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515814-01-4

515814-01-4 structure
515814-01-4 structure
  • Name: Voclosporin-d4
  • Chemical Name: Voclosporin Discontinued
  • CAS Number: 515814-01-4
  • Molecular Formula: C63H111N11O12
  • Molecular Weight: 1214.62000
  • Catalog: Research Areas Inflammation/Immunology
  • Create Date: 2017-12-24 21:18:15
  • Modify Date: 2024-01-04 12:36:29
  • Voclosporin is a calcineurin (CN) inhibitor.

Name Voclosporin Discontinued
Synonyms voclosporin
Description Voclosporin is a calcineurin (CN) inhibitor.
Related Catalog
Target

Calcineurin[1]

In Vitro This novel semi-synthetic calcineurin (CN) inhibitor is designated Voclosporin (ISATX247). The efficacy of Voclosporin as an immunosuppressive agent is examined using an in vitro calcineurin assay[1]. Voclosporin (ISATX247) is a calcineurin inhibitor that has shown more potency than Cyclosporine in vitro[2].
In Vivo All animals tolerate Voclosporin (ISATX247) and Cyclosporine A (CsA) very well. There are no severe adverse effects associated with either drug. In the Voclosporin group, all animals except 1 have diarrhea of different durations during the study (mean 2.3 days, range 2 to 7 days). This differs from the CsA and the control groups, where no animals have diarrhea. Mean weight loss at the end of the study is slightly higher in the Voclosporin group than in the CsA and control groups (3.4% vs 2.0% and 1.0%, respectively)[2].
Animal Admin Monkey[2] Wild-caught, male cynomolgus monkeys, weighing between 5 and 8 kg, are used. Four groups of animals are treated twice daily at 8:00 AM and 6:00 PM for 7 days with the following doses: Group I (n=6), Voclosporin 25 mg/kg; Group II (n=6), Voclosporin 50 mg/kg; Group III (n=5), CsA 25 mg/kg; and Group IV (n=4), vehicle (no drug) 1 mL/kg. Levels of Cyclosporine and Voclosporin in whole blood are measured by liquid chromatography/mass spectrometry[2].
References

[1]. Abel MD, et al. ISATX247: a novel calcineurin inhibitor. J Heart Lung Transplant. 2001 Feb;20(2):161.

[2]. Stalder M, et al. In vivo evaluation of the novel calcineurin inhibitor ISATX247 in non-human primates. J Heart Lung Transplant. 2003 Dec;22(12):1343-52.

Molecular Formula C63H111N11O12
Molecular Weight 1214.62000
Exact Mass 1213.84000
PSA 278.80000
LogP 4.31560
Storage condition 2-8℃