Lumacaftor
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MedKoo CAT#: 510211

CAS#: 936727-05-8

Description: Lumacaftor, also known as VX-809, is a potent CFTR corrector, many be useful for treatment of patients with cystic fibrosis who have a phe508del CFTR mutation. Cystic fibrosis (CF) is a genetic disorder that causes multiorgan morbidity and premature death, most commonly from pulmonary dysfunction.


Price and Availability

Size
Price

100mg
USD 150
1g
USD 550
10g
USD 2950
100g
Ask price
Size
Price

200mg
USD 250
2g
USD 950
20g
USD 3950
Size
Price

500mg
USD 350
5g
USD 1950
50g
USD 6950

Lumacaftor (VX-809), purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 510211
Name: Lumacaftor
CAS#: 936727-05-8
Chemical Formula: C24H18F2N2O5
Exact Mass: 452.11838
Molecular Weight: 452.41
Elemental Analysis: C, 63.72; H, 4.01; F, 8.40; N, 6.19; O, 17.68


Synonym: VX-809; VX809; VX 809; Lumacaftor

IUPAC/Chemical Name: 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid

InChi Key: UFSKUSARDNFIRC-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H18F2N2O5/c1-13-5-8-19(27-20(13)14-3-2-4-15(11-14)21(29)30)28-22(31)23(9-10-23)16-6-7-17-18(12-16)33-24(25,26)32-17/h2-8,11-12H,9-10H2,1H3,(H,29,30)(H,27,28,31)

SMILES Code: O=C(O)C1=CC=CC(C2=NC(NC(C3(C4=CC=C(OC(F)(F)O5)C5=C4)CC3)=O)=CC=C2C)=C1


Technical Data

Appearance:
Solid powder

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

Certificate of Analysis:

Safety Data Sheet (MSDS):

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, not in water

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).

Harmonized System Code:
293490


Additional Information

  
  
 
 


References

1: Arora K, Naren AP. Pharmacological Correction of Cystic Fibrosis: Molecular Mechanisms at the Plasma Membrane to Augment Mutant CFTR Function. Curr Drug Targets. 2015 Dec 8. [Epub ahead of print] PubMed PMID: 26648081.

2: Brewington JJ, McPhail GL, Clancy JP. Lumacaftor alone and combined with ivacaftor: preclinical and clinical trial experience of F508del CFTR correction. Expert Rev Respir Med. 2015 Dec 9:1-13. [Epub ahead of print] PubMed PMID: 26581802.

3: Bosch B, De Boeck K. Searching for a cure for cystic fibrosis. A 25-year quest in a nutshell. Eur J Pediatr. 2015 Nov 14. [Epub ahead of print] PubMed PMID: 26567541.

4: Dong ZW, Chen J, Ruan YC, Zhou T, Chen Y, Chen Y, Tsang LL, Chan HC, Peng YZ. CFTR-regulated MAPK/NF-κB signaling in pulmonary inflammation in thermal inhalation injury. Sci Rep. 2015 Oct 30;5:15946. doi: 10.1038/srep15946. PubMed PMID: 26515683; PubMed Central PMCID: PMC4626762.

5: Rehman A, Baloch NU, Janahi IA. Lumacaftor-Ivacaftor in Patients with Cystic Fibrosis Homozygous for Phe508del CFTR. N Engl J Med. 2015 Oct 29;373(18):1783. doi: 10.1056/NEJMc1510466#SA1. PubMed PMID: 26510035.

6: Wainwright CE, Elborn JS, Ramsey BW. Lumacaftor-Ivacaftor in Patients with Cystic Fibrosis Homozygous for Phe508del CFTR. N Engl J Med. 2015 Oct 29;373(18):1783-4. doi: 10.1056/NEJMc1510466. PubMed PMID: 26510034.

7: Elborn JS, Ramsey B, Wainwright C, Boyle M. Response to: 'Lumacaftor/ivacaftor for patients homozygous for Phe508del-CFTR: should we curb our enthusiasm?' by Jones and Barry. Thorax. 2015 Oct 27. pii: thoraxjnl-2015-207611. doi: 10.1136/thoraxjnl-2015-207611. [Epub ahead of print] PubMed PMID: 26506855.

8: Matthes E, Goepp J, Carlile GW, Luo Y, Dejgaard K, Billet A, Robert R, Thomas DY, Hanrahan JW. Low free drug concentration prevents inhibition of F508del CFTR functional expression by the potentiator VX-770 (ivacaftor). Br J Pharmacol. 2015 Oct 22. doi: 10.1111/bph.13365. [Epub ahead of print] PubMed PMID: 26492939.

9: Gohil K. Pharmaceutical Approval Update. P T. 2015 Sep;40(9):567-8. PubMed PMID: 26417173; PubMed Central PMCID: PMC4571842.

10: Kuk K, Taylor-Cousar JL. Lumacaftor and ivacaftor in the management of patients with cystic fibrosis: current evidence and future prospects. Ther Adv Respir Dis. 2015 Dec;9(6):313-26. doi: 10.1177/1753465815601934. Epub 2015 Sep 28. Review. PubMed PMID: 26416827.

11: Silverman E. Orkambi's Slick Unveiling Puts Insurers in a Bind. Manag Care. 2015 Aug;24(8):16-7. PubMed PMID: 26399136.

12: Ong T, Ramsey BW. Update in Cystic Fibrosis 2014. Am J Respir Crit Care Med. 2015 Sep 15;192(6):669-75. doi: 10.1164/rccm.201504-0656UP. Review. PubMed PMID: 26371812.

13: Bali V, Lazrak A, Guroji P, Fu L, Matalon S, Bebok Z. A synonymous codon change alters the drug sensitivity of ΔF508 cystic fibrosis transmembrane conductance regulator. FASEB J. 2015 Sep 3. pii: fj.15-273714. [Epub ahead of print] PubMed PMID: 26336913.

14: Goralski JL, Davis SD. Improving complex medical care while awaiting next-generation CFTR potentiators and correctors: The current pipeline of therapeutics. Pediatr Pulmonol. 2015 Oct;50 Suppl 40:S66-73. doi: 10.1002/ppul.23253. PubMed PMID: 26335956.

15: Phuan PW, Veit G, Tan JA, Finkbeiner WE, Lukacs GL, Verkman AS. Potentiators of Defective ΔF508-CFTR Gating that Do Not Interfere with Corrector Action. Mol Pharmacol. 2015 Oct;88(4):791-9. doi: 10.1124/mol.115.099689. Epub 2015 Aug 5. PubMed PMID: 26245207; PubMed Central PMCID: PMC4576684.

16: Sinha C, Zhang W, Moon CS, Actis M, Yarlagadda S, Arora K, Woodroofe K, Clancy JP, Lin S, Ziady AG, Frizzell R, Fujii N, Naren AP. Capturing the Direct Binding of CFTR Correctors to CFTR by Using Click Chemistry. Chembiochem. 2015 Sep 21;16(14):2017-22. doi: 10.1002/cbic.201500123. Epub 2015 Aug 11. PubMed PMID: 26227551; PubMed Central PMCID: PMC4672727.

17: Ferkol T, Quinton P. Precision Medicine: At What Price? Am J Respir Crit Care Med. 2015 Sep 15;192(6):658-9. doi: 10.1164/rccm.201507-1428ED. PubMed PMID: 26207804.

18: Tomati V, Sondo E, Armirotti A, Caci E, Pesce E, Marini M, Gianotti A, Jeon YJ, Cilli M, Pistorio A, Mastracci L, Ravazzolo R, Scholte B, Ronai Z, Galietta LJ, Pedemonte N. Genetic Inhibition Of The Ubiquitin Ligase Rnf5 Attenuates Phenotypes Associated To F508del Cystic Fibrosis Mutation. Sci Rep. 2015 Jul 17;5:12138. doi: 10.1038/srep12138. PubMed PMID: 26183966; PubMed Central PMCID: PMC4505316.

19: Nau JY. [Cystic Fibrosis: toward a genetic treatment; Clostridium difficile versus Clostridium difficile]. Rev Med Suisse. 2015 May 27;11(476):1210-1. French. PubMed PMID: 26182641.

20: Farinha CM, Sousa M, Canato S, Schmidt A, Uliyakina I, Amaral MD. Increased efficacy of VX-809 in different cellular systems results from an early stabilization effect of F508del-CFTR. Pharmacol Res Perspect. 2015 Aug;3(4):e00152. doi: 10.1002/prp2.152. Epub 2015 Jun 11. PubMed PMID: 26171232; PubMed Central PMCID: PMC4492728.