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FALECALCITRIOL

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Falecalcitriol, previously known as flocalcitrol, was launched by several codevelopers in Japan for the treatment of secondary hyperthyroidism (SHPT). This hexafluorinated analog of 1α,25-dihydroxyvitamin D3 (calcitriol), the hormonally active form of vitamin D3, can be obtained by several different synthetic routes from a conveniently protected cholestenol, a key step being an aldol reaction with hexafluoroacetone. Falecalcitriol is several times more active than 1,25(OH)<sub>2</sub>D<sub>3</sub> in regulating the proliferation of parathyroid cells and parathyroid hormone (PTH) synthesis that are believed to be mediated through binding to VDR, a nuclear receptor for vitamin D; furthermore, it was proposed that a bioactive 23S-hydroxylated metabolite, resistant to further metabolism, contributes to the retention of an active compound for longer in cells and so, to significantly lengthen the duration of action. In a comparative clinical study conducted in hemodialysis patients with moderate to severe SHPT, falecalcitriol was found to be more active than alfacalcidol in suppressing parathyroid hormone without triggering hypercalcemia.
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  • Company Name:Wuhan Wsem Biological Co., Ltd.
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  • Products Intro:Product Name:Falecalcitriol
    CAS:83805-11-2
    Purity:99% Package:100mg/RMB 35000;200mg/RMB 50000
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  • Company Name:Zhengzhou TRIZ Pharmaceutical Technology Co., Ltd.
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    Purity:98 Package:1kgs;10kgs;100kgs
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