2. Anti-infection Cell Cycle/DNA Damage
  3. Antibiotic Bacterial DNA/RNA Synthesis
  4. Sarecycline

Sarecycline is an orally effective narrow-spectrum tetracycline derivative antibiotic. Sarecycline has anti-inflammatory activity. Sarecycline inhibits the activity of Gram-positive bacteria and several types of keratobacterium acnes. Sarecycline interferes with tRNA accommodation and tethers mRNA to the 70S ribosome. Sarecycline can be used to study moderate to severe acne.

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Sarecycline Chemical Structure

Sarecycline Chemical Structure

CAS No. : 1035654-66-0

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Top Publications Citing Use of Products

    Sarecycline purchased from MedChemExpress. Usage Cited in: Microbiol Spectr. 2022 Dec 8;e0323822.  [Abstract]

    The MIC distributions of Sarecycline against 43 M. fortuitum isolates. The y axis shows the number of strains with each MIC value, with the specific numbers shown above the bars.

    View All Antibiotic Isoform Specific Products:

    View All Isoforms
    Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

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    Description

    Sarecycline is an orally effective narrow-spectrum tetracycline derivative antibiotic. Sarecycline has anti-inflammatory activity. Sarecycline inhibits the activity of Gram-positive bacteria and several types of keratobacterium acnes. Sarecycline interferes with tRNA accommodation and tethers mRNA to the 70S ribosome. Sarecycline can be used to study moderate to severe acne[1][2][3][4][5][6].

    IC50 & Target

    Tetracycline

     

    In Vitro

    Sarecycline inhibits 55 clinical isolates of C. acnes, and the MIC values for Sarecycline ranged from 0.5 to 16  µg/ml; the MIC50 was 0.5 µg/ml, and the MIC90 was 4 µg/ml[1].
    Sarecycline exhibits activity against the macrolide-resistant organisms[1].
    Sarecycline hydrochloride exhibits minimal activity against enteric aerobic Gram-negative bacteria[2].

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

    Sarecycline hydrochloride (0.33-9  mg/kg; i.v.) show potent activity against S. aureus in a murine neutropenic thigh infection model[1].
    Sarecycline can inhibit S. aureus (PD50=0.25 mg/kg), but has no significant effect on E. coli even at the highest dose (>40 mg/kg) in CD-1 mice model of systemic (intraperitoneal) infection[6].
    Sarecycline (1-150mg/kg; Intraperitoneal injection; Single dose) shows anti-inflammatory activity in Sprague Dawley rats model[6].

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

    Animal Model: Carrageenan-induced footpad edema male Sprague Dawley rats model[6]
    Dosage: 1 mg/kg, 5 mg/kg ,10 mg/kg, 25 mg/kg, 50 mg/kg, 75 mg/kg,100 mg/kg, 150 mg/kg
    Administration: Intraperitoneal injection (i.p.); Single dose. Before a subplantar injection of sterile 1 mg/0.1 mL carrageenan solution in the right hind paw.
    Result: Reduced inflammation to 55.7% and 53.1%, respectively, at doses of 75 mg/kg and 100 mg/kg compared to baseline.
    Animal Model: Carrageenan-induced footpad edema male Sprague Dawley rats model[6]
    Dosage: 0.33, 1, 3, or 9 mg/kg
    Administration: Intravenously
    Result: Achieved a 2-log10 reduction in the bacterial burden in the thigh at a dose comparable to that of doxycycline, with ED50s of 8.23 and 8.32 mg/kg, respectively.
    Molecular Weight

    487.50

    Formula

    C24H29N3O8
    CAS No.
    SMILES

    O[C@@](C(O)=C(C(C1=C(C=C2)O)=O)[C@](CC1=C2CN(C)OC)([H])C3)(C(C(C(N)=O)=C4O)=O)[C@]3([H])[C@@H]4N(C)C
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (205.13 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 2.0513 mL 10.2564 mL 20.5128 mL
    5 mM 0.4103 mL 2.0513 mL 4.1026 mL
    View the Complete Stock Solution Preparation Table

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.13 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.13 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0513 mL 10.2564 mL 20.5128 mL 51.2821 mL
    5 mM 0.4103 mL 2.0513 mL 4.1026 mL 10.2564 mL
    10 mM 0.2051 mL 1.0256 mL 2.0513 mL 5.1282 mL
    15 mM 0.1368 mL 0.6838 mL 1.3675 mL 3.4188 mL
    20 mM 0.1026 mL 0.5128 mL 1.0256 mL 2.5641 mL
    25 mM 0.0821 mL 0.4103 mL 0.8205 mL 2.0513 mL
    30 mM 0.0684 mL 0.3419 mL 0.6838 mL 1.7094 mL
    40 mM 0.0513 mL 0.2564 mL 0.5128 mL 1.2821 mL
    50 mM 0.0410 mL 0.2051 mL 0.4103 mL 1.0256 mL
    60 mM 0.0342 mL 0.1709 mL 0.3419 mL 0.8547 mL
    80 mM 0.0256 mL 0.1282 mL 0.2564 mL 0.6410 mL
    100 mM 0.0205 mL 0.1026 mL 0.2051 mL 0.5128 mL
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    Sarecycline Related Classifications

    Keywords:

    Sarecycline1035654-66-0P-005672P005672P 005672AntibioticBacterialDNA/RNA SynthesisAcneInflammationTetracyclinetetracycline-classbacteriaanti-inflammatory70SribosomeInhibitorinhibitorinhibit

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