[CAS NO. 80734-02-7]  Lenampicillin hydrochloride

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PRODUCTS SPECIFICATIONS [80734-02-7]

Catalog
HY-100500
Brand
MCE
CAS
80734-02-7

DESCRIPTION [80734-02-7]

Overview

MDL-
Molecular Weight497.95
Molecular FormulaC21H24ClN3O7S
SMILESO=C([C@@H]1N(C2=O)[C@]([C@@H]2NC([C@@H](C3=CC=CC=C3)N)=O)([H])SC1(C)C)OCC(OC4=O)=C(O4)C.Cl

For research use only. We do not sell to patients.

Summary

Lenampicillin hydrochloride (KBT 1585 hydrochloride) is an orally active prodrug of Ampicillin and is an effective beta-lactam antibacterial agent that inhibits bacterial penicillin-binding proteins (transpeptidase). Lenampicillin hydrochloride has improved absorption and decreased side effects compares to Ampicillin and is applied in the investigation of the suppurative skin and soft tissue infection [1] [2] [3] .


IC50 & Target

IC50: bacterial penicillin-binding proteins (transpeptidase)


In Vivo

Lenampicillin hydrochloride (KBT-1585) (oral adminstration; 0-1000 mg/kg) does not lead to death in dogs, and maximum dose of in this acute toxicity study is recorded because of causing emesis [2] .
Lenampicillin hydrochloride (LAPC) are identified for it main metabolites in rat and dogs. The main metabolite in peripheral plasma is 2,3-butanediol in rats and dog, On the other hand, high levels of acetoin is found in portal plasma for early period after dosing of LAPC. These results shows that the biotransformation of promoiety in LAPC to acetoin carried out mainly in intestinal tissues, but acetoin is converted to 2,3-butanediol in liver [3] .

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


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

-20°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)


Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 200.82 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0082 mL 10.0412 mL 20.0823 mL
5 mM 0.4016 mL 2.0082 mL 4.0165 mL
10 mM 0.2008 mL 1.0041 mL 2.0082 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (5.02 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.02 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.02 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, 6-[[(2R)-2-amino-2-phenylacetyl]amino]-3,3-dimethyl-7-oxo-, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester, hydrochloride (1:1), (2S,5R,6R)-
4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, 6-[(aminophenylacetyl)amino]-3,3-dimethyl-7-oxo-, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester, monohydrochloride, [2S-[2α,5α,6β(S*)]]-
4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, 6-[[(2R)-aminophenylacetyl]amino]-3,3-dimethyl-7-oxo-, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester, monohydrochloride, (2S,5R,6R)-
1,3-Dioxole, 4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid deriv.
KB 1585
KBT 1585
Lenampicillin hydrochloride
Takacillin
Varacillin