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17 alpha-propionate

Cat. No. M5035
17 alpha-propionate Structure
Synonym:

CB-03-01

Size Price Availability Quantity
5mg USD 90 In stock
10mg USD 120 In stock
50mg USD 400 In stock
100mg USD 660 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 402.52
Formula C24H34O5
CAS Number 19608-29-8
Purity >99%
Solubility 10 mM in DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
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
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: 17 alpha-propionate, CB-03-01 supplier, Androgen Receptor, inhibitors

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