Wuhan Vanz Pharm Inc Supply 4'-DiMethylaMino 7,8-Dihydroxyflavone HydrobroMide CAS:1205548-00-0.
The analogue of 7,8-Dihydroxyflavone (7,8-DHF) is a naturally occurring flavone found in Godmania aesculifolia, Tridax procumbens, and primula tree leaves. It has been found to act as a potent and selective small-molecule agonist of the tropomyosin receptor kinase B (TrkB) (Kd ≈ 320 nM), the main signaling receptor of the neurotrophin brain-derived neurotrophic factor (BDNF). 7,8-DHF is both orally bioavailable and able to penetrate the blood–brain barrier. A prodrug of 7,8-DHF with greatly improved potency and pharmacokinetics, R13 (and, formerly, R7), is under development for the treatment of Alzheimer's disease.
7,8-DHF has demonstrated therapeutic efficacy in animal models of a variety of central nervous system disorders, including depression, Alzheimer's disease, cognitive deficits in schizophrenia, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, traumatic brain injury, cerebral ischemia, fragile X syndrome, and Rett syndrome. 7,8-DHF also shows efficacy in animal models of age-associated cognitive impairment and enhances memory consolidation and emotional learning in healthy rodents. In addition, 7,8-DHF possesses powerful antioxidant activity independent of its actions on the TrkB receptor, and protects against glutamate-induced excitotoxicity, 6-hydroxydopamine-induced dopaminergic neurotoxicity, and oxidative stress-induced genotoxicity. It was also found to block methamphetamine-induced dopaminergic neurotoxicity, an effect which, in contrast to the preceding, was found to be TrkB-dependent.
In 2017, evidence was published suggesting that 7,8-DHF and various other reported small-molecule TrkB agonists might not actually be direct agonists of the TrkB and might be mediating their observed effects by other means.
7,8-DHF has been found to act as a weak aromatase inhibitor in vitro (Ki = 10 μM), though there is evidence to suggest that this might not be the case in vivo. In addition, it has been found to inhibit aldehyde dehydrogenase and estrogen sulfotransferase in vitro (Ki = 35 μM and 1–3 μM, respectively), though similarly to the case of aromatase, these activities have not yet been confirmed in vivo. Unlike many other flavonoids, 7,8-DHF does not show any inhibitory activity on 17β-hydroxysteroid dehydrogenase. 7,8-DHF has also been observed to possess in vitro antiestrogenic effects at very high concentrations (Ki = 50 μM).
A variety of close structural analogues of 7,8-DHF have also been found to act as TrkB agonists in vitro, including diosmetin (5,7,3'-trihydroxy-4'-methoxyflavone), norwogonin (5,7,8-trihydroxyflavone), 4'-dimethylamino-7,8-dihydroxyflavone (4'-DMA-7,8-DHF), 7,8,3'-trihydroxyflavone, 7,3'-dihydroxyflavone, 7,8,2'-trihydroxyflavone, 3,7,8,2'-tetrahydroxyflavone, and 3,7-dihydroxyflavone. The highly hydroxylated analogue gossypetin (3,5,7,8,3',4'-hexahydroxyflavone), conversely, appears to be an antagonist of TrkB in vitro.
Wuhan Vanz Pharm Inc, which is specialized in custom synthesis and R&D, is located in Wuhan, China， we Supply Sarms Powder with Top Quality, High Purity and Best Price. Our Sarms Powder products including MK 677, MK2866, GW501516, SR9009, SR9011, S4, S23, LGD4033, RAD140, etc.. We have established long-term cooperation with Shanghai Institute of Organic Chemistry, Wuhan University etc. As a special team in organic chemistry and medicinal chemistry, we support the technology of R&D on new product. We have strong advantages on the process research and product R&D, pay attention to researching and developing new technology which is self-owned intellectual property right. We are special at developing Drug for the respiratory, antidepressant, antivirus. We have completed R&D of more than 20 APIs and intermediates after the company founded.
Our R&D center covers an area of 1000 square meters, with four synthesis labs, one scale-up pilot labs and one analytical lab. The lab is equipped with complete laboratory facilities and equipment. We have a professional research team of highly qualified and experienced chemists. most of our R&D team are Master and higher. With their effort, we quickly transfer the science fruit into production. Our manufacturing site is located in Wuhan which is equipped with 100L~5000L reactors; we can offer one-stop services from R&D to commercial production. (Normal reaction/ High-pressure reaction/ Catalytic reaction/ Low-Temperature reaction).
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