ANT-3310 sodium

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ANT-3310 sodium

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CAS NO:	2410688-61-6
规格:	≥98%

包装与价格：

包装	价格(元)
10mg	询价
25mg	询价
50mg	询价
100mg	询价
250mg	询价

ANT-3310 sodium (ANT3310) is a novel and covalent Serine β-Lactamase inhibitor of the diazabicyclooctane class with a broad-spectrum of antibacterial activity. It uses a strained urea moiety as the warhead to react with the active serine residue in the active site of SBLs, and inhibits serine β-Lactamase with IC50 values ranging from 1 nM to 175 nM (a panel of Serine β-Lactamase). ANT-3310 sodium also potentiates activity of β-lactam antibiotics against Carbapenem-Resistant Enterobacterales (CRE) and Acinetobacter baumannii (CRAB).

理化性质和储存条件

Molecular Formula: C6H8FN2NaO5S;

Molecular Weight: 262.19

Synonym: ANT-3310; ANT 3310; ANT3310; ANT-3310 sodium;

Chemical Name: sodium (2R,5R)-2-fluoro-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl sulfate

InChi Key: UIJIKXQAJBMNIR-JBUOLDKXSA-M

InChi Code: InChI=1S/C6H9FN2O5S.Na/c7-5-2-1-4-3-8(5)6(10)9(4)14-15(11,12)13;/h4-5H,1-3H2,(H,11,12,13);/q;+1/p-1/t4-,5+;/m1./s1

SMILES Code: O=C(N1[C@@H](CC[C@@H]2C1)F)N2OS(=O)(O[Na])=O

In Vitro	ANT-3310 sodium (Compound 21, 0.006 to 3 000 nM, 10 min) inhibits a series of Serine β-Lactamase (AmpC, CTX-M-15, TEM-1, OXA-48, OXA-23, and KPC-2), with IC<>50 values ranging from 1 nM to 175 nM[1]. ANT3310 sodium shows a low in vitro cytotoxicity (IC<>50:> 100 μM) in HepG2 cell, cardiotoxicity (inhibition of the hERG potassium ion channel), and genotoxicity (Ames test)[1].
In Vivo	ANT-3310 sodium (intravenous injection, 25-100 mg/kg, at 1, 3, 5, and 7 h postinfection) reduces bacterial burdens in murine thigh infection model[1]. ANT3310 sodium (intravenous injection, 1 mg/kg, Male Swiss albino mice) shows a T1/2 value of 0.64 h, AUC value of 412 ngoh/mL, and Cl value of 40 mL/min/kg (pharmacokinetic assay)[1]. Animal Model: Murine thigh infection model[1] Dosage: 25, 50, and 100 mg/kg Administration: Intravenous injection, at 1, 3, 5, and 7 h postinfection Result: Reduced bacterial burdens (colony forming units, CFU) in a dose-dependent manner to levels below that of the initial starting inoculum at the highest dose, when treated with the combination of MEM.

In Vitro

ANT-3310 sodium (Compound 21, 0.006 to 3 000 nM, 10 min) inhibits a series of Serine β-Lactamase (AmpC, CTX-M-15, TEM-1, OXA-48, OXA-23, and KPC-2), with IC<>50 values ranging from 1 nM to 175 nM[1]. ANT3310 sodium shows a low in vitro cytotoxicity (IC<>50:> 100 μM) in HepG2 cell, cardiotoxicity (inhibition of the hERG potassium ion channel), and genotoxicity (Ames test)[1].

In Vivo

ANT-3310 sodium (intravenous injection, 25-100 mg/kg, at 1, 3, 5, and 7 h postinfection) reduces bacterial burdens in murine thigh infection model[1]. ANT3310 sodium (intravenous injection, 1 mg/kg, Male Swiss albino mice) shows a T1/2 value of 0.64 h, AUC value of 412 ngoh/mL, and Cl value of 40 mL/min/kg (pharmacokinetic assay)[1]. Animal Model: Murine thigh infection model[1] Dosage: 25, 50, and 100 mg/kg Administration: Intravenous injection, at 1, 3, 5, and 7 h postinfection Result: Reduced bacterial burdens (colony forming units, CFU) in a dose-dependent manner to levels below that of the initial starting inoculum at the highest dose, when treated with the combination of MEM.