NAB815
NAB815 is a specific inhibitor of the Stx2a (Kd = 0.01 μM)/TLR4 interaction. NAB815 inhibits the neutrophil/Stx2a interaction (IC50 = 0.057 μg/mL). NAB815 inhibits the formation of Stx2-containing extracellular vesicles (EVs) produced by leukocytes and platelets and reduces their toxic effects in cellular (Vero cells) and animal models (CD-1 mice). NAB815 reduces bacterial loads in the kidneys, urine, and bladders of Escherichia coli-infected mice. NAB815 is useful in the study of hemolytic uremic syndrome (HUS).
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- CAS No.: 1969250-99-4
- 화학식: C55H94N14O14
- 분자량:1175.42
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보관:
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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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
NAB815 (1 nM, 4 h) inhibits the formation of white blood cell/platelet aggregates by Stx2a[1].
NAB815 (0.01-0.1 μg/mL, 4 h) slightly affects the viability of human leukocytes but has no effect on erythrocytes, inhibits the formation of platelet-derived and leukocyte-derived pathogenic EVs containing Stx2a, impairs the recruitment of complement factors in Stx2-induced EVs[1].
NAB815 (0.01 μg/mL) affords protection against toxicity induced by Stx2a-triggered EVs in Vero cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NAB815 (0.01 μg/mL, 300 μL, i.v., once) affords protection against EV-associated Stx2a in Human EVs CD-1 mice[1].
NAB815 (0.5-2 mg/L, 0.2 mL, s.c., twice a day, 3 days) reduces the bacterial burden in the kidney, urine and bladder in E. coli-infected female OF-1 mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 mice(6-7 weeks old 21-26 g, female) intoxicated with Stx2a (10 and 15 pg/g) [1]
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Dosage:0.01 μg/mL, 100 μL
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Administration:i.v., once
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Result:Improved survival rate without changing body weight, decreased intestinal damage.
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Animal Model:Human EVs (10,400-20,800 g) CD-1 mice (6-7 weeks old 21-26 g, female) intoxicated with Stx2a (10 and 15 pg/g)[1]
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Dosage:0.01 μg/mL, 300 μL
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Administration:i.v., once
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Result:Decreased serum creatinine and a significant rise in serum urea, number of cells with acute tubular injuries (ATIs).
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Animal Model:E. coli-infected (5 × 108) female OF-1 mice (27-33 g)[2]
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Dosage:0.5, 2, 2 mg/L, 0.2 mL
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Administration:s.c., twice a day, 3 days
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Result:Reduced CFU levels.
Chemical Information
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CAS No. 1969250-99-4
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분자량 1175.42
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화학식 C55H94N14O14
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SMILES
O=C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@](C(NCC[C@@H](C(N[C@H](C(N1)=O)CCN)=O)NC([C@@H]([C@@H](O)C)NC([C@H]([C@H](O)C)NC([C@H](CCN)NC(CCCCCCC)=O)=O)=O)=O)=O)([H])[C@H](O)C)=O)CCN)=O)CC)=O)CC(C)C)[C@H]1CC2=CC=CC=C2
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Sequence
Octanoic-{Dab}-Thr-{d-Thr}-{Dab}-{Dab}-{d-Phe}-Leu-{Abu}-{Dab}-Thr (lactam bridge: Dab4-Thr10)
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Sequence Shortening
Octanoic-{Dab}-T-{d-Thr}-{Dab}-{Dab}-{d-Phe}-L-{Abu}-{Dab}-T (lactam bridge: Dab4-Thr10)
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Varrone E, et al. An antibiotic derivative as a new potential tool in the prevention of hemolytic uremic syndrome. iScience. 2025 Jul 7;28(8):113076. [Content Brief]
[2]. Vaara M, et al. Polymyxin derivatives NAB739 and NAB815 are more effective than polymyxin B in murine Escherichia coli pyelonephritis. J Antimicrob Chemother. 2018 Feb 1;73(2):452-455. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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