Voclosporin | CAS#515814-01-4 | calcineurin inhibitor

MedKoo Cat#: 461014 | Name: Voclosporin

Featured

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Voclosporin is a novel calcineurin inhibitor intended for prevention of organ graft rejection and treatment of lupus nephritis. It was approved by the U.S. Food and Drug Administration (FDA) for the treatment of lupus nephritis (LN) on January 22, 2021.

Chemical Structure

Voclosporin

CAS#515814-01-4

Theoretical Analysis

MedKoo Cat#: 461014

Name: Voclosporin

CAS#: 515814-01-4

Chemical Formula: C63H111N11O12

Exact Mass: 1213.8414

Molecular Weight: 1214.64

Elemental Analysis: C, 62.30; H, 9.21; N, 12.68; O, 15.81

Price and Availability

Size	Price	Availability	Quantity
1mg	USD 350.00	2 Weeks
5mg	USD 1,050.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

ISATX 247; ISATX-247; ISATX247; LX 214; LX214; LX-214; R 1524; R1524; R-1524; trans-ISA 247 ISA247; ISA-247; LX211; LX-211; LX 211; Voclosporin; Luveniq;

IUPAC/Chemical Name

(3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-30-ethyl-33-((1R,2R,E)-1-hydroxy-2-methylhepta-4,6-dien-1-yl)-6,9,18,24-tetraisobutyl-3,21-diisopropyl-1,4,7,10,12,15,19,25,28-nonamethyl-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2,5,8,11,14,17,20,23,26,29,32-undecaone

InChi Key

BICRTLVBTLFLRD-PTWUADNWSA-N

InChi Code

InChI=1S/C63H111N11O12/c1-25-27-28-29-41(15)53(76)52-57(80)66-44(26-2)59(82)68(18)34-49(75)69(19)45(30-35(3)4)56(79)67-50(39(11)12)62(85)70(20)46(31-36(5)6)55(78)64-42(16)54(77)65-43(17)58(81)71(21)47(32-37(7)8)60(83)72(22)48(33-38(9)10)61(84)73(23)51(40(13)14)63(86)74(52)24/h25,27-28,35-48,50-53,76H,1,26,29-34H2,2-24H3,(H,64,78)(H,65,77)(H,66,80)(H,67,79)/b28-27+/t41-,42+,43-,44+,45+,46+,47+,48+,50+,51+,52+,53-/m1/s1

SMILES Code

CC[C@@H]1NC([C@@H](N(C([C@@H](N(C([C@@H](N(C([C@@H](N(C([C@H](NC([C@@H](NC([C@@H](N(C([C@H](C(C)C)NC([C@@H](N(C(CN(C1=O)C)=O)C)CC(C)C)=O)=O)C)CC(C)C)=O)C)=O)C)=O)C)CC(C)C)=O)C)CC(C)C)=O)C)C(C)C)=O)C)[C@@H]([C@@H](C/C=C/C=C)C)O)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.03.00

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 1,214.64 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Patel JP, Hardaswani D, Chaniyara SR, Mehta TD, Saiyed F, Bharakhada B, Goswami RJ. Navigating Lupus Nephritis: A Comprehensive Review of the Current Treatment Trends. Cureus. 2024 Oct 29;16(10):e72644. doi: 10.7759/cureus.72644. PMID: 39610592; PMCID: PMC11604181. 2: Dall'Era M, Kalunian K, Solomons N, Truman M, Hodge LS, Yap E, Askanase AD. Comparison of a voclosporin-based triple immunosuppressive therapy to high-dose glucocorticoid-based immunosuppressive therapy: a propensity analysis of the AURA-LV and AURORA 1 studies and ALMS. Lupus Sci Med. 2024 Nov 9;11(2):e001319. doi: 10.1136/lupus-2024-001319. PMID: 39521453; PMCID: PMC11552023. 3: Watanabe A, Akazawa T, Fujiu M. Understanding mechanisms of negative food effect for voclosporin using physiologically based pharmacokinetic modeling. Drug Metab Pharmacokinet. 2024 Dec;59:101032. doi: 10.1016/j.dmpk.2024.101032. Epub 2024 Sep 10. PMID: 39432969. 4: Ceobanu G, Edwards CJ. JAK inhibitors in systemic lupus erythematosus: Translating pathogenesis into therapy. Lupus. 2024 Nov;33(13):1403-1415. doi: 10.1177/09612033241287594. Epub 2024 Oct 9. PMID: 39383302. 5: Shimizu K, Yajima N, Yanai R, Wakabayashi K, Miwa Y, Matsuyama T. Prognostic Factors for Mortality in Patients With Autoimmune Diseases Complicated by Pneumocystis Pneumonia. Cureus. 2024 Aug 25;16(8):e67749. doi: 10.7759/cureus.67749. PMID: 39318924; PMCID: PMC11421872. 6: Claudel SE, Chan M, Scammell MK, Waikar SS. Challenges and Opportunities: Studying CKDu in the United States. Kidney360. 2024 Apr 1;5(4):607-609. doi: 10.34067/KID.0000000000000408. Epub 2024 Mar 6. PMID: 39292855; PMCID: PMC11093537. 7: Tian GQ, Li ZQ. Efficacy and safety of biologics, multitarget therapy, and standard therapy for lupus nephritis: a systematic review and network meta- analysis. Ren Fail. 2024 Dec;46(2):2395451. doi: 10.1080/0886022X.2024.2395451. Epub 2024 Aug 30. PMID: 39212247; PMCID: PMC11370699. 8: Roveta A, Parodi EL, Brezzi B, Tunesi F, Zanetti V, Merlotti G, Francese A, Maconi AG, Quaglia M. Lupus Nephritis from Pathogenesis to New Therapies: An Update. Int J Mol Sci. 2024 Aug 18;25(16):8981. doi: 10.3390/ijms25168981. PMID: 39201667; PMCID: PMC11354900. 9: Xagas E, Drouzas K, Liapis G, Lionaki S. Evidence based treatment for lupus nephritis: present perspectives and challenges. Front Nephrol. 2024 Aug 6;4:1417026. doi: 10.3389/fneph.2024.1417026. PMID: 39165275; PMCID: PMC11333434. 10: Afshinnia F, Rajendiran TM, Byun J, Arnipalli MS, Rehaume LM, Cross JL, Huizinga RB, Pennathur S. Voclosporin Induces Systemic Lipidomic Alterations: Implications for Lupus Nephritis Remission. Kidney Int Rep. 2024 May 9;9(8):2559-2562. doi: 10.1016/j.ekir.2024.04.069. PMID: 39156147; PMCID: PMC11328555. 11: Mucke J, Aringer M. Die 2023 EULAR-Empfehlungen zur Behandlung des systemischen Lupus erythematodes – Implikationen für die Versorgung in Deutschland [EULAR recommendations 2023 on the treatment of systemic lupus erythematosus -Implications for treatment in Germany]. Z Rheumatol. 2024 Aug;83(6):431-438. German. doi: 10.1007/s00393-024-01544-5. Epub 2024 Jul 22. PMID: 39037547. 12: Wiegley N, Arora S, Norouzi S, Rovin B. A Comprehensive and Practical Approach to the Management of Lupus Nephritis in the Current Era. Adv Kidney Dis Health. 2024 May;31(3):234-245. doi: 10.1053/j.akdh.2023.11.003. PMID: 39004463. 13: Wei KY, van Heugten MH, van Megen WH, van Veghel R, Rehaume LM, Cross JL, Viel JJ, van Willigenburg H, Silva PHI, Danser AHJ, de Baaij JHF, Hoorn EJ. Calcineurin inhibitor effects on kidney electrolyte handling and blood pressure: tacrolimus versus voclosporin. Nephrol Dial Transplant. 2024 May 22:gfae119. doi: 10.1093/ndt/gfae119. Epub ahead of print. PMID: 38777623. 14: Kostopoulou M, Mukhtyar CB, Bertsias G, Boumpas DT, Fanouriakis A. Management of systemic lupus erythematosus: a systematic literature review informing the 2023 update of the EULAR recommendations. Ann Rheum Dis. 2024 Oct 21;83(11):1489-1501. doi: 10.1136/ard-2023-225319. PMID: 38777375; PMCID: PMC11503129. 15: Kennedy L, Lee E, Flauto R, Atencio V, Birardi V. Evaluating the cost- effectiveness of voclosporin for the treatment of lupus nephritis in the United States. J Manag Care Spec Pharm. 2024 Aug;30(8):773-781. doi: 10.18553/jmcp.2024.23324. Epub 2024 May 8. PMID: 38717044; PMCID: PMC11293765. 16: Hoi A, Igel T, Mok CC, Arnaud L. Systemic lupus erythematosus. Lancet. 2024 May 25;403(10441):2326-2338. doi: 10.1016/S0140-6736(24)00398-2. Epub 2024 Apr 17. Erratum in: Lancet. 2024 May 25;403(10441):2292. doi: 10.1016/S0140-6736(24)01044-4. PMID: 38642569. 17: Siegel CH, Sammaritano LR. Systemic Lupus Erythematosus: A Review. JAMA. 2024 May 7;331(17):1480-1491. doi: 10.1001/jama.2024.2315. Erratum in: JAMA. 2024 Jun 25;331(24):2136. doi: 10.1001/jama.2024.10468. PMID: 38587826. 18: Karagenova R, Vodusek Z, Krimins R, Krieger A, Timlin H. Treatment With Voclosporin and Anifrolumab in a Patient With Lupus Nephritis and Refractory Discoid Lupus Erythematosus: A Case Report and Literature Review. Cureus. 2024 Mar 1;16(3):e55321. doi: 10.7759/cureus.55321. PMID: 38559540; PMCID: PMC10981842. 19: Moriano C, Bellido-Pastrana D, San Román Gutiérrez C, Rodríguez E. Evolution of diagnosis and treatment for lupus nephritis in Spain. Nefrologia (Engl Ed). 2023 Nov-Dec;43(6):668-675. doi: 10.1016/j.nefroe.2023.12.006. Epub 2024 Jan 20. PMID: 38246809. 20: Jiang Y, Tao M, Chen J, Luo L, You Q, Wu H, Zhang N. Calcineurin inhibitors in the treatment of systemic lupus erythematosus during pregnancy: A narrative review with emphasis on efficacy and safety. Eur J Obstet Gynecol Reprod Biol. 2024 Mar;294:148-155. doi: 10.1016/j.ejogrb.2023.12.039. Epub 2024 Jan 4. PMID: 38245953.