Radezolid
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Hodoodo CAT#: H319632

CAS#: 869884-78-6 (free base)

Description: Radezolid, also known as RX-1741, is a novel oxazolidinone antibiotic being developed by Rib-X Pharmaceuticals, Inc. for the treatment of serious multi-drug–resistant infections. Radezolid has completed two phase-II clinical trials. One of these clinical trials was for uncomplicated skin and skin-structure infections (uSSSI) and the other clinical trial was for community acquired pneumonia (CAP).


Chemical Structure

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Radezolid
CAS# 869884-78-6 (free base)

Theoretical Analysis

Hodoodo Cat#: H319632
Name: Radezolid
CAS#: 869884-78-6 (free base)
Chemical Formula: C22H23FN6O3
Exact Mass: 438.18
Molecular Weight: 438.463
Elemental Analysis: C, 60.27; H, 5.29; F, 4.33; N, 19.17; O, 10.95

Price and Availability

Size Price Availability Quantity
100mg USD 1950 2 Weeks
200mg USD 3650 2 months
500mg USD 3950 2 months
1g USD 6450 2 months
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Related CAS #: 869884-78-6 (free base)   869884-77-5 (HCl)    

Synonym: RX-1741; RX 1741; RX1741; Radezolid.

IUPAC/Chemical Name: (S)-N-((3-(4'-((((1H-1,2,3-triazol-5-yl)methyl)amino)methyl)-2-fluoro-[1,1'-biphenyl]-4-yl)-2-oxooxazolidin-5-yl)methyl)acetamide

InChi Key: BTTNOGHPGJANSW-IBGZPJMESA-N

InChi Code: InChI=1S/C22H23FN6O3/c1-14(30)25-12-19-13-29(22(31)32-19)18-6-7-20(21(23)8-18)16-4-2-15(3-5-16)9-24-10-17-11-26-28-27-17/h2-8,11,19,24H,9-10,12-13H2,1H3,(H,25,30)(H,26,27,28)/t19-/m0/s1

SMILES Code: CC(NC[C@H]1CN(C2=CC=C(C3=CC=C(CNCC4=CN=NN4)C=C3)C(F)=C2)C(O1)=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, 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).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 438.46 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.

Recalculate based on batch purity %
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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Bassetti M, Righi E. Safety profiles of old and new antimicrobials for the treatment of MRSA infections. Expert Opin Drug Saf. 2016 Jan 14. [Epub ahead of print] PubMed PMID: 26764972.

2: Kern WV. [New antibacterial agents on the market and in the pipeline]. Internist (Berl). 2015 Oct 18. [Epub ahead of print] German. PubMed PMID: 26475603.

3: Fulle S, Saini JS, Homeyer N, Gohlke H. Complex long-distance effects of mutations that confer linezolid resistance in the large ribosomal subunit. Nucleic Acids Res. 2015 Sep 18;43(16):7731-43. doi: 10.1093/nar/gkv729. Epub 2015 Jul 21. PubMed PMID: 26202966; PubMed Central PMCID: PMC4652758.

4: Mendes RE, Deshpande LM, Jones RN. Linezolid update: stable in vitro activity following more than a decade of clinical use and summary of associated resistance mechanisms. Drug Resist Updat. 2014 Apr;17(1-2):1-12. doi: 10.1016/j.drup.2014.04.002. Epub 2014 Apr 6. Review. PubMed PMID: 24880801.

5: Saini JS, Homeyer N, Fulle S, Gohlke H. Determinants of the species selectivity of oxazolidinone antibiotics targeting the large ribosomal subunit. Biol Chem. 2013 Nov;394(11):1529-41. doi: 10.1515/hsz-2013-0188. PubMed PMID: 24006327.

6: Bush K. Improving known classes of antibiotics: an optimistic approach for the future. Curr Opin Pharmacol. 2012 Oct;12(5):527-34. doi: 10.1016/j.coph.2012.06.003. Epub 2012 Jun 28. Review. PubMed PMID: 22748801.

7: Sutcliffe JA. Antibiotics in development targeting protein synthesis. Ann N Y Acad Sci. 2011 Dec;1241:122-52. doi: 10.1111/j.1749-6632.2011.06323.x. Review. PubMed PMID: 22191530.

8: Shaw KJ, Barbachyn MR. The oxazolidinones: past, present, and future. Ann N Y Acad Sci. 2011 Dec;1241:48-70. doi: 10.1111/j.1749-6632.2011.06330.x. Review. PubMed PMID: 22191526.

9: Locke JB, Finn J, Hilgers M, Morales G, Rahawi S, G C K, Picazo JJ, Im W, Shaw KJ, Stein JL. Structure-activity relationships of diverse oxazolidinones for linezolid-resistant Staphylococcus aureus strains possessing the cfr methyltransferase gene or ribosomal mutations. Antimicrob Agents Chemother. 2010 Dec;54(12):5337-43. doi: 10.1128/AAC.00663-10. Epub 2010 Sep 13. PubMed PMID: 20837751; PubMed Central PMCID: PMC2981267.

10: Lemaire S, Tulkens PM, Van Bambeke F. Cellular pharmacokinetics of the novel biaryloxazolidinone radezolid in phagocytic cells: studies with macrophages and polymorphonuclear neutrophils. Antimicrob Agents Chemother. 2010 Jun;54(6):2540-8. doi: 10.1128/AAC.01723-09. Epub 2010 Apr 12. PubMed PMID: 20385873; PubMed Central PMCID: PMC2876419.

11: Lemaire S, Kosowska-Shick K, Appelbaum PC, Verween G, Tulkens PM, Van Bambeke F. Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila. Antimicrob Agents Chemother. 2010 Jun;54(6):2549-59. doi: 10.1128/AAC.01724-09. Epub 2010 Apr 12. PubMed PMID: 20385852; PubMed Central PMCID: PMC2876393.