Daptomycin 纯度:99.42% 50mg

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Daptomycin 纯度:99.42% 50mg

市场价：: 1100.00

促销价：: ¥1100.00

货号：HY-B0108

品牌：MCE

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北京朝阳

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商品介绍
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Daptomycin 是一种脂肽类抗生素，具有体外快速杀除革兰氏阳性细菌的活性。

Description

Daptomycin is a lipopeptide antibiotic with rapid in vitro bactericidal activity against gram-positive organisms.

In Vitro

Daptomycin has excellent in-vitro inhibitory and bactericidal activity against nafcillin-susceptible and resistant staphylococci (MIC₉₀ less than or equal to 0.5 mg/L) and against enterococci (MIC₉₀ less than or equal to 2.0 mg/L). Daptomycin is more active than vancomycin against the majority of isolated tested. With the exception of trimethoprim-sulphamethoxazole, daptomycin is the most active agent in vitro against enterococci, and is the most active against nafcillin-resistant staphylococci. Daptomycin and vancomycin show a marked increase in MIC when the inoculum is increased from 10⁵ to 10⁷ cfu/mL^[1]. Daptomycin is effective within a very narrow range of drug concentrations (from 0.125 to 2.0 tLg/mL) and is more active than other agents tested against S. faecalis^[2]. Daptomycin inhibits the formation of these nucleotide-linked intermediates^[3].

In Vivo

At a dose of 10 mg/kg given twice daily, daptomycin reduces the number of organisms per kidney significantly compared with that in infected untreated controls within 48 h after the initiation of therapy. At 20 mg/kg given once a day, daptomycin is less effective but reduces colony counts significantly after 4 days of therapy, and its activity is comparable to that of vancomycin or vancomycin-gentamicin given twice daily^[2].

Solvent & Solubility

In Vitro:

H₂O : ≥ 66.66 mg/mL (41.13 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.6170 mL	3.0851 mL	6.1703 mL
5 mM	0.1234 mL	0.6170 mL	1.2341 mL
10 mM	0.0617 mL	0.3085 mL	0.6170 mL

* Please refer to the solubility information to select the appropriate solvent.

References

[1]. Benson CA, et al. Comparative in-vitro activity of LY146032 a new peptolide, with vancomycin and eight other agents against gram-positive organisms. J Antimicrob Chemother. 1987 Aug;20(2):191-6.

[2]. Miniter PM, et al. Activity of LY146032 in vitro and in experimental enterococcal pyelonephritis. Antimicrob Agents Chemother. 1987 Aug;31(8):1199-203.

[3]. Allen NE, et al. Inhibition of peptidoglycan biosynthesis in gram-positive bacteria by LY146032. Antimicrob Agents Chemother. 1987 Jul;31(7):1093-9.

Animal Administration ^[2]	Inocula containing 109 CFU/mL are prepared from an 18-h brain heart infusion broth culture. The exact number in each inoculum is subsequently determined by the standard serial 10-fold dilution agar pour plate technique. Animals are challenged intravenously with a 1.0-mL inoculum. This inoculum is known to infect the renal medulla of normal rats. Twenty-four hours later the animals are divided into eight groups and are given either saline only (controls) or antibiotic therapy initiated with Daptomycin at 10 mg/kg (Daptomycin10), Daptomycin at 20 mg/kg (Daptomycin20), Daptomycin10 plus gentamicin at 1.5 mg/kg, vancomycin at 20 mg/kg, vancomycin at 20 mg/kg plus gentamicin at 1.5 mg/kg, ampicillin at 30 mg per rat per injection, and ampicillin at 30 mg per rat plus gentamicin at 1.5 mg/kg. Animals receive Daptomycin20 once daily; all other drugs are administered twice daily. Vancomycin and Daptomycin are given subcutaneously; ampicillin and gentamicin are given intramuscularly. Drugs are administered for up to 13 days. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Benson CA, et al. Comparative in-vitro activity of LY146032 a new peptolide, with vancomycin and eight other agents against gram-positive organisms. J Antimicrob Chemother. 1987 Aug;20(2):191-6. [2]. Miniter PM, et al. Activity of LY146032 in vitro and in experimental enterococcal pyelonephritis. Antimicrob Agents Chemother. 1987 Aug;31(8):1199-203. [3]. Allen NE, et al. Inhibition of peptidoglycan biosynthesis in gram-positive bacteria by LY146032. Antimicrob Agents Chemother. 1987 Jul;31(7):1093-9.

Animal Administration
^[2]

Inocula containing 109 CFU/mL are prepared from an 18-h brain heart infusion broth culture. The exact number in each inoculum is subsequently determined by the standard serial 10-fold dilution agar pour plate technique. Animals are challenged intravenously with a 1.0-mL inoculum. This inoculum is known to infect the renal medulla of normal rats. Twenty-four hours later the animals are divided into eight groups and are given either saline only (controls) or antibiotic therapy initiated with Daptomycin at 10 mg/kg (Daptomycin10), Daptomycin at 20 mg/kg (Daptomycin20), Daptomycin10 plus gentamicin at 1.5 mg/kg, vancomycin at 20 mg/kg, vancomycin at 20 mg/kg plus gentamicin at 1.5 mg/kg, ampicillin at 30 mg per rat per injection, and ampicillin at 30 mg per rat plus gentamicin at 1.5 mg/kg. Animals receive Daptomycin20 once daily; all other drugs are administered twice daily. Vancomycin and Daptomycin are given subcutaneously; ampicillin and gentamicin are given intramuscularly. Drugs are administered for up to 13 days.

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

References

[1]. Benson CA, et al. Comparative in-vitro activity of LY146032 a new peptolide, with vancomycin and eight other agents against gram-positive organisms. J Antimicrob Chemother. 1987 Aug;20(2):191-6.

[2]. Miniter PM, et al. Activity of LY146032 in vitro and in experimental enterococcal pyelonephritis. Antimicrob Agents Chemother. 1987 Aug;31(8):1199-203.

[3]. Allen NE, et al. Inhibition of peptidoglycan biosynthesis in gram-positive bacteria by LY146032. Antimicrob Agents Chemother. 1987 Jul;31(7):1093-9.

Molecular Weight

1620.67

Formula

C₇₂H₁₀₁N₁₇O₂₆

CAS No.

103060-53-3

SMILES

O=C(N[C@H](CC(N)=O)C(N[C@@H](CC(O)=O)C(N[C@H](C(NCC(N[C@H](C(N[C@@](C(N[C@@H](C(N[C@H]1CC(O)=O)=O)C)=O)([H])CC(O)=O)=O)CCCN)=O)=O)[C@H](OC([C@](NC([C@](NC([C@@](NC(CNC1=O)=O)([H])CO)=O)([H])[C@H](C)CC(O)=O)=O)([H])CC(C(C=CC=C2)=C2N)=O)=O)C)=O)=O)[C@@H](NC(CCCCCCCCC)=O)CC3=CNC4=CC=CC=C34

Storage