2. Anti-infection
  3. Bacterial Penicillin-binding protein (PBP)
  4. VNRX-14079

VNRX-14079 是一种抗菌剂 (Antibacterial) 和 PBP2 抑制剂，对野生型淋病奈瑟菌 PBP2 的 IC50 值为 1.7 μM。VNRX-14079 可与 PBP2 的 Ser310 形成共价键，与 PBP2 的多个残基相互作用，稳定复合物，并在嵌合型 PBP2 中诱导 β3-β4 环向内的构象。VNRX-14079 对耐 Ceftriaxone (HY-B0712) 的淋病奈瑟菌菌株具有抗菌活性。VNRX-14079 可用于淋病的研究。

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VNRX-14079

VNRX-14079 Chemical Structure

CAS No. : 2872654-37-8

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VNRX-14079 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VNRX-14079 is an antibacterial agent and PBP2 inhibitor, with an IC50 value of 1.7 μM against wild-type Neisseria gonorrhoeae PBP2. VNRX-14079 forms a covalent bond with Ser310 of PBP2, interacts with multiple residues of PBP2 to stabilize the complex, and induces an inward conformational change of the β3-β4 loop in chimeric PBP2. VNRX-14079 exhibits antibacterial activity against Ceftriaxone (HY-B0712)-resistant Neisseria gonorrhoeae strains. VNRX-14079 can be used in the research of gonorrhea[1].

体外研究
(In Vitro)

VNRX-14079 结合野生型淋病奈瑟菌 (FA19 菌株) 的 PBP2，其 IC50 为 1.7 µM[1]。
VNRX-14079 可结合来自 H041 菌株的嵌合淋病奈瑟菌 PBP2，其 IC50 为 3.0 µM[1]。
VNRX-14079 (24 h) 对大多数产生非嵌合型和嵌合型 PBP2 的淋病奈瑟菌菌株表现出强效抗菌活性[1]。
VNRX-14079 (4× MIC-16× MIC; 2-24 h) 对淋病奈瑟菌 ATCC 49226、WHO Q 和 H041 表现出快速杀菌活性，在 4× 和 16× MIC 条件下，6 小时内可使细菌数量减少 ≥2 log10，24 小时内降至检测不到的水平[1]。

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

VNRX-14079 相关抗体:
体内研究
(In Vivo)

VNRX-14079 (10-200 mg/kg；皮下注射；每 8 小时至每 24 小时给 1 次) 在小鼠阴道感染模型中对头孢曲松耐受的淋病奈瑟菌 (N. gonorrhoeae) H041 表现出强大的体内抗菌作用[1]。

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

Animal Model: NCI BALB/c (female, 6-7 weeks old, pretreated with 17β oestradiol and antibiotics to suppress commensal microbiota, vaginally infected with ceftriaxone-resistant Neisseria gonorrhoeae H041)[1]
Dosage: 10 mg/kg; 200 mg/kg; 150 mg/kg
Administration: s.c.; q12h (total 2 doses on day 1); q24h (single dose on day 1); q8h (total 3 doses on day 1)
Result: Achieved 80% bacterial clearance by day 4 with statistically significant reduction in culture-positive mice relative to vehicle controls (P < 0.01) at 10 mg/kg q12h.
Achieved 100% clearance by day 3 with predicted 44% free unbound drug concentration above the MIC over 24 hours at 200 mg/kg q24h.
Resulted in 90% clearance by day 2 at 150 mg/kg q12h.
Achieved 100% clearance by day 2 at 150 mg/kg q8h.
Showed reduced average bacterial burden consistent with clearance rates across all doses.
Detected no evolution of spontaneous gonococcal mutants or adverse effects across all doses.
分子量

646.28

Formula

C22H22BF2N4O12PS
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

VNRX-14079 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VNRX-140792872654-37-8VNRX14079VNRX 14079BacterialPenicillin-binding protein (PBP)H041 strainNeisseria gonorrhoeaeβ3-β4 loopmurine vaginal infection modelceftriaxone-resistant Neisseria gonorrhoeaeFA19 straintopoisomerase/gyrase inhibitorsSer310PBP2gonorrhoeaInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-183080
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