Voclosporin (For research purpose only) 515814-01-4

IUPAC Name: (3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-30-ethyl-33-[(1R,2R,4E)-1-hydroxy-2-methylhepta-4,6-dienyl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone
Molecular Weight:1214.65
Molecular Formula:C63H111N11O12
Quality Standard:In House

product description

Product Specification

Appearance:	White to off white solid
Boiling point:	1303.8 ± 65.0 ° C (Predicted)
Density:	1.016 ± 0.06g/cm3 (Predicted)
Storage conditions:	Storeat -20 ° C
Solubility:	benzene (trace), methanol (trace)
Acidity coefficient (pKa):	13.32 ± 0.70 (Predicted)

description1

PRODUCT DESCRIPTION

Voclosporin is a novel calcium regulated phosphatase inhibitor, structurally similar to cyclosporine A. After modification, its activity is increased by 3-4 times, and it has a dual and synergistic mechanism. By inhibiting calcium regulated phosphatase, it can block the expression of IL-2 and T cell-mediated immune response, stabilize renal podocytes. Cyclosporine is an intracellular calcium/calmodulin dependent serine/threonine phosphatase inhibitor, also known as a calcineurin inhibitor, developed by researchers. It was approved for marketing by the US Food and Drug Administration (FDA) on January 22, 2021, under the commercial name Lupkynis. In February 2021, cyclosporine was approved by the FDA as a combination immunosuppressive therapy for adult patients with active lupus nephritis.

Cyclosporine is the first oral medication used for active lupus nephritis. Compared with cyclosporine, vocyclosporine also has the advantage of less impact on cholesterol and triglycerides, and lower risk of diabetes.

As a calcineurin inhibitor, cyclosporine binds to calcineurin and inhibits its activity, thereby inhibiting lymphocyte proliferation, activating T cell cytoplasmic nuclear factor production, and T cell activation surface antigen expression, thereby reducing inflammation in lupus nephritis. Healthy volunteers take cyclosporine orally twice a day, and the inhibitory effect of the drug on calcineurin can be observed. The time it takes to reach the maximum blood concentration in the body is almost the same as the time it takes to reach the maximum inhibition rate of calcineurin.