Hair Loss Benefit Setipiprant RU58841

Best Minoxidil / RU58841 CAS 38304-91-5 / Setipiprant for Hair Loss Treatment Chemical raw material peptide Quick Details Product name: RU58841 / Minoxidil Powder Other name: 6-(1-Piperidinyl)-2,4-pyrimidinediamine-3-oxide CAS: 38304-91-5 Molecular Formula:C9H15N5O CAS No.:154992-24-2...
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Product Details

Best Minoxidil / RU58841 CAS 38304-91-5 / Setipiprant for Hair Loss Treatment Chemical raw material peptide


Quick Details:

Product name: RU58841 / Minoxidil Powder/ Setipiprant

Other name: 6-(1-Piperidinyl)-2,4-pyrimidinediamine-3-oxide 

CAS: 38304-91-5 

Molecular Formula:C9H15N5O 

CAS No.:154992-24-2

MF:C17H18F3N3O3

Other name: 6-(1-Piperidinyl)-2,4-pyrimidinediamine-3-oxide 

Place of Origin:Shenzhen, China (Mainland)

Grade Standard:Medical Grade

Usage: Hair Loss Setipiprant, Anti Androgens

Brand Name: SENDI

Purity:99%MIN

Shelf life:2 Years Proper Storage

Application:Pharmaceutical Raw Intermediates

Appearance:White Powder

Molecular structure:

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What is RU58841?

RU58841 is an androgen receptor blocker. It binds to androgen receptors with great specificity and tenacity, but does not activate the receptor. Its presence on the receptor prevents androgens such as DHT from binding to and activating the receptor. It has been extensively studied as a topical agent to treat acne and androgenetic alopecia (1, 2, 3).


Androgenetic alopecia, or male-pattern balding, is caused by DHT binding to androgen receptors in the hair follicles. Over time, in susceptible individuals, the activation of the androgen receptors causes the hair follicles to stop producing normal hair and to undergo a process called miniaturization. In laboratory studies, RU58841 has been shown to be quite effective in competing against DHT for access to the androgen receptors.


RU-58841 is an androgen receptor (AR) inhibitor capable of blocking 70% of DHT binding. When compared with the antiandrogenic compound cyproterone acetate, RU-58841 exhibited a 20% increase in AR binding. This compound binds to both the ligand and regulatory domains of the androgen receptor. RU-58841 exerts allosteric binding effects. 


What is Setipiprant?

Setipiprant (INN) (developmental code names ACT-129,968, KYTH-105) is a drug originally developed by Actelion which acts as a selective, orally available antagonist of the prostaglandin D2 receptor 2 (DP2).

It was initially researched as a treatment for allergies and inflammatory disorders, particularly asthma, but despite being well tolerated in clinical trials and showing reasonable efficacy against allergen-induced airway responses in asthmatic patients.


RU58841 / Minoxidil Powder/ Setipiprant Functions:

Minoxidil was the first drug approved by the FDA for the treatment of androgenetic alopecia (hair loss). Before that, minoxidil had been used as vasodilator drug prescribed as oral tablet to treat high blood pressure, with side effects that included hair growth and reversal of male baldness. In the 1980s, UpJohn Corporation came out with a topical solution of 2% minoxidil, called Rogaine, for the specific treatment of androgenetic alopecia. Since the 1990s, numerous generic forms of minoxidil have become available to treat hair loss while the oral form is still used to treat high blood pressure.


Minoxidil is a vasodilator medication known for its ability to slow or stop hair loss and promote hair regrowth. It is available over the counter for treatment of androgenic alopecia, among other baldness treatments, but measurable changes disappear within months after discontinuation of treatment. Its effectiveness has largely been demonstrated in younger men (18 to 41 years of age), the younger the better, and in those with balding in the central (vertex) portion of the scalp.


Minoxidil is a potassium channel agonist. It contains the chemical structure of nitric oxide), a blood vessel dilator, and may be a nitric oxide agonist. This appears to explain its vasodilatory effects, but may also be linked to minoxidil’s ability to stimulate hair growth and treat hair loss. Since minoxidil is a nitric oxide-related compound, it was suspected to act via activation of guanylate cyclase, an enzyme involved in vasodilation.


RU58841 / Minoxidil Powder/ Setipiprant Application:

1. Minoxidil needs to be applied once or twice daily for hair to be maintained. 

2. For maximum effect, the solution should be in contact with the scalp for hours before being washed out. It does not seem capable of reducing DHT or the enzyme responsible for its accumulation around the hair follicle, 5-aliha reductase, which are the main causes of male pattern baldness in genetically susceptible individuals. Therefore, when treatment is stopped, the DHT already accumlated around the follicle has its expected effect, and the follicle usually shrinks again and eventually dies. 

3.Minoxidil powder can promote hair regrowth,slow or stop hair loss and treat high blood pressure.


RU58841 / Minoxidil Powder/ Setipiprant:

The RU58841 effect of androgen receptor transcriptional activation, a nonsteroidal anti-androgen, was studied in the human prostate cancer PC3 cell line by cotransfection with wild-type androgen receptor (wt AR) and an androgen-responsive reporter (MMTV-ARE-CAT) construct. 

Anti-and rogens, hydroxyflutamide, and Casodex, and the antiestrogen, genistein, were studied in parallel for comparison with RU58841. The wt AR was activated only by the androgen dihydrotestosterone (DHT). Neither the anti-androgens nor antiestrogen can enhance AR transcriptional activity at 10(-11)-10(-7)M in PC3 cells. Hydroxyflutamide, RU58841, and Casodex, but not genistein, displayed competitively suppressive effects on DHT activation of wt AR. The potency of RU58841 was comparable to that of hydroxyflutamide.


HPLC:

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