cefsulodin ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antibiotics, cefalosporanic acid derivatives 558 62587-73-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cefsulodin monosodium
  • cefsulodin
  • cefsulodin sodium
  • cefsulodin sodium salt
A pyridinium-substituted semisynthetic, broad-spectrum antibacterial used especially for Pseudomonas infections in debilitated patients.
  • Molecular weight: 532.54
  • Formula: C22H20N4O8S2
  • CLOGP: -8.90
  • LIPINSKI: 2
  • HAC: 12
  • HDO: 3
  • TPSA: 190.88
  • ALOGS: -4.50
  • ROTB: 8

Drug dosage:

DoseUnitRoute
4 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 50 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 60 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 187.77 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 0.29 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.96 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.64 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1981 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J01DD03 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
OTHER BETA-LACTAM ANTIBACTERIALS
Third-generation cephalosporins
CHEBI has role CHEBI:36047 antibacterial drugs
MeSH PA D000900 Anti-Bacterial Agents
MeSH PA D000890 Anti-Infective Agents

Drug Use (View source of the data)

None




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 0.17 acidic
pKa2 2.83 acidic
pKa3 12.0 acidic
pKa4 12.33 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-adrenergic receptor kinase 1 Kinase EC50 7.15 CHEMBL
Tyrosine-protein phosphatase non-receptor type 11 Enzyme IC50 4.77 CHEMBL
Lethal(3)malignant brain tumor-like protein 1 Unclassified IC50 7.01 CHEMBL
Protein-tyrosine phosphatase 1C Enzyme IC50 4.68 CHEMBL
Penicillin-binding protein 1A Enzyme IC50 6.52 WOMBAT-PK
Penicillin-binding protein 1B Enzyme IC50 5.33 WOMBAT-PK
tRNA 2'-phosphotransferase Unclassified IC50 5.77 CHEMBL

External reference:

IDSource
N0000166876 NUI
D02005 KEGG_DRUG
2190 RXNORM
C0007558 UMLSCUI
CHEBI:3507 CHEBI
CHEMBL3351077 ChEMBL_ID
CHEMBL1617285 ChEMBL_ID
D002441 MESH_DESCRIPTOR_UI
DB13499 DRUGBANK_ID
10783 IUPHAR_LIGAND_ID
4390 INN_ID
52152-93-9 SECONDARY_CAS_RN
OV42LHE42B UNII
656575 PUBCHEM_CID
003801 NDDF
003802 NDDF
387537000 SNOMEDCT_US
96053001 SNOMEDCT_US
CHEMBL1590946 ChEMBL_ID
CHEMBL1343544 ChEMBL_ID
3LU PDB_CHEM_ID

Pharmaceutical products:

None