DuP 105 1mg

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Qiagen 凯杰 Biosharp Omega

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首页酶、辅酶及抑制剂MCE>

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商品介绍
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DuP 105 是一种可口服的恶唑烷酮类化合物，能够抗葛兰素阳性菌。

Description

DuP 105 is an orally active oxazolidinone, a new class of synthetic antimicrobial agent with activity against gram-positive bacteria.

In Vitro

DuP 105 shows inhibitory activities against staphylococcal isolates and B. fragilis isolates with MIC₉₀s of 4 to 16 μg/mL and 16 μg/mL^[1]. DuP 105 MICs for 50% of the 216 gram-positive isolates tested (MIC₅₀s) range from 4.0 to 16 μg/mL^[2].

In Vivo

DuP 105 administered by either the oral or the parenteral route is protective against staphylococcal and streptococcal infections in mice with the 50% effective doses of 9 to 23 mg/kg^[1].

Solvent & Solubility

In Vitro:

10 mM in DMSO

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.3745 mL	16.8725 mL	33.7450 mL
5 mM	0.6749 mL	3.3745 mL	6.7490 mL
10 mM	0.3375 mL	1.6873 mL	3.3745 mL

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

References

[1]. Slee AM, et al. Oxazolidinones, a new class of synthetic antibacterial agents: in vitro and in vivo activities of DuP 105 and DuP 721. Antimicrob Agents Chemother. 1987 Nov;31(11):1791-7.

[2]. Barry AL, et al. In vitro evaluation of DuP 105 and DuP 721, two new oxazolidinone antimicrobial agents. Antimicrob Agents Chemother. 1988 Jan;32(1):150-2.

Animal Administration ^[1]	The mice are made neutropenic by the intraperitoneal administration of 100 mg of cyclophosphamide per kg on days -5, -3, and 0 (the day of infection). The extent of immunosuppression is assessed by using a standard hematological technique to determine leukocyte counts. In all experiments, the leukocyte count in the cyclophosphamide-treated mice is less than 15% of that in nontreated mice from day 0 through day 7. On day 0, the mice are injected intraperitoneally with a bacterial inoculum suspended in 0.2 mL of saline containing 5% gastric porcine mucin. This inoculum (2×10⁴ CFU) is fivefold that required to kill all the nontreated immunosuppressed mice in 48 h. Graded doses of the test compounds are administered by the subcutaneous or oral route at 1 and 4 h after infection. In parallel with the immunosuppressed mice, groups of nonimmunosuppressed mice are infected, and treated with the antibacterial drugs. The number of survivors on day 7 in each group is used to calculate the ED₅₀ values of the test compounds. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Slee AM, et al. Oxazolidinones, a new class of synthetic antibacterial agents: in vitro and in vivo activities of DuP 105 and DuP 721. Antimicrob Agents Chemother. 1987 Nov;31(11):1791-7. [2]. Barry AL, et al. In vitro evaluation of DuP 105 and DuP 721, two new oxazolidinone antimicrobial agents. Antimicrob Agents Chemother. 1988 Jan;32(1):150-2.

Animal Administration
^[1]

The mice are made neutropenic by the intraperitoneal administration of 100 mg of cyclophosphamide per kg on days -5, -3, and 0 (the day of infection). The extent of immunosuppression is assessed by using a standard hematological technique to determine leukocyte counts. In all experiments, the leukocyte count in the cyclophosphamide-treated mice is less than 15% of that in nontreated mice from day 0 through day 7. On day 0, the mice are injected intraperitoneally with a bacterial inoculum suspended in 0.2 mL of saline containing 5% gastric porcine mucin. This inoculum (2×10⁴ CFU) is fivefold that required to kill all the nontreated immunosuppressed mice in 48 h. Graded doses of the test compounds are administered by the subcutaneous or oral route at 1 and 4 h after infection. In parallel with the immunosuppressed mice, groups of nonimmunosuppressed mice are infected, and treated with the antibacterial drugs. The number of survivors on day 7 in each group is used to calculate the ED₅₀ values of the test compounds.

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

References

[1]. Slee AM, et al. Oxazolidinones, a new class of synthetic antibacterial agents: in vitro and in vivo activities of DuP 105 and DuP 721. Antimicrob Agents Chemother. 1987 Nov;31(11):1791-7.

[2]. Barry AL, et al. In vitro evaluation of DuP 105 and DuP 721, two new oxazolidinone antimicrobial agents. Antimicrob Agents Chemother. 1988 Jan;32(1):150-2.

Molecular Weight	296.34
Formula	C₁₃H₁₆N₂O₄S
CAS No.	96800-41-8
SMILES	CC(NC[C@H]1CN(C2=CC=C(S(C)=O)C=C2)C(O1)=O)=O
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping	Room temperature in continental US; may vary elsewhere