(3):327-9. [Content Brief]

[2]. Duncan GW, et L. The effect of U-11634 on the vaginal cytology of rats. J Reprod Fertil. 1966 Jun;11(3):459-61. [Content Brief]

[3]. Forist AA, et al. Comparative serum levels of an antifertility oxazolidinethione (U-11634) in rats and monkeys. J Reprod Fertil. 1968 Jul;16(2):317-8. [Content Brief]

[4]. Duncan GW, et al. The inhibition of pregnancy with an oxazolidinethione (U-11634). J. Reprod. Fertil. 1966 Feb; 11(1):85–95

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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