2. Anti-infection
  3. Bacterial
  4. MAC-545496

MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA).

For research use only. We do not sell to patients.

MAC-545496 Chemical Structure

MAC-545496 Chemical Structure

CAS No. : 838810-96-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 83 In-stock
Solution
10 mM * 1 mL in DMSO USD 83 In-stock
Solid
1 mg USD 47 In-stock
5 mg USD 75 In-stock
10 mg USD 120 In-stock
25 mg USD 220 In-stock
50 mg USD 350 In-stock
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Based on 1 publication(s) in Google Scholar

MAC-545496 Related Antibodies

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Description

MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA)[1].

IC50 & Target

Glycopeptide-resistance-associated protein R (GraR)[1]
In Vitro

MAC-545496 potently synergizes with Cefuroxime; concentrations as low as 0.03 µg/mL (~75 nM) lowers the β-lactam MIC from 512 to 8 µg/mL against S. aureus USA300. MAC545496 also synergizes with Cefuroxime and Oxacillin against a collection of ten S. aureus clinical isolates. In addition, MAC-545496 potentiates the effect of Cefuroxime against representatives of other circulating MRSA strains such as USA100, USA400 and USA500 to different extents, with the exception of CMRSA4, a USA200/EMRSA16 isolate. MAC-545496 also synergizes with the antimicrobial peptides colistin and polymyxin B[1].
MAC-545496 shows inhibition of mprF expression in a concentration-dependent manner; the IC50 value is 0.0376 µg/mL[1].
MAC-545496 also inhibits the citrateinduced biofilm formation in the wild type in a concentration dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MAC-545496 Related Antibodies
In Vivo

In vivo, MAC-545496 is effective as a monotherapy for MRSA infected Galleria mellonella larvae. MAC-545496 activity is evidenced by increased survival of the drug-treated larvae as compared to infected untreated ones. This corresponded to concentration-dependent killing of S. aureus in the hemolymph of the larvae observed from the CFUs recovered from the hemolymph 200 min after infection. Treatment of S. aureus-infected larvae with MAC-545496 occurred 30min after infection that mimics acquiring bacterial infection before initiating antimicrobial therapy [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

419.89

Formula

C18H18ClN5O3S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC(NC1=NC=C(Cl)C=C1)=S)C2=CC=C(N3CCCCC3)C([N+]([O-])=O)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (595.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3816 mL 11.9079 mL 23.8158 mL
5 mM 0.4763 mL 2.3816 mL 4.7632 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3816 mL 11.9079 mL 23.8158 mL 59.5394 mL
5 mM 0.4763 mL 2.3816 mL 4.7632 mL 11.9079 mL
10 mM 0.2382 mL 1.1908 mL 2.3816 mL 5.9539 mL
15 mM 0.1588 mL 0.7939 mL 1.5877 mL 3.9693 mL
20 mM 0.1191 mL 0.5954 mL 1.1908 mL 2.9770 mL
25 mM 0.0953 mL 0.4763 mL 0.9526 mL 2.3816 mL
30 mM 0.0794 mL 0.3969 mL 0.7939 mL 1.9846 mL
40 mM 0.0595 mL 0.2977 mL 0.5954 mL 1.4885 mL
50 mM 0.0476 mL 0.2382 mL 0.4763 mL 1.1908 mL
60 mM 0.0397 mL 0.1985 mL 0.3969 mL 0.9923 mL
80 mM 0.0298 mL 0.1488 mL 0.2977 mL 0.7442 mL
100 mM 0.0238 mL 0.1191 mL 0.2382 mL 0.5954 mL
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MAC-545496 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MAC-545496838810-96-1MAC545496MAC 545496BacterialAntivirulenceβ-lactamMRSAGraRnanomolarbiofilmsurvivalvirulencemprFS. aureusInhibitorinhibitorinhibit

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