1. Anti-infection
  2. Beta-lactamase
  3. WCK-4234 free base

WCK-4234 free base 是一种二氮杂双环辛烷类 β-内酰胺酶 (β-lactamase) 抑制剂和药敏恢复剂。WCK-4234 free base 可抑制 A 类、C 类、D 类 β-内酰胺酶以及超广谱 β-内酰胺酶,从而增强 Imipenem (HY-B1369A) 和 Meropenem (HY-13678) 对革兰氏阴性病原体的活性。WCK-4234 free base 无直接抗菌活性,不能增强 Ciprofloxacin (HY-B0356) 的作用,也无法增强 imipenem 或 meropenem 对产金属 β-内酰胺酶菌株的活性。WCK-4234 free base 可用于革兰氏阴性细菌感染以及 β-内酰胺酶介导的碳青霉烯类耐药细菌感染的研究。

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WCK-4234 free base

WCK-4234 free base Chemical Structure

CAS No. : 1706523-58-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

WCK-4234 free base is a diazabicyclooctane β-lactamase inhibitor and susceptibility restorer. WCK-4234 free base inhibits class A, C, D β-lactamases and extended-spectrum β-lactamases to potentiate Imipenem (HY-B1369A) and Meropenem (HY-13678) activity against Gram-negative pathogens. WCK-4234 free base lacks direct antibacterial activity, does not potentiate Ciprofloxacin (HY-B0356), and fails to potentiate imipenem or meropenem against metallo-β-lactamase-producing strains. WCK-4234 free base can be used for the research of gram-negative bacterial infections and β-lactamase-mediated carbapenem-resistant bacterial infections[1][2].

体外研究
(In Vitro)

WCK-4234 (4-8 mg/L) free base 可强效增强亚胺培南和美罗培南对产 KPC、OXA-48 或 OXA-181 碳青霉烯酶,或同时具有 AmpC/超广谱 β-内酰胺酶 (ESBL) 活性与膜通透性降低的临床肠杆菌科分离株的作用,将碳青霉烯类药物的几何平均 MIC 降至≤1 mg/L,但对产金属 β-内酰胺酶 (MBL) 的肠杆菌科菌株无碳青霉烯类药物增强活性[2]
WCK-4234 (4-8 mg/L) free base 可增强亚胺培南和美罗培南对产 AmpC 酶、OprD 缺失及产 OXA-181 酶的铜绿假单胞菌分离株的活性,使碳青霉烯类药物的 MIC50 降低 4 倍或以上,但无法增强碳青霉烯类药物对产 MBL 酶的铜绿假单胞菌的活性[2]
WCK-4234 (4-8 mg/L) free base 可强效增强亚胺培南和美罗培南对产 OXA-23 及高产 OXA-51 的鲍曼不动杆菌分离株的活性,在大多数情况下可使碳青霉烯类药物的几何平均 MIC50 降低 8~40 倍至 ≤2 mg/L,但无法增强碳青霉烯类药物对产 MBL 的鲍曼不动杆菌的活性[2]

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

分子量

247.23

Formula

C7H9N3O5S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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WCK-4234 free base
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HY-125604A
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