VNRX-14079
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2872654-37-8
- 分子式: C22H22BF2N4O12PS
- 分子量:646.28
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
VNRX-14079 binds to PBP2 of wild-type *Neisseria gonorrhoeae* (strain FA19) with an IC50 of 1.7 µM[1].
VNRX-14079 binds to chimeric Neisseria gonorrhoeae PBP2 from strain H041, with an IC50 of 3.0 µM[1].
VNRX-14079 (24 h) exhibits potent antibacterial activity against most Neisseria gonorrhoeae strains producing non-mosaic and mosaic PBP2[1].
VNRX-14079 (4× MIC-16× MIC; 2-24 h) exhibits rapid bactericidal activity against *Neisseria gonorrhoeae* ATCC 49226, WHO Q and H041. At 4× and 16× MIC, it reduces bacterial counts by ≥2 log10 within 6 hours and lowers them to undetectable levels within 24 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:10 mg/kg; 200 mg/kg; 150 mg/kg
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Administration:s.c.; q12h (total 2 doses on day 1); q24h (single dose on day 1); q8h (total 3 doses on day 1)
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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.
化学情報
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CAS 番号 2872654-37-8
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分子量 646.28
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分子式 C22H22BF2N4O12PS
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SMILES
O=C(O)C1=C(F)C=CC(C2)=C1OB(O)[C@H]2NC([C@H](NC(N3C(N(S(=O)(C)=O)CC3)=O)=O)C4=CC=C(P(O)(O)=O)C(F)=C4)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
VNRX-14079 関連分類
HY-183080 関連分類
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