DA-7867

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

MedKoo CAT#: 581147

CAS#: 380382-38-7

Description: DA-7867 is a novel oxazolidinone. In vitro activities of DA-7867 were compared to those of linezolid and commonly used antimicrobials. DA-7867 had the lowest MIC for 90% of the aerobic gram-positive bacterial strains tested, </=0.25 micro g/ml, and it was more potent than linezolid. The in vitro activities of DA-7867, were compared to those of linezolid in 67 susceptible and drug-resistant clinical isolates of Mycobacterium tuberculosis. DA-7867 was the most active drug with an MIC(90) of 0.125 microg/ml, compared to the MIC(90)s of 4 microg/ml of garenoxacin and 2 microg/ml of linezolid.


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DA-7867 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 581147
Name: DA-7867
CAS#: 380382-38-7
Chemical Formula: C19H18FN7O3
Exact Mass: 411.1455
Molecular Weight: 411.4
Elemental Analysis: C, 55.47; H, 4.41; F, 4.62; N, 23.83; O, 11.67


Synonym: DA-7867; DA 7867; DA7867; UNII-491MT9GU8K;

IUPAC/Chemical Name: Acetamide, N-(((5S)-3-(3-fluoro-4-(6-(1-methyl-1H-tetrazol-5-yl)-3-pyridinyl)phenyl)-2-oxo-5-oxazolidinyl)methyl)-

InChi Key: XLLXHGCGAQJLLK-AWEZNQCLSA-N

InChi Code: InChI=1S/C19H18FN7O3/c1-11(28)21-9-14-10-27(19(29)30-14)13-4-5-15(16(20)7-13)12-3-6-17(22-8-12)18-23-24-25-26(18)2/h3-8,14H,9-10H2,1-2H3,(H,21,28)/t14-/m0/s1

SMILES Code: CC(NC[C@H]1CN(C2=CC=C(C3=CC=C(C4=NN=NN4C)N=C3)C(F)=C2)C(O1)=O)=O


Technical Data

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).

Harmonized System Code:
293490


References

1: Vera-Cabrera L, Castro-Garza J, Rendon A, Ocampo-Candiani J, Welsh O, Choi SH, Blackwood K, Molina-Torres C. In vitro susceptibility of Mycobacterium tuberculosis clinical isolates to garenoxacin and DA-7867. Antimicrob Agents Chemother. 2005 Oct;49(10):4351-3. PubMed PMID: 16189119; PubMed Central PMCID: PMC1251498.

2: Yong D, Yum JH, Lee K, Chong Y, Choi SH, Rhee JK. In vitro activities of DA-7867, a novel oxazolidinone, against recent clinical isolates of aerobic and anaerobic bacteria. Antimicrob Agents Chemother. 2004 Jan;48(1):352-7. Erratum in: Antimicrob Agents Chemother. 2004 May;48(5):1918. PubMed PMID: 14693566; PubMed Central PMCID: PMC310204.

3: Vera-Cabrera L, Brown-Elliott BA, Wallace RJ Jr, Ocampo-Candiani J, Welsh O, Choi SH, Molina-Torres CA. In vitro activities of the novel oxazolidinones DA-7867 and DA-7157 against rapidly and slowly growing mycobacteria. Antimicrob Agents Chemother. 2006 Dec;50(12):4027-9. Epub 2006 Oct 2. PubMed PMID: 17015632; PubMed Central PMCID: PMC1693997.

4: Vera-Cabrera L, Daw-Garza A, Said-Fernández S, Lozano-Garza HG, de Torres NW, Rocha NC, Ocampo-Candiani J, Choi SH, Welsh O. Therapeutic effect of a novel oxazolidinone, DA-7867, in BALB/c mice infected with Nocardia brasiliensis. PLoS Negl Trop Dis. 2008 Sep 10;2(9):e289. doi: 10.1371/journal.pntd.0000289. PubMed PMID: 18820738; PubMed Central PMCID: PMC2553479.

5: Yoon EJ, Jo YW, Choi SH, Lee TH, Rhee JK, Yoo M, Shim MJ, Choi EC. In vitro and in vivo activities of DA-7867, a new oxazolidinone, against aerobic gram-positive bacteria. Antimicrob Agents Chemother. 2005 Jun;49(6):2498-500. PubMed PMID: 15917554; PubMed Central PMCID: PMC1140508.

6: Ji HY, Lee HW, Chang SG, Lee JJ, Rhee JK, Kim WB, Lee HS. Liquid chromatography-tandem mass spectrometry for the determination of a new oxazolidinone antibiotic DA-7867 in human plasma. Biomed Chromatogr. 2004 Mar;18(2):86-9. PubMed PMID: 15039959.

7: Bae SK, Kwon JW, Kim WB, Lee I, Lee MG. Effects of acute renal failure on the pharmacokinetics of DA-7867, a new oxazolidinone, in rats. Biopharm Drug Dispos. 2006 Jan;27(1):29-37. PubMed PMID: 16302289.

8: Bae SK, Lee SJ, Kwon JW, Kim WB, Lee MG. Effects of protein-calorie malnutrition on the pharmacokinetics of DA-7867, a new oxazolidinone, in rats. J Pharm Pharmacol. 2004 May;56(5):635-42. PubMed PMID: 15142341.

9: Bae SK, Chung WS, Kim EJ, Rhee JK, Kwon JW, Kim WB, Lee MG. Pharmacokinetics, blood partition and protein binding of DA-7867, a new oxazolidinone. Biopharm Drug Dispos. 2004 Apr;25(3):127-35. PubMed PMID: 15083501.

10: Bae SK, Kim YC, Lee JK, Kwon JW, Yoo M, Lee I, Lee MG. Effects of water deprivation for 72 hours on the pharmacokinetics of DA-7867, a new oxazolidinone, in rats. Biopharm Drug Dispos. 2006 Apr;27(3):147-56. PubMed PMID: 16408258.

11: Bae SK, Yang SH, Lee SJ, Kwon JW, Kim WB, Lee DC, Lee MG. Pharmacokinetic changes of DA-7867, a new oxazolidinone, after intravenous and oral administration to rats with short-term and long-term diabetes mellitus induced by streptozotocin. Eur J Pharm Sci. 2005 Jun;25(2-3):337-45. Epub 2005 Apr 22. PubMed PMID: 15911231.

12: Bae SK, Chung WS, Kim EJ, Rhee JK, Kwon JW, Kim WB, Lee MG. Pharmacokinetics of DA-7867, a new oxazolidinone, after intravenous or oral administration to rats: intestinal first-pass effect. Antimicrob Agents Chemother. 2004 Feb;48(2):659-62. PubMed PMID: 14742232; PubMed Central PMCID: PMC321507.

13: Bae SK, Kim EJ, Kwon JW, Kim WB, Lee MG. High-performance liquid chromatographic analysis of DA-7867, a new oxazolidinone, in human plasma and urine and in rat tissue homogenates. J Chromatogr B Analyt Technol Biomed Life Sci. 2003 Sep 5;794(2):397-403. PubMed PMID: 12954392.

14: Bae SK, Kim EJ, Kwon JW, Kim WB, Lee I, Lee MG. Excretion and metabolism of DA-7867, a new oxazolidinone, in rats. Biopharm Drug Dispos. 2005 Mar;26(2):67-75. PubMed PMID: 15617136.

15: Bae SK, Lee SJ, Kwon JW, Kim WB, Lee I, Lee MG. Effects of bacterial lipopolysaccharide on the pharmacokinetics of DA-7867, a new oxazolidinone, in rats. J Pharm Sci. 2004 Sep;93(9):2364-73. PubMed PMID: 15295796.

16: Vera-Cabrera L, Ochoa-Felix EY, Gonzalez G, Tijerina R, Choi SH, Welsh O. In vitro activities of new quinolones and oxazolidinones against Actinomadura madurae. Antimicrob Agents Chemother. 2004 Mar;48(3):1037-9. PubMed PMID: 14982804; PubMed Central PMCID: PMC353109.

17: Vera-Cabrera L, Gonzalez E, Choi SH, Welsh O. In vitro activities of new antimicrobials against Nocardia brasiliensis. Antimicrob Agents Chemother. 2004 Feb;48(2):602-4. PubMed PMID: 14742215; PubMed Central PMCID: PMC321515.

18: Sood R, Bhadauriya T, Rao M, Gautam R, Malhotra S, Barman TK, Upadhyay DJ, Rattan A. Antimycobacterial activities of oxazolidinones: a review. Infect Disord Drug Targets. 2006 Dec;6(4):343-54. Review. PubMed PMID: 17168800.