Solithromycin
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MedKoo CAT#: 314272

CAS#: 760981-83-7

Description: Solithromycin, also known as CEM-101 and OP-1068, is a ketolide antibiotic undergoing clinical development for the treatment of community-acquired pneumonia (CAP) and other infections. It is expected to be the first macrolide antibiotic available in intravenous, oral, and pediatric suspension formulations in over 20 years. Solithromycin exhibits excellent in vitro activity against a broad spectrum of Gram-positive respiratory tract pathogens, including macrolide-resistant strains. Solithromycin has activity against a wide variety of pathogens, and further research is being conducted for other infections.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 150 Same day
25mg USD 250 Same day
50mg USD 450 Same day
100mg USD 750 Same day
200mg USD 1250 Same day
500mg USD 1950 Same day
1g USD 2650 Same day
2g USD 4250 Same day
5g USD 6950 Two weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-27. Prices are subject to change without notice.

Solithromycin, purity > 98%, is in stock . Price updated on 1/19/2016. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 314272
Name: Solithromycin
CAS#: 760981-83-7
Chemical Formula: C43H65FN6O10
Exact Mass: 844.47462
Molecular Weight: 845.01
Elemental Analysis: C, 61.12; H, 7.75; F, 2.25; N, 9.95; O, 18.93


Synonym: CEM101; CEM101; CEM 101; OP1068; OP1068; OP 1068; Solithromycin

IUPAC/Chemical Name: (3aS,4R,7R,9R,10R,11R,13R,15S,15aR)-1-(4-(4-(3-aminophenyl)-1H-1,2,3-triazol-1-yl)butyl)-10-(((2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-4-ethyl-7-fluoro-11-methoxy-3a,7,9,11,13,15-hexamethyloctahydro-1H-[1]oxacyclotetradecino[4,3-d]oxazole-2,6,8,14(7H,9H)-tetraone

InChi Key: IXXFZUPTQVDPPK-QIFQIIIXSA-N

InChi Code: InChI=1S/C43H65FN6O10/c1-12-32-43(8)35(50(40(55)60-43)19-14-13-18-49-23-30(46-47-49)28-16-15-17-29(45)21-28)26(4)33(51)24(2)22-41(6,56-11)37(27(5)36(53)42(7,44)39(54)58-32)59-38-34(52)31(48(9)10)20-25(3)57-38/h15-17,21,23-27,31-32,34-35,37-38,52H,12-14,18-20,22,45H2,1-11H3/t24-,25-,26-,27+,31+,32-,34-,35-,37-,38+,41-,42-,43-/m1/s1

SMILES Code: CC[C@@H]1[C@]2(C)[C@H](N(CCCCN3C=C(C4=CC(N)=CC=C4)N=N3)C(O2)=O)[C@H](C)C([C@H](C)C[C@@](C)(OC)[C@H](O[C@H]5[C@H](O)[C@@H](N(C)C)C[C@@H](C)O5)[C@@H](C)C([C@@](C)(F)C(O1)=O)=O)=O


Technical Data

Appearance:
Solid powder

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

Certificate of Analysis:

Safety Data Sheet (SDS):

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


References

1: Jamieson BD, Ciric S, Fernandes P. Safety and Pharmacokinetics of Solithromycin in Subjects with Hepatic Impairment. Antimicrob Agents Chemother. 2015 Apr 13. pii: AAC.04652-14. [Epub ahead of print] PubMed PMID: 25870056.

2: Vandevelde NM, Tulkens PM, Muccioli GG, Van Bambeke F. Modulation of the activity of moxifloxacin and solithromycin in an in vitro pharmacodynamic model of Streptococcus pneumoniae naive and induced biofilms. J Antimicrob Chemother. 2015 Feb 23. pii: dkv032. [Epub ahead of print] PubMed PMID: 25712316.

3: Farrell DJ, Mendes RE, Jones RN. Antimicrobial Activity of Solithromycin against Serotyped Macrolide-Resistant Streptococcus pneumoniae Isolates Collected from U.S. Medical Centers in 2012. Antimicrob Agents Chemother. 2015 Apr;59(4):2432-4. doi: 10.1128/AAC.04568-14. Epub 2015 Jan 20. PubMed PMID: 25605359; PubMed Central PMCID: PMC4356815.

4: Keelan JA, Pugazhenthi K. Trans-placental passage and anti-inflammatory effects of solithromycin in the human placenta. Placenta. 2014 Dec;35(12):1043-8. doi: 10.1016/j.placenta.2014.09.009. Epub 2014 Sep 22. PubMed PMID: 25280973.

5: Miura Y, Payne MS, Keelan JA, Noe A, Carter S, Watts R, Spiller OB, Jobe AH, Kallapur SG, Saito M, Stock SJ, Newnham JP, Kemp MW. Maternal intravenous treatment with either azithromycin or solithromycin clears Ureaplasma parvum from the amniotic fluid in an ovine model of intrauterine infection. Antimicrob Agents Chemother. 2014 Sep;58(9):5413-20. doi: 10.1128/AAC.03187-14. Epub 2014 Jun 30. PubMed PMID: 24982089; PubMed Central PMCID: PMC4135857.

6: Jensen JS, Fernandes P, Unemo M. In vitro activity of the new fluoroketolide solithromycin (CEM-101) against macrolide-resistant and -susceptible Mycoplasma genitalium strains. Antimicrob Agents Chemother. 2014 Jun;58(6):3151-6. doi: 10.1128/AAC.02411-14. Epub 2014 Mar 17. PubMed PMID: 24637681; PubMed Central PMCID: PMC4068426.

7: Piccinelli G, Fernandes P, Bonfanti C, Caccuri F, Caruso A, De Francesco MA. In vitro activity of solithromycin against erythromycin-resistant Streptococcus agalactiae. Antimicrob Agents Chemother. 2014;58(3):1693-8. doi: 10.1128/AAC.02210-13. Epub 2013 Dec 30. PubMed PMID: 24379197; PubMed Central PMCID: PMC3957870.

8: Mallegol J, Fernandes P, Melano RG, Guyard C. Antimicrobial activity of solithromycin against clinical isolates of Legionella pneumophila serogroup 1. Antimicrob Agents Chemother. 2014;58(2):909-15. doi: 10.1128/AAC.01639-13. Epub 2013 Nov 25. PubMed PMID: 24277019; PubMed Central PMCID: PMC3910839.

9: Keelan JA, Kemp MW, Payne MS, Johnson D, Stock SJ, Saito M, Fernandes P, Newnham JP. Maternal administration of solithromycin, a new, potent, broad-spectrum fluoroketolide antibiotic, achieves fetal and intra-amniotic antimicrobial protection in a pregnant sheep model. Antimicrob Agents Chemother. 2014;58(1):447-54. doi: 10.1128/AAC.01743-13. Epub 2013 Nov 4. PubMed PMID: 24189250; PubMed Central PMCID: PMC3910757.

10: Mallegol J, Fernandes P, Seah C, Guyard C, Melano RG. Determination of in vitro activity of solithromycin at different pHs and its intracellular activity tested against clinical isolates of Neisseria gonorrhoeae from a laboratory collection. Antimicrob Agents Chemother. 2013 Jun 24. [Epub ahead of print] PubMed PMID: 23796936; PubMed Central PMCID: PMC3754335.

11: Kobayashi Y, Wada H, Rossios C, Takagi D, Charron C, Barnes PJ, Ito K. A novel macrolide/fluoroketolide, solithromycin (CEM-101), reverses corticosteroid insensitivity via phosphoinositide 3-kinase pathway inhibition. Br J Pharmacol. 2013 Jul;169(5):1024-34. doi: 10.1111/bph.12187. PubMed PMID: 23758162; PubMed Central PMCID: PMC3696326.

12: Oldach D, Clark K, Schranz J, Das A, Craft JC, Scott D, Jamieson BD, Fernandes P. Randomized, double-blind, multicenter phase 2 study comparing the efficacy and safety of oral solithromycin (CEM-101) to those of oral levofloxacin in the treatment of patients with community-acquired bacterial pneumonia. Antimicrob Agents Chemother. 2013 Jun;57(6):2526-34. doi: 10.1128/AAC.00197-13. Epub 2013 Mar 18. PubMed PMID: 23507282; PubMed Central PMCID: PMC3716175.

13: Kobayashi Y, Wada H, Rossios C, Takagi D, Higaki M, Mikura S, Goto H, Barnes PJ, Ito K. A novel macrolide solithromycin exerts superior anti-inflammatory effect via NF-κB inhibition. J Pharmacol Exp Ther. 2013 Apr;345(1):76-84. doi: 10.1124/jpet.112.200733. Epub 2013 Jan 28. PubMed PMID: 23359665.

14: Rodgers W, Frazier AD, Champney WS. Solithromycin inhibition of protein synthesis and ribosome biogenesis in Staphylococcus aureus, Streptococcus pneumoniae, and Haemophilus influenzae. Antimicrob Agents Chemother. 2013 Apr;57(4):1632-7. doi: 10.1128/AAC.02316-12. Epub 2013 Jan 14. PubMed PMID: 23318809; PubMed Central PMCID: PMC3623315.

15: Rodvold KA, Gotfried MH, Still JG, Clark K, Fernandes P. Comparison of plasma, epithelial lining fluid, and alveolar macrophage concentrations of solithromycin (CEM-101) in healthy adult subjects. Antimicrob Agents Chemother. 2012 Oct;56(10):5076-81. doi: 10.1128/AAC.00766-12. Epub 2012 Jul 16. PubMed PMID: 22802254; PubMed Central PMCID: PMC3457395.

16: Golparian D, Fernandes P, Ohnishi M, Jensen JS, Unemo M. In vitro activity of the new fluoroketolide solithromycin (CEM-101) against a large collection of clinical Neisseria gonorrhoeae isolates and international reference strains, including those with high-level antimicrobial resistance: potential treatment option for gonorrhea? Antimicrob Agents Chemother. 2012 May;56(5):2739-42. doi: 10.1128/AAC.00036-12. Epub 2012 Feb 21. PubMed PMID: 22354296; PubMed Central PMCID: PMC3346660.

17: Wittlin S, Ekland E, Craft JC, Lotharius J, Bathurst I, Fidock DA, Fernandes P. In vitro and in vivo activity of solithromycin (CEM-101) against Plasmodium species. Antimicrob Agents Chemother. 2012 Feb;56(2):703-7. doi: 10.1128/AAC.05039-11. Epub 2011 Nov 14. PubMed PMID: 22083475; PubMed Central PMCID: PMC3264280.

18: Still JG, Schranz J, Degenhardt TP, Scott D, Fernandes P, Gutierrez MJ, Clark K. Pharmacokinetics of solithromycin (CEM-101) after single or multiple oral doses and effects of food on single-dose bioavailability in healthy adult subjects. Antimicrob Agents Chemother. 2011 May;55(5):1997-2003. doi: 10.1128/AAC.01429-10. Epub 2011 Jan 31. PubMed PMID: 21282444; PubMed Central PMCID: PMC3088205.

19: Putnam SD, Sader HS, Farrell DJ, Biedenbach DJ, Castanheira M. Antimicrobial characterisation of solithromycin (CEM-101), a novel fluoroketolide: activity against staphylococci and enterococci. Int J Antimicrob Agents. 2011 Jan;37(1):39-45. doi: 10.1016/j.ijantimicag.2010.08.021. PubMed PMID: 21075602.

20: Farrell DJ, Castanheira M, Sader HS, Jones RN. The in vitro evaluation of solithromycin (CEM-101) against pathogens isolated in the United States and Europe (2009). J Infect. 2010 Dec;61(6):476-83. doi: 10.1016/j.jinf.2010.08.010. Epub 2010 Sep 8. PubMed PMID: 20831882.