sodium,(6R,7R)-3-[(5-methyl-1,3,4-thiadiazol-2-yl)sulfanylmethyl]-8-oxo-7-[[2-(tetrazol-1-yl)acetyl]amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate,pentahydrate

Names

[ CAS No. ]:
115850-11-8

[ Name ]:
sodium,(6R,7R)-3-[(5-methyl-1,3,4-thiadiazol-2-yl)sulfanylmethyl]-8-oxo-7-[[2-(tetrazol-1-yl)acetyl]amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate,pentahydrate

[Synonym ]:
UNII-XLJ4VSY381
Cefazolin sodium hydrate (JP16)
5-Thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylicacid,3-[[(5-methyl-1,3,4-thiadiazol-2-yl)thio]methyl]-8-oxo-7-[[2-(1H-tetrazol-1-yl)acetyl]amino]-,sodium salt,hydrate (1:1:5),(6R,7R)

Biological Activity

[Description]:

Cefazolin sodium pentahydrate is a first-generation cephalosporin antibiotic and can be used in varieties of bacterial infections research[1]. Cefazolin sodium pentahydrate has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD)[2].

[Related Catalog]:

Research Areas >> Infection
Research Areas >> Inflammation/Immunology
Research Areas >> Neurological Disease
Signaling Pathways >> Anti-infection >> Bacterial

[In Vitro]

Cefazolin sodium pentahydrate (0-300 μg/ml; 6 or 24 h) has a direct anti-inflammatory effect on C8-B4 cells stimulated by lipopolysaccharide[2]. Cefazolin sodium pentahydrate (0-400 μM; 72 h) treatment inhibits IL-2, IL-4 and IL-15-induced cell proliferation[3]. Cefazolin sodium pentahydrate (0-400 μM; 30 min) treatment inhibits IL-2, IL-4, IL-15 and IL-21-stimulated JAK3 phosphorylation[3]. Cell Viability Assay[2] Cell Line: C8-B4 cells Concentration: 0, 50, 100, 150, 200, 250, or 300 μg/ml Incubation Time: 6 or 24 hours Result: Inhibited the increase of IL-1β at all doses, but inhibited the increase of IL-6 only at 200 μg/ml. Cell Proliferation Assay[3] Cell Line: PBMC, and TF-1 cells Concentration: 0, 100, 200, and 400 μM Incubation Time: 72 hours Result: Reduced IL-2, IL-4 and IL-15-induced cell proliferation, suggested that Cefazolin interferes not only with IL-15Rα, but also with IL-2/IL-15Rβ and/or γc. Western Blot Analysis[3] Cell Line: PBMC, NK-92, and TF-1 cells Concentration: 0, 100, 200, and 400 μM Incubation Time: 30 min Result: Diminished the phosphorylation of JAK3 in response to the cytokine treatment, concluded suppressing signal transduction by γc receptors.

[In Vivo]

Cefazolin sodium pentahydrate (Subcutaneous injection; 300-500 mg/kg; once daily; 5 d) treatment improves learning and memory in mice after surgery[2]. Animal Model: 6- to 8-week-old male CD-1 mice underwent clinical exploratory laparotomy[2] Dosage: 300-500 mg/kg Administration: Subcutaneous injection; 300-500 mg/kg; once daily; 5 days Result: Attenuated learning and memory dysfunction induced by the surgery.

[References]

[1]. R Quintiliani, et al. Cefazolin. Ann Intern Med. 1978 Nov;89(5 Pt 1):650-6.

[2]. Peng Liang, et al. Perioperative use of cefazolin ameliorates postoperative cognitive dysfunction but induces gut inflammation in mice. J Neuroinflammation. 2018 Aug 22;15(1):235.

[3]. Barbara Żyżyńska-Granica, et al. The anti-inflammatory potential of cefazolin as common gamma chain cytokine inhibitor. Sci Rep. 2020 Feb 19;10(1):2886.

Chemical & Physical Properties

[ Molecular Formula ]:
C14H23N8NaO9S3

[ Molecular Weight ]:
566.56500

[ Exact Mass ]:
566.06500

[ PSA ]:
287.40000