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Cadazolid
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cadazolid图片
CAS NO:1025097-10-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
ACT-179811
产品介绍
Cadazolid (ACT-179811) 是一种新的恶唑烷酮类抗生素,对Clostridium difficile具有有效的活性。
生物活性

Cadazolid (ACT-179811) is a newoxazolidinoneantibiotic with potent activity againstClostridium difficile.

IC50& Target

Oxazolidinone

 

体外研究
(In Vitro)

Cadazolid is a new antibiotic in development for the treatment ofClostridium difficile-associated diarrhea[1]. Cadazolid is active against all (including linezolid- and moxifloxacin-resistant)Clostridium difficilestrains (MIC900.125, range 0.03-0.25 mg/L). The cadazolid geometric mean MIC is 152-fold, 16-fold, 9-fold and 7-fold lower than those of moxifloxacin, linezolid, metronidazole and vancomycin, respectively. Both cadazolid dosing regimens rapidly reduceClostridium difficileviable counts and cytotoxin with no evidence of recurrence. Cadazolid levels persists at 50-100-fold supra-MIC for 14 days post-dosing. Cadazolid inhibition of enumerated gut microflora is limited, with the exception of bifidobacteria;Bacteroides fragilisgroup andLactobacillus spp.counts are unaffected. There is no evidence for selection of strains resistant to cadazolid, quinolones or linezolid[2].

体内研究
(In Vivo)

Cadazolid is well tolerated up to 3000 mg given twice daily for 10 days. The most common adverse event is headache, with no observed relationship between dose or treatment duration and adverse events. Plasma concentrations of cadazolid are low. No plasma concentrations >3.3 ng/mL are observed after single doses or >6.9 ng/mL after 10 days of multiple doses. Food increased the mean Cmax from 0.73 to 1.87 ng/mL and mean AUC0–t from 3.13 to 15.69 ng·h/mL after a single 300 mg dose. The increase in systemic exposure to cadazolid across doses is less than dose-proportional. The mean cumulative faecal recovery is 81.0%–93.5%. Urinary recovery of unchanged compound is less than 0.015%[1].

Clinical Trial
分子量

585.55

性状

Solid

Formula

C29H29F2N3O8

CAS 号

1025097-10-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(170.78 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.7078 mL8.5390 mL17.0780 mL
5 mM0.3416 mL1.7078 mL3.4156 mL
10 mM0.1708 mL0.8539 mL1.7078 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (4.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.27 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (4.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.27 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。