Demeclocycline

SKU: orb2901642

Description

Demeclocycline is an orally active tetracycline antibiotic. Demeclocycline impairs protein synthesis by binding to the 30S ribosomal subunit to inhibit binding of aminoacyl tRNA. Demeclocycline shows anti-bacterial activitise to a wide variety of bacterial infections.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 127-33-3
• MW: 464.85
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₁ClN₂O₈
• SMILES: [H][C@]12C[C@@]3([H])[C@H](N(C)C)C(O)=C(C(N)=O)C(=O)[C@@]3(O)C(O)=C1C(=O)c1c(O)ccc(Cl)c1[C@H]2O
• Target: Antibacterial
• Solubility: In Vitro: H2O : 40 mg/mL (86.05 mM; Ultrasonic) DMSO : 25 mg/mL (53.78 mM; Ultrasonic )

Bioactivity

• In Vivo:
  Demeclocycline (Intraperitoneal injection; 40 mg/kg; once daily; 48 h) treatment results in a significant reduction of hyponatremia and a significant correction of the hypoosmolality, and is not nephrotoxic. Animal model: Male Wistar rats induced with hyponatremia. Dosage: 40 mg/kg. Administration: Intraperitoneal injection; 40 mg/kg; once daily; 48 hours. Result: Increased urine volume, decreased urine osmolality, and caused a significantly increased fractional excretion of water. Animal model: Male Wistar rats induced with hyponatremia. Dosage: 40 mg/kg. Administration: Intraperitoneal injection; 40 mg/kg; once daily; 48 hours. Result: Indicated the effect in the renal inner medulla for AQP2 and AC5/6 specifically, and not secondary toxicity effect.
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• In Vitro:
  Demeclocycline (0-100 μM; 24 h) treatment reduces AQP2 abundance in mpkCCD cells. Demeclocycline (10 μM; 24 h) treatment promotes the activity of monocytes and macrophages. Demeclocycline (1-10 μM; 72 h) treatment directly affects the growth of brain tumorinitiating cells. Western blot analysis. Cell line: MpkCCD cells. Concentration: 0-100 μM. Incubation time: 24 hours. Result: Decreased AQP2 abundance in mpkCCD cells, with significant effects at 50 μM. Cell Viability Assay Cell line: mouse bone marrow derived macrophages and monocytes. Concentration: 10 μM. Incubation time: 24 hours. Result: Enhanced TNF-α production and modulated monocyte functions. Cell Viability Assay Cell line: brain tumorinitiating cells. Concentration: 1, 5, and 10 μM. Incubation time: 72 hours. Result: Inhibited cells growth in two ways: using monocytes as an intermediary, and directly by affecting the proliferation and sphere-forming capacity of brain tumorinitiating cells.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Antibacterial