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Gepotidacin

Product Name
Gepotidacin
CAS No.
1075236-89-3
Chemical Name
Gepotidacin
Synonyms
Buagafuran;Gepotidacin;GSK-2140944;Gepotidacin (GSK2140944);(R)-2-((4-(((3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-yl)methyl)amino)piperidin-1-yl)methyl)-1,2-dihydro-3H,8H-2a,5,8a-triazaacenaphthylene-3,8-dione;3H,8H-2a,5,8a-Triazaacenaphthylene-3,8-dione, 2-[[4-[[(3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-yl)methyl]amino]-1-piperidinyl]methyl]-1,2-dihydro-, (2R)-;(R)-2-((4-(((3,4-Dihydro-2H-pyrano[2,3-c]pyridin-6-yl)methyl)amino)piperidin-1-yl)methyl)-1,2-dihydro-3H,8H-2a,5,8a-triazaacenaphthylene-3,8-dione , Gepotidacin
CBNumber
CB13133117
Molecular Formula
C24H28N6O3
Formula Weight
448.52
MOL File
1075236-89-3.mol
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Gepotidacin Property

Boiling point:
661.9±65.0 °C(Predicted)
Density 
1.52±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO : 7.14 mg/mL (15.92 mM)
form 
Solid
pka
7.88±0.10(Predicted)
color 
White to yellow
InChIKey
PZFAZQUREQIODZ-LJQANCHMSA-N
SMILES
C1N2C3=C(C=CC2=O)N=CC(=O)N3[C@@H]1CN1CCC(NCC2N=CC3OCCCC=3C=2)CC1
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H373May cause damage to organs through prolonged or repeated exposure

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P314Get medical advice/attention if you feel unwell.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

ChemScene
Product number
CS-6531
Product name
Gepotidacin
Purity
99.75%
Packaging
1mg
Price
$132
Updated
2021/12/16
ChemScene
Product number
CS-6531
Product name
Gepotidacin
Purity
99.75%
Packaging
5mg
Price
$420
Updated
2021/12/16
ChemScene
Product number
CS-6531
Product name
Gepotidacin
Purity
99.75%
Packaging
10mg
Price
$720
Updated
2021/12/16
ChemScene
Product number
CS-6531
Product name
Gepotidacin
Purity
99.75%
Packaging
50mg
Price
$2340
Updated
2021/12/16
ChemScene
Product number
CS-6531
Product name
Gepotidacin
Purity
99.75%
Packaging
100mg
Price
$3360
Updated
2021/12/16
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Gepotidacin Chemical Properties,Usage,Production

Description

Gepotidacin (GSK2140944) is a triazaacenaphtylene developed by GSK and belongs to the class of Novel Bacterial Topoisomerase Inhibitors (NBTI). This new antibiotic is currently being investigated in three phase 3 clinical trials.

Uses

Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.

Mechanism of action

Gepotidacin's primary mechanism of action involves inhibiting bacterial DNA replication, specifically targeting DNA gyrase (topoisomerase II) and topoisomerase IV. These enzymes are vital for bacterial processes such as replication, transcription, and cell division, as they regulate the topological state of DNA during these activities.

in vivo

GSK2140944 MICs are 0.125 to 0.5 mg/L against the six MRSA isolates. ELF penetration ratios range from 1.1 to 1.4. Observed maximal decreases are 1.1 to 3.1 log10 CFU in neutropenic mice. The mean fAUC/MIC ratios required for stasis and 1-log-unit decreases are 59.3 ± 34.6 and 148.4 ± 83.3, respectively.

References

[1] Farrell DJ, et al. In Vitro Activity of Gepotidacin (GSK2140944) against Neisseria gonorrhoeae. Antimicrob Agents Chemother. 2017 Feb 23;61(3). DOI:10.1128/AAC.02047-16
[2] Biedenbach DJ, et al. In Vitro Activity of Gepotidacin, a Novel Triazaacenaphthylene Bacterial Topoisomerase Inhibitor, against a Broad Spectrum of Bacterial Pathogens. Antimicrob Agents Chemother. 2016 Jan 4;60(3):1918-23. DOI:10.1128/AAC.02820-15
[3] O'Riordan W, et al. Efficacy, Safety, and Tolerability of Gepotidacin (GSK2140944) in the Treatment of Patients with Suspected or Confirmed Gram-Positive Acute Bacterial Skin and Skin Structure Infections. Antimicrob Agents Chemother. 2017 May 24;61(6). DOI:10.1128/AAC.02095-16
[4] So W, et al. Pharmacodynamic Profile of GSK2140944 against Methicillin-Resistant Staphylococcus aureus in a Murine Lung Infection Model. Antimicrob Agents Chemother. 2015 Aug;59(8):4956-61. DOI:10.1128/AAC.00625-15

Gepotidacin Preparation Products And Raw materials

Raw materials

Preparation Products

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Gepotidacin Suppliers

Taizhou Nanfeng Pharmaceutical Research Institute
Tel
nanfengdrug@163.com; 18616377689
Email
nanfengdrug@163.com
Country
China
ProdList
20009
Advantage
58
Shanghai Yunpun industrial Co.,Ltd
Tel
21-61726900 15202122459
Fax
+86-21-60277507
Email
sales@yunpun.com
Country
China
ProdList
494
Advantage
58
Bayee Biotech (Anqing) Co., Ltd.
Tel
0556-5032306 18917961636
Email
wtx@bayeebio.com
Country
China
ProdList
239
Advantage
61
Shanghai Hongboshangyi Pharmaceutical Technology Co. , Ltd.
Tel
15927323052
Email
shenqianyan@prssh.com
Country
China
ProdList
999
Advantage
58
Shanghai Boc Chemical Co.,Ltd
Tel
021-34975603-808 18721111801
Fax
+86-21-34975602-805
Email
sales@bocpharma.com
Country
China
ProdList
1009
Advantage
64
ChemCell Biomedicine Co.,Ltd.
Tel
020-13556033878 2965585218 13556033878
Fax
0086-0757-85406358
Email
chemcell@hotmail.com
Country
China
ProdList
369
Advantage
52
Shenzhen HwaGen Pharmaceutical Co.,Ltd
Tel
17722620669
Fax
0752-5319394
Email
liangcong.yi@rafflespt.com
Country
China
ProdList
279
Advantage
58
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
Advantage
55
Xiamen Halosyntech Co., Ltd
Tel
0592-6688068 18106901346
Fax
0592-6686768
Email
qbl2015@halolife.cn
Country
China
ProdList
127
Advantage
55
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View Lastest Price from Gepotidacin manufacturers

Shanghai Joiny Pharmaceutical Co.,LTD
Product
Gepotidacin 1075236-89-3
Price
US $0.00/kg
Min. Order
1kg
Purity
98%
Supply Ability
1000kg
Release date
2025-11-12
RongNa Biotechnology Co.,Ltd
Product
Gepotidacin 1075236-89-3
Price
US $10.00/ASSAYS
Min. Order
1ASSAYS
Purity
99%
Supply Ability
1 ton
Release date
2025-08-20

1075236-89-3, GepotidacinRelated Search:


  • Gepotidacin
  • Buagafuran
  • GSK-2140944
  • Gepotidacin (GSK2140944)
  • 3H,8H-2a,5,8a-Triazaacenaphthylene-3,8-dione, 2-[[4-[[(3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-yl)methyl]amino]-1-piperidinyl]methyl]-1,2-dihydro-, (2R)-
  • (R)-2-((4-(((3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-yl)methyl)amino)piperidin-1-yl)methyl)-1,2-dihydro-3H,8H-2a,5,8a-triazaacenaphthylene-3,8-dione
  • (R)-2-((4-(((3,4-Dihydro-2H-pyrano[2,3-c]pyridin-6-yl)methyl)amino)piperidin-1-yl)methyl)-1,2-dihydro-3H,8H-2a,5,8a-triazaacenaphthylene-3,8-dione , Gepotidacin
  • 1075236-89-3