[CAS NO. 161715-24-8] Tebipenempivoxil
PRODUCTS SPECIFICATIONS [161715-24-8]
DESCRIPTION [161715-24-8]
Overview
| MDL | MFCD17215369 |
|---|---|
| Molecular Weight | 497.63 |
| Molecular Formula | C22H31N3O6S2 |
| SMILES | O=C(C(N1C2=O)=C(SC3CN(C4=NCCS4)C3)[C@H](C)[C@]1([H])[C@@]2([H])[C@H](O)C)OCOC(C(C)(C)C)=O |
Summary
Tebipenem pivoxil (L084) is an orally active antibiotic against a variety of pathogenic bacteria . Tebipenem pivoxil binds penicillin-binding protein (PBP), thereby inhibiting cell wall synthesis [1] .
In Vitro
Tebipenem pivoxil (0-128 μg/mL; 18–24 h) displays excellent antibacterial activity against a variety of pathogenic bacteria [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | Gram-positive and Gram-negative bacteria |
| Concentration: | 0-128 μg/mL |
| Incubation Time: | 18–24 h |
| Result: | Showed inhibition with MIC 50 s below 64 μg/mL against tested Gram-positive and Gram-negative bacteria. |
In Vivo
Tebipenem pivoxil (L084) (0-4.00 g/kg; p.o.; once) shows minimal lethal dosage (MLD) of 4.00 g/kg and the maximum tolerance dosage (MTD) of 3.40 g/kg in mice
[1]
.
Tebipenem pivoxil (50 and 100 mg/kg; p.o.; once) significantly protects the sepsis mice challenged with various pathogenic bacteria
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | KM mice weighing 18–22 g [1] |
| Dosage: | 2.89, 3.40 and 4.00 g/kg |
| Administration: | Oral administration (tablet), once |
| Result: | Within the 14-day observation period, only one mouse was dead in the maximum oral dosage (4.00 g/kg). The minimal lethal dosage (MLD) was 4.00 g/kg and the maximum tolerance dosage (MTD) in the mice was 3.40 g/kg. Showed dose-dependent liver and kidney damage. |
| Animal Model: | ICR mice, sepsis mouse models [1] |
| Dosage: | 50 and 100 mg/kg |
| Administration: | Oral administration (tablet), once |
| Result: | Significantly increased the survival number of the sepsis mice within a 168 h observation period. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04238195 | Spero Therapeutics|Celerion |
TQT Study
|
January 19, 2020 | Phase 1 |
| NCT04178577 | Spero Therapeutics |
Renal Impairment
|
December 6, 2019 | Phase 1 |
| NCT04919954 | Hartford Hospital|Spero Therapeutics Inc |
Diabetes|Wound Infection|ABSSSI|Healthy Volunteers
|
July 1, 2021 | Phase 1 |
| NCT05121974 | International Centre for Diarrhoeal Disease Research, Bangladesh|University of Washington|GlaxoSmithKline |
Shigellosis
|
August 2022 | Phase 2 |
| NCT04421885 | Spero Therapeutics |
Healthy Volunteers
|
June 1, 2020 | Phase 1 |
| NCT04368585 | Spero Therapeutics |
Healthy Volunteers
|
July 1, 2020 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 200 mg/mL ( 401.91 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0095 mL | 10.0476 mL | 20.0953 mL |
| 5 mM | 0.4019 mL | 2.0095 mL | 4.0191 mL |
| 10 mM | 0.2010 mL | 1.0048 mL | 2.0095 mL |
Synonyms