Everything about Cortexolone 17α-propionate powder
|1.What cause Hair Loss?|
|2.How to treatment Hair Loss?|
|3.What is Cortexolone 17α-propionate?|
|4.what is the difference between RU58841 and CB-03-01?|
|5.Where To Buy Cortexolone 17α-propionate powder?|
|6.17α-propionate powder supplier|
Cortexolone 17α-propionate powder basic Characters:
|Name:||Cortexolone 17α-propionate powder|
|Storage Temp:||Room Temperature|
|Color:||White to off-white powder powder|
Male-pattern baldness, more properly called androgenic alopecia, affects a significant proportion of the male population and quite a few women. In this condition, inherited genetic factors cause the hair follicles on the head to be abnormally sensitive to the presence of a hormone called dihydrotestosterone (DHT). An enzyme called 5-alpha-reductase turns testosterone into DHT. The DHT then binds to androgen receptors in the hair follicles. In susceptible hair follicles, prolonged exposure to DHT causes the hair follicle to spend more time resting rather than growing hair, and over time, the follicle undergoes a gradual miniaturization process, eventually producing only tiny fine hair called vellum.
Many researchers have identified the androgen receptors as good targets for treating androgenic alopecia. If the androgen receptors in the hair follicles can be blocked or disabled, then DHT cannot affect the hair follicles. However, systemic administration of androgen receptor blockers, such as the drugs used to treat prostate cancer, cause a lot of serious side effects. Since baldness affects the skin, which is readily accessible, topical application of an effective androgen receptor blocker should stop the balding process without causing any systemic side-effects. Researchers have already identified molecules that function in exactly this way.
There is no doubt that antiandrogens are among the most effective treatments for male balding (androgenetic alopecia, AGA) in the present year. Antiandrogens like finasteride and dutasteride stop hair loss in a high proportion of users and even improve density in a good proportion as well. However they don’t help everyone and side effects (sexual dysfunction, depression, etc) limit their wide spread use. Safer anti androgens, if they worked well, would be a great addition to the treatments we currently use.
We’ve seen an increasing interest in topical anti androgens in recent years, including agents such as topical finasteride, topical Fluridil, topical RU 54481 and others.
To date there is no topical anti androgen approved by the FDA for use in male AGA. In theory a good topical anti androgen should have potent activity that is confined to the skin, have no systemic side effects and have good tolerability.
Cortexolone 17α-propionate (developmental code name CB-03-01; tentative brand names Breezula powder(for acne), Winlevi powder(for androgenic alopecia)), or 11-deoxycortisol 17α-propionate, is a synthetic steroidal antiandrogen – specifically, an androgen receptor antagonist – that is under development by Cassiopea and Intrepid Therapeutics for use as a topical medication in the treatment of androgen-dependent conditions including acne vulgaris and androgenic alopecia (male-pattern hair loss). It is the C17α propionate ester of 11-deoxycortisol (cortexolone); C17α esters of 11-deoxycortisol were unexpectedly found to possess antiandrogen activity, and cortexolone 17α-propionate CAS 19608-29-8 was selected for development based on its optimum drug profile.
In rats, the drug has been found to possess strong local antiandrogen activity, but negligible systemic antiandrogen activity when administered via subcutaneous injection. In addition, cortexolone 17α-propionate is not progonadotropic, suggesting that it is peripherally selective.In a bioassay, the topical potency of the drug was greater than that of progesterone, flutamide, and finasteride and was equivalent to that of cyproterone acetate.
A pilot clinical trial in 2011 of men treated with topical cortexolone 17α-propionate 1% cream for acne found that the drug was very well-tolerated and significantly reduced symptoms of acne. Moreover, its effectiveness was significantly greater than that of the active comparator, tretinoin 0.05% cream. As of 2017, the drug is in phase III clinical trials for acne vulgaris and phase II clinical trials for androgenic alopecia.
CB-03-01 is a topical anti-androgen compound patented by Cosmo and investigated under the name Breezula. It is an androgen receptor antagonist rather than an inhibitor of 5 alpha reductase. It has good penetration through the skin. Studies are underway to determine if the drug has benefit in male pattern balding or not. In fact, a 26 week study by Intreprid is now underway to compare 5 % CB-03-01 to 5 % minoxidil and placebo. It will be interesting to see if CB-03-01 has any benefit and if so, how it compares to topical minoxidil.
To date, there are only two published studies in the medical literature about CB-03-01. So we have limited information on the drug. It appears that CB-03-01 is rapidly metabolized to cortexolone which does not have any anti androgen activity. Second, it appears that CB-03-01 has an anti-inflammatory effect which could be important in treating AGA which is known to be associated with inflammation in many cases. Studies in rats and rabbits showed that it is not mutagenic. Studies in humans have not shown any significant adverse events.
RU58841 is an androgen receptor blocker that was first discovered in the early 1990s, and it has been extensively studied in animal models. When applied topically, it is highly effective in stopping the progression of balding and can even stimulate some hair re-growth. No systemic side effects have been found in monkeys treated topically with RU58841. However, due to issues unrelated to RU58841 itself, it has never gone through the formal human testing processes to allow it to be approved by the FDA and other regulatory agencies for marketing as a balding treatment. It is available for purchase as a research chemical, and many individuals have been using it to treat balding over the last few decades. It is reported to be very effective in stopping hair loss with minimal side effects. A few individuals report that it stimulates hair re-growth as well.
- Cortexolone 17 Alpha-Propionate, or “CB-03-01″
CB-03-01 is an androgen receptor blocker first discovered in the 2000s. Initial studies in animal models found it could block androgen receptors when applied topically but not when given systemically. Its lack of activity when applied systemically means it exhibited no systemic anti-androgenic side effects in rats injected with the drug. Its ability to block topical androgen activity was described by the early researchers as being about three times more potent than flutamide. The fact that it has no anti-androgenic activity when applied systemically is probably due to the fact that after it enters the body it is almost immediately metabolized into an inactive form.
- Strength Comparison
Early studies of RU588541 also compared its efficacy to other androgen receptor blockers, such as flutamide, nilutamide, and bicalutamide. When taken systemically, RU58841 has strong side effects similar to any oral androgen receptor blocker. In studies of RU58841, it was found to a much more potent blocker of androgen receptors than any previously-known androgen receptor blockers; in fact, the researchers concluded it was the “most potent antiandrogen” known at that time (1998), with up to 100 times the activity of flutamide, suggesting it is a much more potent androgen receptor blocker than CB-03-01.
Although the two agents have never been directly compared, they have both been evaluated in similar tests against reference drugs. Hamsters have a special glands in their skin that develop in response to male hormones. The ability of anti-androgenic drugs to block this gland development is commonly used in the laboratory. In hamster skin gland tests, at a dose of 400 micrograms per day, CP-03-01 was less effective than flutamide (84% vs. 55%, respectively) in blocking development of the organ in response to male hormones but it was slightly more effective than cyproterone acetate (only 93% blockage)
However, at a dose of only 10 micrograms per day, RU58841 was capable of blocking development of the gland by 60%, and it was found to be a much more potent topical androgen receptor blocker than either flutamide or cyproterone acetate. Simple deduction suggests it is also a much more potent agent than CP-03-01.
- Acne Treatment
Unlike RU58841, which appears to have been abandoned by the pharmaceutical industry, CB-03-01 is being actively studied, primarily as a treatment for acne. CB-03-01 is manufactured by Cosmo Pharmaceuticals, an Italian company. The company licensed the drug to Medicis in 2012 for development in the US. Early studies of the drug as a hair loss treatment required a special method of delivering the drug to the hair follicles using an electrical current (iontophoresis), but once delivered, it did seem to be reasonably effective in treating hair loss. However, few patients are going to be willing to be treated several times a week for decades by iontophoresis.
The study evaluated the efficacy of CB-03-01 in 40 men with androgenetic alopecia grade 1-4 according to the Hamilton scale, and in 30 post-menopausal women with androgenetic alopecia grade 1 according to the Ludwig scale.
A presentation by Cosmo in 2013 indicates they may have solved the delivery problem. They have performed skin permeation tests, and have shown that a 5% solution of the drug in a special carrier cream is able to penetrate the hair follicles. They have also performed toxicity and irritation tests in pigs. The 2013 presentation suggested they were about to begin studies in human volunteers. A more recent report from the company indicated that the results of a trial comparing it to minodoxil in 120 human volunteers will be available in late 2015.
Although both RU58841 and CB-03-01 are available for purchase as research chemicals for individual use, it is difficult for a casual purchaser to “try out” CB-03-01 at home. Unlike RU58841, which can be dissolved in alcohol or other readily available carriers, CB-03-01 apparently needs to be prepared in a special carrier cream in order to get it to enter the hair follicles. Therefore, because none of Cosmo’s studies on hair loss have been published as of yet, and no one has been able to “try out” CB-03-01 at home, it is unclear how effective it is relative to RU58841 for treating balding. CB-03-01 appears to have a much shorter half-life than RU58841, and it may be a less potent blocker of androgen receptors. When applied topically, neither product should exhibit any systemic side-effects.
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