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Chemical Compound Review:

Fulstan (1S,3S,5Z)-5-[(2E)-2- [(1R,3aR,7aR)-7a...

Synonyms: Hornel, Horner, Flocacitriol, Flocalcitriol, falecalcitriol, ...

Harada, M. et al., Hayashi, K. et al., Yoshimura, T. et al., Tanaka, M. et al., Komuro, S. et al., et al.

Akiba, Marumo, Owada, Kurihara, Inoue, Chida, Ando, Shinoda, Ishida, Ohashi, Komuro, Sato, Kanamaru, Kaneko, Nakatsuka, Yoshitake,

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Disease relevance of ST 630

Therefore, the high potency of ST-630 in stimulating bone resorption in organ culture may be associated with a difference between ST-630 and 1,25(OH)2D3 in the mode of metabolism in the cultured bones [1].

High impact information on ST 630

Controlled trial of falecalcitriol versus alfacalcidol in suppression of parathyroid hormone in hemodialysis patients with secondary hyperparathyroidism [2].
In vivo and in vitro pharmacokinetics and metabolism studies of 26,26,26,27,27,27-F6-1,25(OH)2 vitamin D3 (Falecalcitriol) in rat: induction of vitamin D3-24-hydroxylase (CYP24) responsible for 23S-hydroxylation in target tissues and the drop in serum levels [3].
These results indicate that ST-630 was more effective in inducing Cyp24 and calbindin-D9k gene expression than 1, 25(OH)2D3 when both compounds were injected into vitamin-D-deficient mice [4].
ST-630 was more effective than 1, 25-dihydroxyvitamin D3 [1,25(OH)2D3] with respect to the induction of Cyp24 and calbindin-D9k mRNAs in the kidney and in the small intestine [4].
3. These results show the direct evidence that CYP24 plays an essential role in the metabolism of ST-630 to yield its 23S-hydroxylated metabolite, as observed in cultured cells and experimental animal studies [5].

Biological context of ST 630

Furthermore, from the competitive binding experiments at 4 degrees C, the affinity of ST-630 was 6.4-fold lower than that of 1,25(OH)2D3 [6].

Anatomical context of ST 630

Sucrose density gradient experiments demonstrated that [3H]1,25(OH)2D3 bound to the 6S macromolecule in the cytosol of MC3T3-E1 cells at 4 degrees C. The inhibitory effect of 1,25(OH)2D3 was compared with that of ST-630 [6].
We investigated the metabolism of 26,26,26,27,27,27-hexafluoro-1 alpha,25-dihydroxyvitamin D3 (26,27-F6-1,25(OH)2D3, ST-630) and 1 alpha,25-dihydroxyvitamin (1,25(OH)2D3) in cultured neonatal mouse calvaria to elucidate why ST-630 is more potent than 1,25(OH)2D3 in stimulating bone resorption in organ culture [1].

Analytical, diagnostic and therapeutic context of ST 630

This metabolite was found to be 26,26,26,27,27,27-hexafluoro-23S-hydroxcalcitriol, a biologically active metabolite of ST-630, based on cochromatography on HPLC and mass spectrometric analysis [5].

References

Differences in metabolism between 26,26,26,27,27,27-hexafluoro-1 alpha, 25-dihydroxyvitamin D3 and 1 alpha, 25-dihydroxyvitamin D3 in cultured neonatal mouse calvaria. Harada, M., Miyahara, T., Kajita-Kondo, S., Kozakai, A., Higuchi, S., Otomo, S., Kozuka, H. Res. Commun. Mol. Pathol. Pharmacol. (1994) [Pubmed]
Controlled trial of falecalcitriol versus alfacalcidol in suppression of parathyroid hormone in hemodialysis patients with secondary hyperparathyroidism. Akiba, T., Marumo, F., Owada, A., Kurihara, S., Inoue, A., Chida, Y., Ando, R., Shinoda, T., Ishida, Y., Ohashi, Y. Am. J. Kidney Dis. (1998) [Pubmed]
In vivo and in vitro pharmacokinetics and metabolism studies of 26,26,26,27,27,27-F6-1,25(OH)2 vitamin D3 (Falecalcitriol) in rat: induction of vitamin D3-24-hydroxylase (CYP24) responsible for 23S-hydroxylation in target tissues and the drop in serum levels. Komuro, S., Sato, M., Kanamaru, H., Kaneko, H., Nakatsuka, I., Yoshitake, A. Xenobiotica (1999) [Pubmed]
Effect of 26,26,26,27,27,27-Hexafluoro-1,25-dihydroxyvitamin D3 on the expression of vitamin-D-responsive genes in vitamin-D-deficient mice. Yoshimura, T., Itoh, S., Tsujikawa, K., Yamada, E., Ishii, T., Iemura, O., Kameda, Y., Mimura, T., Kohama, Y. Pharmacology (1998) [Pubmed]
Rat CYP24 catalyses 23S-hydroxylation of 26,26,26,27,27,27-hexafluorocalcitriol in vitro. Hayashi, K., Akiyoshi-Shibata, M., Sakaki, T., Yabusaki, Y. Xenobiotica (1998) [Pubmed]
Temperature-dependent alteration of 1,25-dihydroxy-vitamin D3 receptor macromolecules in MC3T3-E1 cells: affinity of hexafluoro analog of 1,25-dihydroxyvitamin D3, ST-630, for these forms. Tanaka, M., Muramatsu, M., Higuchi, S., Otomo, S. Res. Commun. Mol. Pathol. Pharmacol. (1994) [Pubmed]

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