LED209 |
| Catalog No.GC16931 |
LED209 est un puissant inhibiteur À petite molécule du récepteur bactérien QseC, est un promédicament puissant hautement sélectif pour QseC.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 245342-14-7
Sample solution is provided at 25 µL, 10mM.
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Description:
IC50: <10 μM
Many bacterial pathogens rely on a conserved membrane histidine sensor kinase, QseC, to respond to host adrenergic signaling molecules and bacterial signals in order to promote the expression of virulence factors. LED209 is a potent prodrug that is highly selective for QseC.
In vitro: LED209-mediated inhibition of virulence gene expression inhibited the secretion of EspA and EspB, two proteins encoded within the locus of enterocyte effacement that are required for Escherichia coli (EHEC) to translocate bacterial proteins into host cells and cause attaching-effacing (AE) lesions. At 5 pM, LED209 abolished EHEC AE lesion formation on cultured epithelial cells. Unlike conventional antibiotics, LED209 does not kill or hinder EHEC growth or trigger the EHEC SOS response [1].
In vivo: LED209 [20 mg per kilogram of body weight (mg/kg)] was given orally to mice 3 hours before and 3 hours after intraperitoneal injection of a lethal dose of S. typhimurium. Twenty-four hours after infection, only 30% of untreated mice remained alive, whereas 80% of the LED209-treated mice were still alive. All the S. typhimurium– infected mice died within 72 hours of infection, and 20% of LED209-treated mice survived up to 12 days [1].
Clinical trial: Up to now, LED209 is still in the preclinical development stage.
Reference:
[1] Rasko DA, Moreira CG, Li de R, Reading NC, Ritchie JM, Waldor MK, Williams N, Taussig R, Wei S, Roth M, Hughes DT, Huntley JF, Fina MW, Falck JR, Sperandio V. Targeting QseC signaling and virulence for antibiotic development. Science. 2008 Aug 22;321(5892):1078-80.
| Cas No. | 245342-14-7 | SDF | |
| Chemical Name | (Z)-N'-phenyl-N-(4-(N-phenylsulfamoyl)phenyl)carbamimidothioic acid | ||
| Canonical SMILES | O=S(C1=CC=C(N/C(S)=N/C2=CC=CC=C2)C=C1)(NC3=CC=CC=C3)=O | ||
| Formula | C19H17N3O2S2 | M.Wt | 383.49 |
| Solubility | <3.83 mg/mL in DMSO, <2.33 mg/mL in EtOH, <2.38 mg/mL in Water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6076 mL | 13.0381 mL | 26.0763 mL |
| 5 mM | 0.5215 mL | 2.6076 mL | 5.2153 mL |
| 10 mM | 0.2608 mL | 1.3038 mL | 2.6076 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)
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