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17 alpha-propionate is a new potent topical antiandrogen potentially useful in acne vulgaris. CB-03-01 1% cream was very well tolerated, and was significantly better than placebo regarding TLC (P = 0·0017), ILC (P = 0·0134) and ASI (P = 0·0090), and also clinically more effective than comparator. The product also induced a faster attainment of 50% improvement in all the above parameters.
| Cell Experiment | |
|---|---|
| Cell lines | PBMC |
| Preparation method | Because of the extent of these experiments, the drugs were divided into two groups: dexamethasone, budesonide, beclomethasone dipropionate and fluticasone (first group); and dexamethasone, CsA, FK506 (tacrolimus) and mycophenolate (second group). |
| Concentrations | 10^-2 mol/L |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Female Golden hamsters |
| Formulation | 0.05 mL of acetone containing 4 μg of testosterone propionate (TP) |
| Dosages | 100−200−400 μg/animal |
| Administration | s.c. |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
| Molecular Weight | 402.52 |
| Formula | C24H34O5 |
| CAS Number | 19608-29-8 |
| Purity | >98% |
| Solubility | 10 mM in DMSO |
| Storage | at -20°C |
 |
Source | J Microbiol Biotechnol (2016). Figure 4. 17 alpha-propionate |
| Method | Western Blot | |
| Cell Lines | bacteria | |
| Concentrations | 140 mg/l | |
| Incubation Time | 6 h | |
| Results | As shown in Fig. 4, propionate-oxidizing bacteria relevant band B3 was enhanced with the pH decrease rom 7.1 to 6.0, indicating that this propionate degrader (band B3) is slightly acid tolerant. | |
| Rating |
Biological profile of cortexolone 17alpha-propionate (CB-03-01), a new topical and peripherally selective androgen antagonist.
Celasco G,et.al. Arzneimittelforschung. 2004;881-6. PMID: 15646372.
Biotransformation of the topical glucocorticoids budesonide and beclomethasone 17 alpha,21-dipropionate in human liver and lung homogenate.
Andersson P, et al. J Pharm Pharmacol. 1984 Nov;36(11):763-5. PMID: 6150981.
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