Product Name :
Gepotidacin
Description:
Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.
CAS:
1075236-89-3
Molecular Weight:
448.52
Formula:
C24H28N6O3
Chemical Name:
(3R)-3-(4-[(2H,3H,4H-pyrano[2,3-c]pyridin-6-ylmethyl)amino]piperidin-1-ylmethyl)-1,4,7-triazatricyclo[6.3.1.0⁴,¹²]dodeca-6,8(12),9-triene-5,11-dione
Smiles :
O=C1C=CC2N=CC(=O)N3[C@H](CN4CCC(CC4)NCC4=CC5CCCOC=5C=N4)CN1C3=2
InChiKey:
PZFAZQUREQIODZ-LJQANCHMSA-N
InChi :
InChI=1S/C24H28N6O3/c31-22-4-3-20-24-29(22)15-19(30(24)23(32)13-27-20)14-28-7-5-17(6-8-28)25-11-18-10-16-2-1-9-33-21(16)12-26-18/h3-4,10,12-13,17,19,25H,1-2,5-9,11,14-15H2/t19-/m1/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.|Product information|CAS Number: 1075236-89-3|Molecular Weight: 448.52|Formula: C24H28N6O3|Chemical Name: (3R)-3-(4-[(2H,3H,4H-pyrano[2,3-c]pyridin-6-ylmethyl)amino]piperidin-1-ylmethyl)-1,4,7-triazatricyclo[6.Clopidogrel-related Compound B In Vivo 3.1.0⁴,¹²]dodeca-6,8(12),9-triene-5,11-dione|Smiles: O=C1C=CC2N=CC(=O)N3[C@H](CN4CCC(CC4)NCC4=CC5CCCOC=5C=N4)CN1C3=2|InChiKey: PZFAZQUREQIODZ-LJQANCHMSA-N|InChi: InChI=1S/C24H28N6O3/c31-22-4-3-20-24-29(22)15-19(30(24)23(32)13-27-20)14-28-7-5-17(6-8-28)25-11-18-10-16-2-1-9-33-21(16)12-26-18/h3-4,10,12-13,17,19,25H,1-2,5-9,11,14-15H2/t19-/m1/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 7.14 mg/mL (15.92 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.Bexotegrast TGF-beta/Smad |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:32798356 |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|Gepotidacin is a novel, first-in-class, triazaacenaphthylene antibacterial that inhibits bacterial DNA gyrase and topoisomerase IV via a unique mechanism and has demonstrated in vitro activity against gram-negative and gram-positive bacterias , including drug-resistant strains, and also targets pathogens associated with other conventional and biothreat infections. The MIC50 and MIC90 for gepotidacin against the 25 N. gonorrhoeae isolates tested are 0.12 and 0.25 μg/mL, respectively. The gepotidacin MIC90s are as follows (in μg/mL): Streptococcus pyogenes, 0.25; Escherichia coli, 2; Moraxella catarrhalis, ≤0.06; Streptococcus pneumoniae, 0.25; Haemophilus influenzae, 1; Clostridium perfringens, 0.5; and Shigella spp., 1. Gepotidacin hasin vitroactivity against causative pathogens of acute bacterial skin and skin structure infections (ABSSSIs).|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.|Products are for research use only. Not for human use.|
