For research use only. Not for therapeutic Use.
Ceftobiprole medocaril (BAL5788) sodium is the parenteral proagent of Ceftobiprole (HY-112579). Ceftobiprole is a parenteral pyrrolidinone cephalosporin. Ceftobiprole is a broad-spectrum cephalosporin with high levels of in vitro activity against methicillin- (MRSA) and vancomycin-resistant staphylococci (VRSA) and penicillin-resistant streptococci. Ceftobiprole also inhibits gram-positive and gram-negative pathogens[1][2].
Ceftobiprole medocaril (s.c.; 3 × q12h; total daily doses of BAL9141 equivalents, 2.1, 4.2, or 8.4 mg/kg) causes ten-day cumulative survival rates ranged from 57 to 100% for female Swiss albino mice (body weight, 20 to 22 g) infected Penr Cros Ctxs strain P-15986[1].
Ceftobiprole medocaril (10, 40, 160 mg/kg; single dose; sc) has T1/2s from 20 min to 31 min, as the dose rose from 40 mg/kg to 160 mg/kg. The AUC/dose values for the escalating single doses ranges from 0.585 to 1.33, and the Cmax/dose values decreases from 1.08 to 0.90 in neutropenic thigh-infected mice[2].
| Catalog Number | I024349 |
| CAS Number | 252188-71-9 |
| Synonyms | sodium;(6R,7R)-7-[[(2Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-hydroxyiminoacetyl]amino]-3-[(E)-[1-[(3R)-1-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methoxycarbonyl]pyrrolidin-3-yl]-2-oxopyrrolidin-3-ylidene]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate |
| Molecular Formula | C26H25N8NaO11S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C26H26N8O11S2.Na/c1-10-14(45-26(41)44-10)8-43-25(40)32-4-3-13(7-32)33-5-2-11(20(33)36)6-12-9-46-22-16(21(37)34(22)17(12)23(38)39)28-19(35)15(30-42)18-29-24(27)47-31-18;/h6,13,16,22,42H,2-5,7-9H2,1H3,(H,28,35)(H,38,39)(H2,27,29,31);/q;+1/p-1/b11-6+,30-15-;/t13-,16-,22-;/m1./s1 |
| InChIKey | MFAWUGGPPMTWPU-LCJFHXTKSA-M |
| SMILES | CC1=C(OC(=O)O1)COC(=O)N2CCC(C2)N3CCC(=CC4=C(N5C(C(C5=O)NC(=O)C(=NO)C6=NSC(=N6)N)SC4)C(=O)[O-])C3=O.[Na+] |
| Reference | [1]. E Azoulay-Dupuis, et al. Efficacy of BAL5788, a prodrug of cephalosporin BAL9141, in a mouse model of acute pneumococcal pneumonia. Antimicrob Agents Chemother. 2004 Apr;48(4):1105-11. [2]. W A Craig, et al. In vivo pharmacodynamics of ceftobiprole against multiple bacterial pathogens in murine thigh and lung infection models. Antimicrob Agents Chemother. 2008 Oct;52(10):3492-6. |
