Voclosporin( —— )

Catalog No. M33531 CAS No. 515814-01-4

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Product Name

Voclosporin
Note

Research use only, not for human use.
Brief Description

Voclosporin (ISAtx-247) is a novel, orally available calcium-modulated phosphatase (CN; PP2B) inhibitor and immunosuppressant used for treating lupus nephritis.
Description

Voclosporin (ISAtx-247) is a calcineurin (PP2B) (CN) inhibitor.
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. Voclosporin (ISATX247) is a calcineurin inhibitor that has shown more potency than Cyclosporine in vitro.
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).
Synonyms

——
Pathway

Metabolic Enzyme/Protease
Target

Phosphatase
Recptor

Phosphatase
Research Area

——
Indication

——

CAS Number

515814-01-4
Formula Weight

1214.62
Molecular Formula

C63H111N11O12
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : ≥ 50 mg/mL (41.17 mM; )
SMILES

[H][C@@]1(CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@@]([H])(NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C(=O)[C@H](CC)NC(=O)[C@]([H])([C@H](O)[C@H](C)C\C=C\C=C)N(C)C(=O)[C@]([H])(C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C1=O)C(C)C
Chemical Name

——

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

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