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Voclosporin

Catalog No. T17235 CAS 515814-01-4

Synonyms: ISAtx-247

Voclosporin (ISAtx-247) is a novel and orally available calcium-modulated phosphatase (CN; PP2B) inhibitor and immunosuppressant for the treatment of lupus nephritis.

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Voclosporin, CAS 515814-01-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 139.00
5 mg	In stock	$ 372.00
10 mg	In stock	$ 597.00
25 mg	In stock	$ 1,190.00
50 mg	In stock	$ 1,890.00
100 mg	In stock	$ 2,970.00
1 mL * 10 mM (in DMSO)	In stock	$ 798.00

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Purity: 99.85%

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Description	Voclosporin (ISAtx-247) is a novel and orally available calcium-modulated phosphatase (CN; PP2B) inhibitor and immunosuppressant for the treatment of lupus nephritis.
In vitro	Voclosporin (ISATX247) is a calcineurin inhibitor that has shown more potency than Cyclosporine in vitro.[2]
In vivo	Voclosporin (23.7 mg or 39.5 mg, each twice daily; 265 subjects; 48 weeks) versus placebo in combination with mycophenolate mofetil (2 g/d) and rapidly tapered low-dose oral corticosteroids for induction of remission in LN. CRR at week 24 was achieved by 29 (32.6%) subjects in the low-dose voclosporin group, 24 (27.3%) subjects in the high-dose voclosporin group, and 17 (19.3%) subjects in the placebo group (OR=2.03 for low-dose voclosporin versus placebo). The significantly greater CRR rate in the low-dose voclosporin group persisted at 48 weeks, and CRRs were also significantly more common in the high-dose voclosporin group compared to placebo at 48 weeks. There were more serious adverse events in both voclosporin groups, and more deaths in the low-dose group compared to placebo and high-dose voclosporin groups (11.2%, 1.1%, and 2.3%, respectively). These results suggest that the addition of low-dose voclosporin to mycophenolate mofetil and corticosteroids for induction therapy of active LN results in a superior renal response compared to mycophenolate mofetil and corticosteroids alone, but higher rates of adverse events including death were observed.[3]

Synonyms	ISAtx-247
Molecular Weight	1214.62
Formula	C63H111N11O12
CAS No.	515814-01-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45.0 mg/mL (37.1 mM)

References and Literature

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. 3. Rovin BH, et al. A randomized, controlled double-blind study comparing the efficacy and safety of dose-ranging voclosporin with placebo in achieving remission in patients with active lupus nephritis. Kidney Int. 2019;95(1):219-231. 4. Arriens C, et al. Update on the Efficacy and Safety Profile of Voclosporin: An Integrated Analysis of Clinical Trials in Lupus Nephritis. Arthritis Care Res (Hoboken). 2023;75(7):1399-1408. 5. Cunningham MA, et al. LX211 (voclosporin) suppresses experimental uveitis and inhibits human T cells. Invest Ophthalmol Vis Sci. 2009;50(1):249-255.

Related compound libraries

This product is contained In the following compound libraries：

Approved Drug Library FDA-Approved & Pharmacopeia Drug Library

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Keywords

Voclosporin 515814-01-4 Metabolism Phosphatase ISAtx-247 inhibitor inhibit

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