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  2. Cell Cycle/DNA Damage Anti-infection
  3. Antifolate Bacterial
  4. Diaveridine

Diaveridine  (Synonyms: 二氨藜蘆啶; EGIS-5645)

目錄號(hào): HY-B1902 純度: 99.79%
COA 產(chǎn)品使用指南 技術(shù)支持

Diaveridine (EGIS-5645) 是二氫葉酸還原酶 (DHFR) 的抑制劑，對(duì)于野生型 DHFR 的 Ki 值為 11.5 nM，Diaveridine 也是一種抗菌劑。

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Diaveridine Chemical Structure

Diaveridine Chemical Structure

CAS No. : 5355-16-8

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10 mM * 1 mL in DMSO ￥550
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Other Forms of Diaveridine:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.

IC50 & Target

Ki: 11.5 nM (DHFR) [1]
Bacterial[2]
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 1000 μM
Compound: Diaveridine
Cytotoxicity against human A549 cells after 24 to 48 hrs by fluorescence-based assay
Cytotoxicity against human A549 cells after 24 to 48 hrs by fluorescence-based assay
[PMID: 29784273]
體外研究
(In Vitro)

Diaveridine is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent[1]. Treatments with Diaveridine for 90 min have a strong bactericidal effect on S. typhimurium TA1535, and no bacterial growth is observed at 10μg/mL or more. Without metabolic activation, treatment with Diaveridine for 48 h, but not 24 h, causes a dose-dependent, significant increase in the frequency of aberrant metaphases. At 100 μg/mL, 60% of the metaphases contain chromosome aberrations[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

The sperm abnormality of the Diaveridine (DVD) treatment groups at all dose levels (Diaveridine, 128 to 512 mg/kg) shows no significant differences compare with the negative control group. There are no significant differences of micronucleus between the negative control group and the Diaveridine treatment groups (Diaveridine, 128 to 512 mg/kg). The chromosome aberration of the Diaveridine treatment groups at all dose levels and the negative control group are significantly lower than those in the positive control group treated with cyclophosphamide (P<0.05), indicating that Diaveridine at the doses studied does not cause abnormal chromosome aberration. The results demonstrate that the Diaveridine administration does not produce significant changes in the ratio of organ-to-body weight, compare with the negative control group in the end period of the study[3].

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

260.29

Formula

C13H16N4O2
CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

二氨藜蘆啶
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 33.33 mg/mL (128.05 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.8419 mL 19.2093 mL 38.4187 mL
5 mM 0.7684 mL 3.8419 mL 7.6837 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.60 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.60 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料
參考文獻(xiàn)
Cell Assay
[2]

Cells are cultured at 37°C in a humidified atmosphere of 5% CO2 in air. The growth medium is Eagle’s MEM supplemented with 10% fetal bovine serum. In the experiment without metabolic activation, the cells are treated for 24 or 48 h continuously without a medium change. In the experiment with metabolic activation, the cells are pulse treated with test compounds (including Diaveridine) at varying doses for 6 h and incubated for 18 h in fresh culture medium. Breakage type chromatid aberrations, exchange type chromatid aberrations, breakage type chromosome aberrations, and exchange type chromosome aberrations are scored. Gaps are also counted. Mitotic index is determined from scoring 2000 cells[2].

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

3]Fifty male ICR mice, weighing 25 to 35 g, are assigned to five groups randomly with 10 mice in each group. Mice in the experiment groups receive Diaveridine (DVD) via IG at ed 128 mg/kg (low doses), 256 mg/kg (medium doses), and 512 mg/kg (high doses) body weight for 5 consecutive days, respectively. Mice in negative and positive control groups receive IG 1% CMC-Na solvent and 40 mg/kg body weight of cyclophosphamide, respectively. The testing groups are administered 0.2 mL/10 g Diaveridine (mixed with 1% of CMC-Na, to obtain the concentration of 2 mg/mL.) body weight, once a day, for 5 days. The behavioral changes are recorded on the daily basis[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.8419 mL 19.2093 mL 38.4187 mL 96.0467 mL
5 mM 0.7684 mL 3.8419 mL 7.6837 mL 19.2093 mL
10 mM 0.3842 mL 1.9209 mL 3.8419 mL 9.6047 mL
15 mM 0.2561 mL 1.2806 mL 2.5612 mL 6.4031 mL
20 mM 0.1921 mL 0.9605 mL 1.9209 mL 4.8023 mL
25 mM 0.1537 mL 0.7684 mL 1.5367 mL 3.8419 mL
30 mM 0.1281 mL 0.6403 mL 1.2806 mL 3.2016 mL
40 mM 0.0960 mL 0.4802 mL 0.9605 mL 2.4012 mL
50 mM 0.0768 mL 0.3842 mL 0.7684 mL 1.9209 mL
60 mM 0.0640 mL 0.3202 mL 0.6403 mL 1.6008 mL
80 mM 0.0480 mL 0.2401 mL 0.4802 mL 1.2006 mL
100 mM 0.0384 mL 0.1921 mL 0.3842 mL 0.9605 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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