| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
U-11634 (compound 12) (1×10-4 M) showed moderate inhibition of purified bovine adrenal dopamine β-hydroxylase in vitro, reducing enzyme activity to 52% of the control level through non-competitive inhibition [1].
|
|---|---|
| ln Vivo |
U-11634 (compound 12) (200 mg/kg; intraperitoneal injection; single dose) reduced norepinephrine levels in the rat brain to 82% of the control group 4 hours after a single intraperitoneal injection of 200 mg/kg and to 72% of the control group 16 hours after a single injection [1]. U-11634 (616 mg/kg/24 h; oral; single dose, lasting 24 hours) reduced spontaneous kinetic activity in mice to 67% of the control group [1]. U-11634 (5–10 mg/day; subcutaneous injection; once daily; lasting 20 days) did not alter vaginal cytology, weight gain, mating interval after treatment, or birth outcomes in periodically mature female Sprague-Dawley rats [2]. U-11634 (5-10 mg/day; subcutaneous injection; once daily; administered on days 4, 5, and 6 of pseudopregnancy) did not significantly alter the time interval from the onset of pseudopregnancy to the appearance of estrus-like smears after the first treatment in Sprague-Dawley rats [2]. Oral administration of U-11634 (25 mg; orally; single dose) to female Sprague-Dawley rats resulted in rapid absorption, with a peak serum concentration of 13.3 μg/mL (based on 100 mg/kg) after 2 hours and a stable serum concentration that remained for up to 24 hours [3]. Oral administration of U-11634 (200 mg/kg; orally; single dose) to male cynomolgus monkeys resulted in slower absorption, with peak serum concentrations of 33.0 μg/mL and 49.4 μg/mL in the two animals after 12 hours, respectively, and slow metabolism/excretion over 24 hours [3]. U-11634 (0.25–10 mg; subcutaneous injection; once daily from proestrus to day 6; single dose on days 2, 4, 6, 12, or 16; once daily from day 1 to day 3; once daily from day 3 to day 6) completely suppressed pregnancy in Sprague-Dawley rats before implantation and no fetal toxicity was observed at therapeutic doses[4]. U-11634 (3–12 mg/rat; feed; mean daily intake from proestrus to day 6) completely suppressed pregnancy in Sprague-Dawley rats before implantation and no fetal toxicity was observed at therapeutic doses[4]. U-11634 (1.0–5.0 mg/rat; oral administration; once daily for 7 or 13 days from proestrus) completely suppressed pregnancy in Sprague-Dawley rats before early implantation and no fetal toxicity was observed at therapeutic doses[4]. U-11634 (1.0–5.0 mg; subcutaneous injection; once daily for 8 days) inhibited pregnancy in Swiss-Webster mice[4]. U-11634 (0.25 mg/mouse; oral administration; once daily for 8 days) significantly inhibited pregnancy in Swiss-Webster mice[4]. U-11634 (0.05–6.4 mg/rat; subcutaneous injection; once daily for 10 days) did not show gonadotropin-suppressing activity in immature male Sprague-Dawley rats at antifertility doses, with only slight effects on reproductive tissues observed at four times the therapeutic dose[4]. U-11634 (0.05–2.0 mg; oral administration; once daily for 10 days) did not show uterine growth-promoting or anti-estrogenic activity in bilaterally ovariectomized immature Sprague-Dawley rats at oral doses up to 2.0 mg/rat per day[4]. U-11634 (0.5–8.0 mg/rat; orally; once daily for 10 days) did not exhibit androgenic activity in castrated immature male Sprague-Dawley rats at daily oral doses up to 8.0 mg/rat [4]. U-11634 (10 mg/rat; orally; once daily from day 5 to day 8) inhibited decidual tumor formation in fully ovariectomized and hormone-treated pseudopregnant Sprague-Dawley rats, suggesting that interference with uterine decidualization is its mechanism of pregnancy suppression [4]. U-11634 (12.5–50 mg/kg; orally; once daily from day 9 to day 15 of gestation) at daily oral doses up to 50 mg/kg during mid-gestation did not cause significant fetal toxicity, death, or developmental abnormalities in pregnant Sprague-Dawley rats [4].
|
| Animal Protocol |
Animal/Disease Models:Sprague-Dawley mice (male, 140-200 g) [1]
Doses: 200 mg/kg Route of Administration: Intraperitoneal injection; single dose Experimental Results: 2 hours after administration, the mice remained at 100% of the control group. 4 hours after administration, the mice decreased to 82% of the control group. 16 hours after administration, the mice decreased to 72% of the control group. Animal/Disease Models:CF-1 (male) [1] Doses: 616 mg/kg Route of Administration: Oral; single dose 24 hours later Experimental Results: Spontaneous kinetic activity decreased to 67% of the control. Animal/Disease Models:Sprague-Dawley (mature female, cyclical) [2] Doses: 5 mg/day; 10 mg/day Route of Administration: Subcutaneous injection; daily; 20 days Experimental Results: No effect on vaginal cytology compared to the vector control group. There were no significant differences among the groups in terms of weight gain (5 mg/day group: +25 g; 10 mg/day group: +23 g), number of days from the end of treatment to mating (5 mg/day group: 2.0 days; 10 mg/day group: 3.6 days), number of litters (5 mg/day group: 11.6 fetuses; 10 mg/day group: 11.2 fetuses), mean fetal weight (5 mg/day group: 2.9 g; 10 mg/day group: 2.6 g), and overall fetal condition. Animal/Disease Models:Sprague-Dawley mice (lactating period, litter size reduced to 8)[2] Doses: 10 mg/day Route of Administration: Subcutaneous injection; once daily; days 5, 6, and 7 of lactation Experimental Results: Compared with the control group, there was no effect on pup weight (average daily weight gain of 1.5 g) or pup survival rate (no pup mortality). Compared with the control group, there was also no effect on the timing of vaginal cytology examination (observation of keratotic estrus smears on day 18 or 19, consistent with the control group). Animal/Disease Models:Sprague-Dawley mice (female, 219-231 g)[3] Doses: 100 mg/kg Route of Administration: Oral; Single dose Experimental Results: Serum concentration reached 10.0 μg/mL at 1 hour. Serum concentration reached 13.3 μg/mL at 2 hours. Serum concentration reached 14.2 μg/mL at 4 hours. Serum concentration reached 12.8 μg/mL at 6 hours. Serum concentration reached 14.4 μg/mL at 8 hours. Serum concentration reached 15.8 μg/mL at 12 hours. Serum concentration returned to normal at 10.0 μg/mL 18 hours after administration. Serum concentration returned to normal at 15.3 μg/mL 24 hours after administration. Peak concentration was reached 1-2 hours after administration. Serum concentrations remained relatively stable over 2-24 hours. Animal/Disease Models:Two male macaques (weighing 4 kg and 5 kg respectively)[3] Doses: 200 mg/kg Route of Administration: Oral; Single dose Experimental Results: Serum concentration of monkey No. 635 reached 10.4 μg/mL 2 hours after administration. Serum concentration of monkey No. 635 reached 20.0 μg/mL 4 hours after administration. Serum concentration of monkey No. 635 reached 29.2 μg/mL 6 hours after administration. Serum concentration of monkey No. 635 reached 32.6 μg/mL 8 hours after administration. Serum concentration of monkey No. 635 reached 33.0 μg/mL 12 hours after administration. Serum concentration of monkey No. 635 reached 14.7 μg/mL 24 hours after administration. Serum concentration of monkey No. 636 reached 12.7 μg/mL 2 hours after administration. Serum concentration of monkey No. 636 reached 24.6 μg/mL 4 hours after administration. In monkey 636, the serum concentration was 32.7 μg/mL at 6 hours after administration. The serum concentration reached 42.4 μg/mL at 8 hours, 49.4 μg/mL at 12 hours, and 50.4 μg/mL at 24 hours. Peak concentrations were observed at or after 12 hours post-administration. Animal/Disease Models:Sprague-Dawley (mature nulliparous female rats, weighing 200 to 250 g, pregnancy model established by mating with fertile males) [4] Doses: 0.25 mg/rat; 1 mg/rat; 2.5 mg/rat; 5 mg/rat; 10 mg/rat Route of Administration: Subcutaneous injection; once daily from proestrus to day 6 Experimental Results: Subcutaneous injection of 2.5, 5.0 and 10 mg/rat daily from proestrus to day 6 completely suppressed pregnancy (0 decidual sites per rat). Animal/Disease Models:Mice (weight 25-28 g, pregnancy model) [4] Doses: 1.0 mg/mouse; 2.5 mg/mouse; 5.0 mg/mouse Route of Administration: Subcutaneous injection; once daily from day 1 to day 8 Experimental Results: From day 1 to day 8, subcutaneous injection of 1.0, 2.5 and 5.0 mg/mouse once daily suppressed pregnancy. At doses of 1.0 and 5.0 mg/mouse, only 1/5 of the mice showed a reduction in decidual area and no progression. Animal/Disease Models:Mice (weight 25-28 g, pregnancy model) [4] Doses: 0.05 mg/mouse; 0.10 mg/mouse; 0.25 mg/mouse; 1 mg/mouse; 5.0 mg/mouse Route of Administration: Oral; once daily from day 1 to day 8 Experimental Results: The lowest effective dose of 0.25 mg/mouse orally per day significantly inhibited pregnancy; however, all tested oral doses failed to completely inhibit pregnancy. Animal/Disease Models:Sprague-Dawley (immature males, 26 to 28 days old) [4] Doses: 0.05 mg/rat; 0.8 mg/rat; 1.6 mg/rat; 3.2 mg/rat; 6.4 mg/rat Route of Administration: Subcutaneous injection; once daily for 10 days Experimental Results: Compared with the control group, no significant changes were observed in testicular, seminal vesicle or levator ani muscle weight or body weight in rats receiving 1.6 mg/rat (equivalent to the minimum effective dose for 100% infertility control). Slight reductions in testicular weight (1.10 g vs. 1.34 g control group), seminal vesicle weight (12 mg vs. 17 mg control group), and levator ani muscle weight (25 mg vs. 33 mg control group) were observed, and weight gain was reduced at 6.4 mg/rat (four times the antifertility dose) (42 g vs. 50 g control group). Animal/Disease Models:Sprague-Dawley rats (immature bilateral ovariectomy, weighing approximately 70 g) [4] Doses: 0.05 mg/rat; 0.20 mg/rat; 0.40 mg/rat; 1.0 mg/rat; 2.0 mg/rat Route of Administration: Oral; once daily for 10 days Experimental Results: At all tested oral doses, there was no increase in uterine weight compared to the solvent control group (mean uterine weight 25.2 mg, not significantly different from the control group). At all tested doses, there was no significant decrease in the increase in uterine weight compared to concurrent estradiol administration (estradiol-only group 122 mg, not significantly different from the U-11634 combined administration group). Animal/Disease Models:Sprague-Dawley (immature castrated male, weighing approximately 100 g) [4] Doses: 0.5 mg/rat; 8.0 mg/rat Route of Administration: Oral; once daily for 10 days Experimental Results: At any of the tested oral doses, there was no significant increase in the weight of the seminal vesicles (control group 6.0 mg) or prostate (control group 32.2 mg) compared to the solvent control group. Animal/Disease Models:Sprague-Dawley mice (pregnant females) [4] Doses: 12.5 mg/kg; 25 mg/kg; 50 mg/kg Route of Administration: Oral; once daily from day 9 to day 15 of gestation Experimental Results: There were no significant differences between the treatment and control groups in terms of average number of fetuses per litter, average fetal weight, crown-rump length, number of implantation sites, or number of resorption sites. No fetal deaths occurred, and only one isolated fetal malformation (taillessness) was observed in the 50 mg/kg group. |
| References |
|
| Molecular Formula |
C11H10F3NO2S
|
|---|---|
| Molecular Weight |
277.26
|
| CAS # |
3414-47-9
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
FC(F)(C1=CC(OCC2OC(NC2)=S)=CC=C1)F
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6067 mL | 18.0336 mL | 36.0672 mL | |
| 5 mM | 0.7213 mL | 3.6067 mL | 7.2134 mL | |
| 10 mM | 0.3607 mL | 1.8034 mL | 3.6067 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
