Delpazolid
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MedKoo CAT#: 329495

CAS#: 1219707-39-7

Description: Delpazolid, also known as LCB01-0371, is a new oxazolidinone with cyclic amidrazone. In vitro activity of LCB01-0371 against 624 clinical isolates was evaluated and compared with those of linezolid, vancomycin, and other antibiotics. LCB01-0371 showed good activity against Gram-positive pathogens. In vivo activity of LCB01-0371 against systemic infections in mice was also evaluated. LCB01-0371 was more active than linezolid against these systemic infections. LCB01-0371 showed bacteriostatic activity against Staphylococcus aureus.

Chemical Structure

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Delpazolid
CAS# 1219707-39-7
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 329495
Name: Delpazolid
CAS#: 1219707-39-7
Chemical Formula: C14H17FN4O3
Exact Mass: 308.13
Molecular Weight: 308.313
Elemental Analysis: C, 54.54; H, 5.56; F, 6.16; N, 18.17; O, 15.57

Price and Availability

Size Price Availability Quantity
50mg USD 450
100mg USD 750
200mg USD 1250
500mg USD 1950
1g USD 3250
2g USD 4850
5g USD 7450
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Synonym: Delpazolid; LCB01-0371; LCB 01-0371; LCB-01-0371; LCB010371; LCB 010371; LCB-010371.

IUPAC/Chemical Name: (5R)-3-[3-fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one

InChi Key: QLUWQAFDTNAYPN-LLVKDONJSA-N

InChi Code: InChI=1S/C14H17FN4O3/c1-17-4-5-18(9-16-17)13-3-2-10(6-12(13)15)19-7-11(8-20)22-14(19)21/h2-3,6,9,11,20H,4-5,7-8H2,1H3/t11-/m1/s1

SMILES Code: O=C1O[C@@H](CO)CN1C2=CC=C(N3C=NN(C)CC3)C(F)=C2

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:

Product Data:
Product Data
Instruction:
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Biological target: Delpazolid is a novel oxazolidinone antibiotic agent which can inhibit the growth of MSSA and MRSA with a MIC90 of 2 μg/mL for both of them.
In vitro activity: The intracellular antimicrobial activity of LCB01-0371 against M. abscessus was assessed after 8 h of replication inside murine bone marrow-derived macrophage (mBMDM) macrophages. As shown in Fig. 3, LCB01-0371 dramatically decreased the number of intracellular mycobacteria present at 2 days after infection at concentrations of 0.1, 1, and 10 μg/ml. LCB01-0371 treatment led to a 79% reduction in mycobacteria, which was comparable to that elicited by clarithromycin (96%). Hence, it is concluded that LCB010371 was active against intracellular M. abscessus. This result demonstrated that LCB01-0371 was an effective compound for the in vitro and intracellular inhibition of M. abscessus. Reference: Antimicrob Agents Chemother. 2017 Sep; 61(9): e02752-16. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5571369/
In vivo activity: The effects of LCB01-0371 therapy in mice intranasally infected with M. abscessus are shown in Fig. 4. LCB01-0371 was administered at 100 mg/kg in the mouse in vivo efficacy study (Tables S1 and S2) (22, 23). When LCB01-0371 was administered at 100 mg/kg daily (by gavage), the CFU counts tended to be decreased in the lungs of mice at 7 days after infection. LCB01-0371 showed a statistically significant effect compared with the saline control. Mice treated with 100 mg/kg LCB01-0371 resulted in the reduction of CFU in lungs to 3.7 log10, which was very similar to the values obtained for linezolid (Fig. 4A). This result demonstrated that the in vivo activity of LCB01-0371 against M. abscessus in the mouse model was comparable to that of linezolid, an antibiotic that is used for the treatment of M. abscessus infection. Thus, it was suggested that LCB01-0371 could replace linezolid for the treatment of lung infections, owing to its improved safety profile, such as reduced myelosuppression in a human study (phase 1b trial) (Fig. S1 and S2) and low toxicity (Table S3). Reference: Antimicrob Agents Chemother. 2017 Sep; 61(9): e02752-16. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5571369/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 30.0 97.30

Preparing Stock Solutions

The following data is based on the product molecular weight 308.31 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: 1. Kim TS, Choe JH, Kim YJ, Yang CS, Kwon HJ, Jeong J, Kim G, Park DE, Jo EK, Cho YL, Jang J. Activity of LCB01-0371, a Novel Oxazolidinone, against Mycobacterium abscessus. Antimicrob Agents Chemother. 2017 Aug 24;61(9):e02752-16. doi: 10.1128/AAC.02752-16. PMID: 28674049; PMCID: PMC5571369. 2. Jeong JW, Jung SJ, Lee HH, Kim YZ, Park TK, Cho YL, Chae SE, Baek SY, Woo SH, Lee HS, Kwak JH. In vitro and in vivo activities of LCB01-0371, a new oxazolidinone. Antimicrob Agents Chemother. 2010 Dec;54(12):5359-62. doi: 10.1128/AAC.0072310. Epub 2010 Sep 20. PMID: 20855730; PMCID: PMC2981296.
In vitro protocol: 1. Kim TS, Choe JH, Kim YJ, Yang CS, Kwon HJ, Jeong J, Kim G, Park DE, Jo EK, Cho YL, Jang J. Activity of LCB01-0371, a Novel Oxazolidinone, against Mycobacterium abscessus. Antimicrob Agents Chemother. 2017 Aug 24;61(9):e02752-16. doi: 10.1128/AAC.02752-16. PMID: 28674049; PMCID: PMC5571369. 2. Jeong JW, Jung SJ, Lee HH, Kim YZ, Park TK, Cho YL, Chae SE, Baek SY, Woo SH, Lee HS, Kwak JH. In vitro and in vivo activities of LCB01-0371, a new oxazolidinone. Antimicrob Agents Chemother. 2010 Dec;54(12):5359-62. doi: 10.1128/AAC.0072310. Epub 2010 Sep 20. PMID: 20855730; PMCID: PMC2981296.
In vivo protocol: 1. Kim TS, Choe JH, Kim YJ, Yang CS, Kwon HJ, Jeong J, Kim G, Park DE, Jo EK, Cho YL, Jang J. Activity of LCB01-0371, a Novel Oxazolidinone, against Mycobacterium abscessus. Antimicrob Agents Chemother. 2017 Aug 24;61(9):e02752-16. doi: 10.1128/AAC.02752-16. PMID: 28674049; PMCID: PMC5571369. 2. Jeong JW, Jung SJ, Lee HH, Kim YZ, Park TK, Cho YL, Chae SE, Baek SY, Woo SH, Lee HS, Kwak JH. In vitro and in vivo activities of LCB01-0371, a new oxazolidinone. Antimicrob Agents Chemother. 2010 Dec;54(12):5359-62. doi: 10.1128/AAC.0072310. Epub 2010 Sep 20. PMID: 20855730; PMCID: PMC2981296.

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1: Kim JS, Kim YH, Lee SH, Kim YH, Kim JW, Kang JY, Kim SK, Kim SJ, Kang YS, Kim TH, Mok J, Byun MK, Park HJ, Joh JS, Park YB, Lim HS, Choi H, Lee SH, Kim H, Yang J, Kim H, Shen X, Alsultan A, Cho I, Geiter L, Shim TS. Early Bactericidal Activity of Delpazolid (LCB01-0371) in Patients with Pulmonary Tuberculosis. Antimicrob Agents Chemother. 2022 Feb 15;66(2):e0168421. doi: 10.1128/AAC.01684-21. Epub 2021 Dec 6. PMID: 34871098; PMCID: PMC8846473.


2: Domínguez J, Boeree MJ, Cambau E, Chesov D, Conradie F, Cox V, Dheda K, Dudnyk A, Farhat MR, Gagneux S, Grobusch MP, Gröschel MI, Guglielmetti L, Kontsevaya I, Lange B, van Leth F, Lienhardt C, Mandalakas AM, Maurer FP, Merker M, Miotto P, Molina-Moya B, Morel F, Niemann S, Veziris N, Whitelaw A, Horsburgh CR Jr, Lange C; TBnet and RESIST-TB networks. Clinical implications of molecular drug resistance testing for Mycobacterium tuberculosis: a 2023 TBnet/RESIST-TB consensus statement. Lancet Infect Dis. 2023 Apr;23(4):e122-e137. doi: 10.1016/S1473-3099(22)00875-1. Epub 2023 Feb 28. Erratum in: Lancet Infect Dis. 2023 Mar 28;: PMID: 36868253.


3: Bahuguna A, Rawat DS. An overview of new antitubercular drugs, drug candidates, and their targets. Med Res Rev. 2020 Jan;40(1):263-292. doi: 10.1002/med.21602. Epub 2019 Jun 28. PMID: 31254295.


4: Park JS, Choi YJ, Kwon K, Choi SJ, Moon SM, Song KH, Kim ES, Park KU, Kim HB. In-vitro Activity of Delpazolid and Comparator Agents Against Methicillin-resistant Staphylococcus aureus Involved in Bloodstream Infection. Ann Lab Med. 2023 Jul 1;43(4):389-391. doi: 10.3343/alm.2023.43.4.389. Epub 2023 Feb 24. PMID: 36843409; PMCID: PMC9989538.


5: Zong Z, Jing W, Shi J, Wen S, Zhang T, Huo F, Shang Y, Liang Q, Huang H, Pang Y. Comparison of In Vitro Activity and MIC Distributions between the Novel Oxazolidinone Delpazolid and Linezolid against Multidrug-Resistant and Extensively Drug-Resistant Mycobacterium tuberculosis in China. Antimicrob Agents Chemother. 2018 Jul 27;62(8):e00165-18. doi: 10.1128/AAC.00165-18. PMID: 29844043; PMCID: PMC6105784.


6: Wen S, Gao X, Zhao W, Huo F, Jiang G, Dong L, Zhao L, Wang F, Yu X, Huang H. Comparison of the in vitro activity of linezolid, tedizolid, sutezolid, and delpazolid against rapidly growing mycobacteria isolated in Beijing, China. Int J Infect Dis. 2021 Aug;109:253-260. doi: 10.1016/j.ijid.2021.06.055. Epub 2021 Jul 1. PMID: 34216736.


7: Yu X, Huo F, Wang F, Wen S, Jiang G, Xue Y, Dong L, Zhao L, Zhu R, Huang H. In vitro Antimicrobial Activity Comparison of Linezolid, Tedizolid, Sutezolid and Delpazolid Against Slowly Growing Mycobacteria Isolated in Beijing, China. Infect Drug Resist. 2021 Nov 9;14:4689-4697. doi: 10.2147/IDR.S332835. PMID: 34785916; PMCID: PMC8590452.


8: Foti C, Piperno A, Scala A, Giuffrè O. Oxazolidinone Antibiotics: Chemical, Biological and Analytical Aspects. Molecules. 2021 Jul 14;26(14):4280. doi: 10.3390/molecules26144280. PMID: 34299555; PMCID: PMC8305375.


9: Chen J, Lv S, Liu J, Yu Y, Wang H, Zhang H. An Overview of Bioactive 1,3-Oxazole-Containing Alkaloids from Marine Organisms. Pharmaceuticals (Basel). 2021 Dec 6;14(12):1274. doi: 10.3390/ph14121274. PMID: 34959674; PMCID: PMC8706051.


10: Dierig A, Hoelscher M, Schultz S, Hoffmann L, Jarchow-MacDonald A, Svensson EM, Te Brake L, Aarnoutse R, Boeree M, McHugh TD, Wildner LM, Gong X, Phillips P, Minja LT, Ntinginya N, Mpagama S, Liyoyo A, Wallis RS, Sebe M, Mhimbira FA, Mbeya B, Rassool M, Geiter L, Cho YL, Heinrich N. A phase IIb, open-label, randomized controlled dose ranging multi-centre trial to evaluate the safety, tolerability, pharmacokinetics and exposure-response relationship of different doses of delpazolid in combination with bedaquiline delamanid moxifloxacin in adult subjects with newly diagnosed, uncomplicated, smear-positive, drug- sensitive pulmonary tuberculosis. Trials. 2023 Jun 6;24(1):382. doi: 10.1186/s13063-023-07354-5. PMID: 37280643; PMCID: PMC10243693.


11: Black TA, Buchwald UK. The pipeline of new molecules and regimens against drug-resistant tuberculosis. J Clin Tuberc Other Mycobact Dis. 2021 Nov 5;25:100285. doi: 10.1016/j.jctube.2021.100285. PMID: 34816020; PMCID: PMC8593651.


12: Yu JJ, Tang SJ. [Annual progress of chemotherapy of multidrug/rifampicin- resistant tuberculosis in 2022]. Zhonghua Jie He He Hu Xi Za Zhi. 2023 Jan 12;46(1):62-66. Chinese. doi: 10.3760/cma.j.cn112147-20221030-00853. PMID: 36617931.


13: Sellarès-Nadal J, Burgos J, Falcó V, Almirante B. Investigational and Experimental Drugs for Community-Acquired Pneumonia: the Current Evidence. J Exp Pharmacol. 2020 Nov 19;12:529-538. doi: 10.2147/JEP.S259286. PMID: 33239925; PMCID: PMC7682597.


14: Edwards BD, Field SK. The Struggle to End a Millennia-Long Pandemic: Novel Candidate and Repurposed Drugs for the Treatment of Tuberculosis. Drugs. 2022 Dec;82(18):1695-1715. doi: 10.1007/s40265-022-01817-w. Epub 2022 Dec 7. PMID: 36479687; PMCID: PMC9734533.


15: Wang C, Wang G, Huo F, Xue Y, Jia J, Dong L, Zhao L, Wang F, Huang H, Duan H. Novel oxazolidinones harbor potent in vitro activity against the clinical isolates of multidrug-resistant Mycobacterium tuberculosis in China. Front Med (Lausanne). 2022 Nov 29;9:1067516. doi: 10.3389/fmed.2022.1067516. PMID: 36523787; PMCID: PMC9745032.


16: Gao T, Yao C, Shang Y, Su R, Zhang X, Ren W, Li S, Shu W, Pang Y, Li Q. Antimicrobial Effect of Oxazolidinones and Its Synergistic Effect with Bedaquiline Against Mycobacterium abscessus Complex. Infect Drug Resist. 2023 Jan 14;16:279-287. doi: 10.2147/IDR.S395750. PMID: 36683910; PMCID: PMC9850832.


17: Kim DH, Kim SY, Koh WJ, Jhun BW. In Vitro Activity of Oxazolidinone against Nontuberculous Mycobacteria, Including Macrolide-Resistant Clinical Isolates. Antimicrob Agents Chemother. 2021 Jun 17;65(7):e0230620. doi: 10.1128/AAC.02306-20. Epub 2021 Jun 17. PMID: 33903101; PMCID: PMC8218642.


18: Egorova A, Jackson M, Gavrilyuk V, Makarov V. Pipeline of anti-Mycobacterium abscessus small molecules: Repurposable drugs and promising novel chemical entities. Med Res Rev. 2021 Jul;41(4):2350-2387. doi: 10.1002/med.21798. Epub 2021 Mar 1. PMID: 33645845; PMCID: PMC8217127.


19: Kim TS, Choe JH, Kim YJ, Yang CS, Kwon HJ, Jeong J, Kim G, Park DE, Jo EK, Cho YL, Jang J. Activity of LCB01-0371, a Novel Oxazolidinone, against Mycobacterium abscessus. Antimicrob Agents Chemother. 2017 Aug 24;61(9):e02752-16. doi: 10.1128/AAC.02752-16. PMID: 28674049; PMCID: PMC5571369.


20: Cho YS, Lim HS, Han S, Yoon SK, Kim H, Cho YL, Nam HS, Bae KS. Single-dose Intravenous Safety, Tolerability, and Pharmacokinetics and Absolute Bioavailability of LCB01-0371. Clin Ther. 2019 Jan;41(1):92-106. doi: 10.1016/j.clinthera.2018.11.009. Epub 2018 Dec 15. PMID: 30559004.