ANT3310

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ANT3310 是一种广谱共价丝氨酸 β-内酰胺酶抑制剂，对 AmpC、CTX-M-15、TEM-1、OXA-48、OXA-23 和 KPC-2 的 IC50 范围为 1 nM 至 175 nM。 ANT3310可用于细菌感染的研究。

ANT3310 is an inhibitor of broad-spectrum covalent Serine β-Lactamase with IC50s ranging from 1 nM to 175 nM for AmpC, CTX-M-15, TEM-1, OXA-48, OXA-23, and KPC-2. ANT3310 can be used in studies about bacterial infection.(In Vitro):ANT3310 shows a low in vitro cytotoxicity (IC50 > 100 μM), cardiotoxicity (inhibition of the hERG potassium ion channel) and genotoxicity in HepG2 cell. ANT3310 (0.006 to 3 000 nM) inhibits a series of Serine β-Lactamase including AmpC, CTX-M-15, TEM-1, OXA-48, OXA-23, and KPC-2, with IC<>50 values ranging from 1 nM to 175 nM.(In Vivo):In male Swiss albino mice, ANT3310 (1 mg/kg; i.v.) shows a T1/2 value of 0.64 h, AUC value of 412 ng?h/mL, and Cl value of 40 mL/min/kg. In the murine thigh infection model, ANT3310 (25, 50 and 100 mg/kg; i.v.) reduces bacterial burdens 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.

ANT3310 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.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).

ANT3310 sodium (intravenous injection, 25-100 mg/kg, at 1, 3, 5, and 7 h postinfection) reduces bacterial burdens in murine thigh infection model.ANT3310 sodium (intravenous injection, 1 mg/kg, Male Swiss albino mice) shows a T1/2 value of 0.64 h, AUC value of 412 ng?h/mL, and Cl value of 40 mL/min/kg (pharmacokinetic assay). Animal Model:Murine thigh infection modelDosage: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.

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GPCR/G Protein

Antibacterial

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2410688-61-6

263.2

C6H9FN2NaO5S

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (953.51 mM)

O(S(=O)(=O)O)N1[C@H]2C[N@@](C1=O)[C@H](F)CC2.[Na]

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(-20℃)

With Ice Pack

≥ 2 years