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Voclosporin

Name: Voclosporin
Brand: TargetMol
SKU: T17235
Price: 106 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T17235Cas No. 515814-01-4

Alias ISAtx-247

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

Voclosporin

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Purity: 99.85%

Catalog No. T17235Alias ISAtx-247Cas No. 515814-01-4

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

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$106	-	In Stock
5 mg	$297	-	In Stock
10 mg	$419	-	In Stock
25 mg	$757	-	In Stock
50 mg	$1,060	-	In Stock
100 mg	$1,490	-	In Stock
1 mL x 10 mM (in DMSO)	$673	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.85%

Appearance:Solid

Color:White

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COA HPLC MS

Product Introduction

Bioactivity

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

Chemical Properties

Molecular Weight	1214.62
Formula	C₆₃H₁₁₁N₁₁O₁₂
Cas No.	515814-01-4
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
Relative Density.	1.016 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 31.25 mg/mL (25.73 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2 mg/mL (1.65 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	0.8233 mL	4.1165 mL	8.2330 mL	41.1651 mL
5 mM	0.1647 mL	0.8233 mL	1.6466 mL	8.2330 mL
10 mM	0.0823 mL	0.4117 mL	0.8233 mL	4.1165 mL
20 mM	0.0412 mL	0.2058 mL	0.4117 mL	2.0583 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc