Senicapoc | ICA-17043 | CAS#289656-45-7 | Gardos Channel Inhibitor

MedKoo Cat#: 526815 | Name: Senicapoc

Description:

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

Senicapoc, also known as ICA-17043, is a potent Gardos Channel Inhibitor for the treatment of a subset of Hereditary Xerocytosis caused by mutations in the Gardos channel. Senicapoc (ICA-17043) is a potential therapy for the prevention and treatment of hemolysis-associated complications in sickle cell anemia. Senicapoc exhibits Antimalarial Activity.

Chemical Structure

Senicapoc

CAS#289656-45-7

Theoretical Analysis

MedKoo Cat#: 526815

Name: Senicapoc

CAS#: 289656-45-7

Chemical Formula: C20H15F2NO

Exact Mass: 323.1122

Molecular Weight: 323.34

Elemental Analysis: C, 74.29; H, 4.68; F, 11.75; N, 4.33; O, 4.95

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

Bulk Inquiry

Related CAS #

No Data

Synonym

ICA-17043; ICA 17043; ICA17043; Senicapoc

IUPAC/Chemical Name

2,2-bis(4-fluorophenyl)-2-phenylacetamide

InChi Key

SCTZUZTYRMOMKT-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H15F2NO/c21-17-10-6-15(7-11-17)20(19(23)24,14-4-2-1-3-5-14)16-8-12-18(22)13-9-16/h1-13H,(H2,23,24)

SMILES Code

C1=CC=C(C=C1)C(C2=CC=C(C=C2)F)(C3=CC=C(C=C3)F)C(=O)N

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

>2 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

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 323.34 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: Rapetti-Mauss R, Soriani O, Vinti H, Badens C, Guizouarn H. Senicapoc: a potent candidate for the treatment of a subset of Hereditary Xerocytosis caused by mutations in the Gardos channel. Haematologica. 2016 Jul 21. pii: haematol.2016.149104. [Epub ahead of print] PubMed PMID: 27443288. 2: Dale E, Staal RG, Eder C, Möller T. K(Ca) 3.1-a microglial target ready for drug repurposing? Glia. 2016 Apr 28. doi: 10.1002/glia.22992. [Epub ahead of print] Review. PubMed PMID: 27121595. 3: Nagalla S, Ballas SK. Drugs for preventing red blood cell dehydration in people with sickle cell disease. Cochrane Database Syst Rev. 2016 Mar 4;3:CD003426. doi: 10.1002/14651858.CD003426.pub5. Review. PubMed PMID: 26942338. 4: Tubman VN, Mejia P, Shmukler BE, Bei AK, Alper SL, Mitchell JR, Brugnara C, Duraisingh MT. The Clinically Tested Gardos Channel Inhibitor Senicapoc Exhibits Antimalarial Activity. Antimicrob Agents Chemother. 2015 Oct 12;60(1):613-6. doi: 10.1128/AAC.01668-15. PubMed PMID: 26459896; PubMed Central PMCID: PMC4704178. 5: Roach KM, Feghali-Bostwick C, Wulff H, Amrani Y, Bradding P. Human lung myofibroblast TGFβ1-dependent Smad2/3 signalling is Ca(2+)-dependent and regulated by KCa3.1 K(+) channels. Fibrogenesis Tissue Repair. 2015 Mar 26;8:5. doi: 10.1186/s13069-015-0022-0. eCollection 2015. PubMed PMID: 25829947; PubMed Central PMCID: PMC4379608. 6: Roach KM, Wulff H, Feghali-Bostwick C, Amrani Y, Bradding P. Increased constitutive αSMA and Smad2/3 expression in idiopathic pulmonary fibrosis myofibroblasts is KCa3.1-dependent. Respir Res. 2014 Dec 5;15:155. doi: 10.1186/s12931-014-0155-5. PubMed PMID: 25476248; PubMed Central PMCID: PMC4263015. 7: Koch Hansen L, Sevelsted-Møller L, Rabjerg M, Larsen D, Hansen TP, Klinge L, Wulff H, Knudsen T, Kjeldsen J, Köhler R. Expression of T-cell KV1.3 potassium channel correlates with pro-inflammatory cytokines and disease activity in ulcerative colitis. J Crohns Colitis. 2014 Nov;8(11):1378-91. doi: 10.1016/j.crohns.2014.04.003. Epub 2014 May 3. PubMed PMID: 24793818; PubMed Central PMCID: PMC4216648. 8: Roach KM, Duffy SM, Coward W, Feghali-Bostwick C, Wulff H, Bradding P. The K+ channel KCa3.1 as a novel target for idiopathic pulmonary fibrosis. PLoS One. 2013 Dec 31;8(12):e85244. doi: 10.1371/journal.pone.0085244. eCollection 2013. Erratum in: PLoS One. 2014;9(1). doi:10.1371/annotation/790e86f8-3506-49d6-b7d0-7dbbc580d808. Roach, Katy Morgan [corrected to Roach, Katy M]. PubMed PMID: 24392001; PubMed Central PMCID: PMC3877378. 9: Van Der Velden J, Sum G, Barker D, Koumoundouros E, Barcham G, Wulff H, Castle N, Bradding P, Snibson K. K(Ca)3.1 channel-blockade attenuates airway pathophysiology in a sheep model of chronic asthma. PLoS One. 2013 Jun 24;8(6):e66886. doi: 10.1371/journal.pone.0066886. Print 2013. PubMed PMID: 23826167; PubMed Central PMCID: PMC3691218. 10: Jørgensen S, Dyhring T, Brown DT, Strøbæk D, Christophersen P, Demnitz J. A high-throughput screening campaign for detection of ca(2+)-activated k(+) channel activators and inhibitors using a fluorometric imaging plate reader-based tl(+)-influx assay. Assay Drug Dev Technol. 2013 Apr;11(3):163-72. doi: 10.1089/adt.2012.479. Epub 2012 Nov 30. PubMed PMID: 23198866. 11: Nagalla S, Ballas SK. Drugs for preventing red blood cell dehydration in people with sickle cell disease. Cochrane Database Syst Rev. 2012 Jul 11;(7):CD003426. doi: 10.1002/14651858.CD003426.pub4. Review. Update in: Cochrane Database Syst Rev. 2016;3:CD003426. PubMed PMID: 22786485. 12: Castro OL, Gordeuk VR, Gladwin MT, Steinberg MH. Senicapoc trial results support the existence of different sub-phenotypes of sickle cell disease with possible drug-induced phenotypic shifts. Br J Haematol. 2011 Dec;155(5):636-8. doi: 10.1111/j.1365-2141.2011.08758.x. Epub 2011 Jul 7. PubMed PMID: 21732927. 13: Minniti CP, Wilson J, Mendelsohn L, Rigdon GC, Stocker JW, Remaley AT, Kato GJ. Anti-haemolytic effect of senicapoc and decrease in NT-proBNP in adults with sickle cell anaemia. Br J Haematol. 2011 Dec;155(5):634-6. doi: 10.1111/j.1365-2141.2011.08757.x. Epub 2011 Jun 8. PubMed PMID: 21651507; PubMed Central PMCID: PMC3215801. 14: Ataga KI, Reid M, Ballas SK, Yasin Z, Bigelow C, James LS, Smith WR, Galacteros F, Kutlar A, Hull JH, Stocker JW; ICA-17043-10 Study Investigators. Improvements in haemolysis and indicators of erythrocyte survival do not correlate with acute vaso-occlusive crises in patients with sickle cell disease: a phase III randomized, placebo-controlled, double-blind study of the Gardos channel blocker senicapoc (ICA-17043). Br J Haematol. 2011 Apr;153(1):92-104. doi: 10.1111/j.1365-2141.2010.08520.x. Epub 2011 Feb 17. PubMed PMID: 21323872. 15: Nagalla S, Ballas SK. Drugs for preventing red blood cell dehydration in people with sickle cell disease. Cochrane Database Syst Rev. 2010 Jan 20;(1):CD003426. doi: 10.1002/14651858.CD003426.pub3. Review. Update in: Cochrane Database Syst Rev. 2012;7:CD003426. PubMed PMID: 20091545. 16: Raghupathy R, Billett HH. Promising therapies in sickle cell disease. Cardiovasc Hematol Disord Drug Targets. 2009 Mar;9(1):1-8. Review. PubMed PMID: 19275572. 17: Ataga KI, Stocker J. Senicapoc (ICA-17043): a potential therapy for the prevention and treatment of hemolysis-associated complications in sickle cell anemia. Expert Opin Investig Drugs. 2009 Feb;18(2):231-9. doi: 10.1517/13543780802708011 . Review. PubMed PMID: 19236269. 18: Joiner CH. Gardos pathway to sickle cell therapies? Blood. 2008 Apr 15;111(8):3918-9. PubMed PMID: 18434967; PubMed Central PMCID: PMC2288713. 19: McNaughton-Smith GA, Burns JF, Stocker JW, Rigdon GC, Creech C, Arrington S, Shelton T, de Franceschi L. Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. J Med Chem. 2008 Feb 28;51(4):976-82. doi: 10.1021/jm070663s. Epub 2008 Jan 31. PubMed PMID: 18232633. 20: Ataga KI, Smith WR, De Castro LM, Swerdlow P, Saunthararajah Y, Castro O, Vichinsky E, Kutlar A, Orringer EP, Rigdon GC, Stocker JW; ICA-17043-05 Investigators. Efficacy and safety of the Gardos channel blocker, senicapoc (ICA-17043), in patients with sickle cell anemia. Blood. 2008 Apr 15;111(8):3991-7. doi: 10.1182/blood-2007-08-110098. Epub 2008 Jan 11. PubMed PMID: 18192510.