セファドロキシル  (Synonyms: Cefadroxil; BL-S 578)

Cefadroxil is an orally active broad-spectrum cephalosporin antibiotic. Cefadroxil inhibits bacterial cell wall synthesis and enhances the expression of glutamate transporter-1. Cefadroxil is dependent on the intestinal peptide transporter PepT1 for small intestinal absorption. Cefadroxil has inhibitory and bactericidal activity against a variety of Gram-positive and Gram-negative bacteria and has analgesic effects on neuropathic pain^{[1][2][3][4][5][6][7]}.

Cefadroxil has similar inhibitory activity against most Gram-positive and Gram-negative bacteria as Cephalexin and Cephradine (HY-B1156), but is twice as active as Cephalexin (HY-B0200) against Streptococcus pyogenes^[2].

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

Cefadroxil (25-200 mg/kg; p.o.) attains peak blood concentrations similar to Cephalexin at 25 and 100 mg/kg^[1].
Cefadroxil (150 mg/kg; p.o.) exerts analgesic effects on mechanical allodynia in rats and mice with spared nerve injury (SNI) model, and also shows analgesic effect on cold pain in mice^[4].
Cefadroxil (0.39-100 mg/kg; p.o.; single dose or three times at 24, 27, and 30 h) is more effective than Cephalexin in the rat streptococcal pneumonia model, with a larger AUC in lung tissue and a longer half-life^[6].

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

363.39

C₁₆H₁₇N₃O₅S

50370-12-2

Solid

White to off-white

O=C(C(N12)=C(C)CS[C@]2([H])[C@H](NC([C@H](N)C3=CC=C(O)C=C3)=O)C1=O)O

Room temperature in continental US; may vary elsewhere.

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. Buck RE, et al. Cefadroxil, a new broad-spectrum cephalosporin. Antimicrob Agents Chemother. 1977 Feb;11(2):324-30.  [Content Brief]

  [2]. Posada MM, et al. Relevance of PepT1 in the intestinal permeability and oral absorption of cefadroxil. Pharm Res. 2013 Apr;30(4):1017-25.  [Content Brief]

  [3]. Hu Y, et al. Species differences in the pharmacokinetics of cefadroxil as determined in wildtype and humanized PepT1 mice. Biochem Pharmacol. 2016 May 1;107:81-90.  [Content Brief]

  [4]. Han CJ, et al. Antinociceptive effects of cefadroxil and ceftriaxone in experimental animal models of pain. Neuro Endocrinol Lett. 2023 Jul 28;44(5):309-320.  [Content Brief]

  [5]. Tan Z, et al. Physiologically Based Pharmacokinetic Modeling of Cefadroxil in Mouse, Rat, and Human to Predict Concentration-Time Profile at Infected Tissue. Front Pharmacol. 2021 Dec 23;12:692741.  [Content Brief]

  [6]. Chisholm DR, et al. Therapeutic efficacy of cefadroxil and cephalexin for pneumonia in a rat test model. Antimicrob Agents Chemother. 1986 Jul;30(1):105-9.  [Content Brief]

  [7]. Chen X, et al. Influence of peptide transporter 2 (PEPT2) on the distribution of cefadroxil in mouse brain: A microdialysis study. Biochem Pharmacol. 2017 May 1;131:89-97.  [Content Brief]