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  1. Metabolic Enzyme/Protease Anti-infection
  2. Phosphatase Orthopoxvirus
  3. Idoxuridine

Idoxuridine  (Synonyms: 碘苷; 5-Iodo-2′-deoxyuridine; 5-IUdR; IdUrd)

目錄號: HY-B0307 純度: 99.81%
COA 產(chǎn)品使用指南 技術(shù)支持

Idoxuridine (5-Iodo-2′-deoxyuridine, 5-IUdR, IdUrd) 是一種碘化的胸苷類似物,可競爭性抑制磷酸化酶 (phosphorylases)。 Idoxuridine 可以通過抑制 DNA 聚合酶 (DNA polymerase),影響病毒的復(fù)制,從而抑制病毒活性,特別是眼部病毒性感染,包括單純皰疹性角膜炎。Idoxuridine 作用于貓皰疹病毒的 IC50 值為 4.3 μM。Idoxuridine 具有抗正痘病毒活性。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報,我們不為任何個人用途提供產(chǎn)品和服務(wù)

Idoxuridine Chemical Structure

Idoxuridine Chemical Structure

CAS No. : 54-42-2

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10 mM * 1 mL in DMSO ¥231
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500 mg ¥210
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1 g ¥330
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Other Forms of Idoxuridine:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Idoxuridine (5-Iodo-2′-deoxyuridine, 5-IUdR, IdUrd) is an iodinated thymidine analogue that competitively inhibits phosphorylases. Idoxuridine can inhibit viral activity, particularly viral eye infections, including herpes simplex keratitis, by inhibiting DNA polymerase and affecting viral replication. Idoxuridine against feline herpesvirus has the IC50 value of 4.3 μM[1]. Idoxuridine shows anti-orthopoxvirus activity.

IC50 & Target[4]

HSV-1

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 EC50
> 100 μM
Compound: 4; IDU
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 27032331]
HEL CC50
> 50 μg/mL
Compound: IDU
Tested for the cytotoxic concentration, required to reduce cell growth by 50% in human embryonic lung (HEL) cells.
Tested for the cytotoxic concentration, required to reduce cell growth by 50% in human embryonic lung (HEL) cells.
[PMID: 7877148]
HEL IC50
> 50 μg/mL
Compound: IDU
Tested for the inhibitory concentration required to reduce cytomegalovirus (CMV) strain Davis plaque formation by 50%.
Tested for the inhibitory concentration required to reduce cytomegalovirus (CMV) strain Davis plaque formation by 50%.
[PMID: 7877148]
HEL IC50
0.17 μg/mL
Compound: IDU
Tested for the inhibitory concentration required to reduce TK+ Varicella-Zoster virus (TK+ VZV) strain OKA plaque formation by 50%.
Tested for the inhibitory concentration required to reduce TK+ Varicella-Zoster virus (TK+ VZV) strain OKA plaque formation by 50%.
[PMID: 7877148]
HEL IC50
0.4 μg/mL
Compound: IDU
Tested for the 50% inhibitory concentration required to reduce TK+ Varicella-Zoster virus (TK+ VZV) strain YS plaque formation by 50%
Tested for the 50% inhibitory concentration required to reduce TK+ Varicella-Zoster virus (TK+ VZV) strain YS plaque formation by 50%
[PMID: 7877148]
HEL IC50
20 μg/mL
Compound: IDU
Tested for the inhibitory concentration required to reduce cytomegalovirus (CMV) strain AD-169 plaque formation by 50%.
Tested for the inhibitory concentration required to reduce cytomegalovirus (CMV) strain AD-169 plaque formation by 50%.
[PMID: 7877148]
HEL IC50
4 μg/mL
Compound: IDU
Tested for the inhibitory concentration required to reduce thymidine kinase deficient Varicella-Zoster virus (TK- VZV) strain 07/1 plaque formation by 50%.
Tested for the inhibitory concentration required to reduce thymidine kinase deficient Varicella-Zoster virus (TK- VZV) strain 07/1 plaque formation by 50%.
[PMID: 7877148]
HEL IC50
4 μg/mL
Compound: IDU
Tested for the inhibitory concentration required to reduce thymidine kinase deficient Varicella-Zoster virus (TK- VZV) strain YS/R plaque formation by 50%.
Tested for the inhibitory concentration required to reduce thymidine kinase deficient Varicella-Zoster virus (TK- VZV) strain YS/R plaque formation by 50%.
[PMID: 7877148]
HFF CC50
> 260 μM
Compound: 5-iodo-2'-deoxyuridine
Cytotoxicity against HFF cells by neutral red uptake assay
Cytotoxicity against HFF cells by neutral red uptake assay
[PMID: 16821766]
HFF EC50
1.1 μM
Compound: IDU, idoxuridine
Antiviral activity against TK+ Cowpox virus Delta crmA in HFF cells after 48 hrs by beta-galactosidase assay
Antiviral activity against TK+ Cowpox virus Delta crmA in HFF cells after 48 hrs by beta-galactosidase assay
[PMID: 17325220]
HFF EC50
1.8 μM
Compound: IDU, idoxuridine
Antiviral activity against Cowpox virus Brighton in HFF cells after 1 hr by plaque reduction assay
Antiviral activity against Cowpox virus Brighton in HFF cells after 1 hr by plaque reduction assay
[PMID: 17325220]
HFF EC50
2 μM
Compound: 5-iodo-2'-deoxyuridine
Antiviral activity against cowpox virus in HFF cells by plaque reduction assay
Antiviral activity against cowpox virus in HFF cells by plaque reduction assay
[PMID: 16821766]
HFF EC50
5.6 μM
Compound: IDU, idoxuridine
Antiviral activity against Vaccinia virus in HFF cells after 1 hr by plaque reduction assay
Antiviral activity against Vaccinia virus in HFF cells after 1 hr by plaque reduction assay
[PMID: 17325220]
HFF EC50
6 μM
Compound: 5-iodo-2'-deoxyuridine
Antiviral activity against vaccinia virus in HFF cells by plaque reduction assay
Antiviral activity against vaccinia virus in HFF cells by plaque reduction assay
[PMID: 16821766]
HFF EC50
76 μM
Compound: IDU, idoxuridine
Antiviral activity against TK- Cowpox virus TK:GFP lacZ in HFF cells after 48 hrs by beta-galactosidase assay
Antiviral activity against TK- Cowpox virus TK:GFP lacZ in HFF cells after 48 hrs by beta-galactosidase assay
[PMID: 17325220]
Jurkat EC50
79.7 μM
Compound: 4; IDU
Cytotoxicity against human Jurkat cells assessed as reduction in cell viability after 72 hrs by MTS assay
Cytotoxicity against human Jurkat cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 27032331]
L5178Y IC50
4.6 μM
Compound: IdUrd
In vitro growth inhibition of L5178Y-Parental murine leukemia cells by incorporation of [14C]Leu.
In vitro growth inhibition of L5178Y-Parental murine leukemia cells by incorporation of [14C]Leu.
[PMID: 11101356]
L5178Y IC50
5.4 μM
Compound: IdUrd
In vitro growth inhibition of L5178Y-Parental murine leukemia cells by incorporation of [14C]-Thd.
In vitro growth inhibition of L5178Y-Parental murine leukemia cells by incorporation of [14C]-Thd.
[PMID: 11101356]
NC-37 CC50
80 μg/mL
Compound: IDU
Cytotoxic concentration required to inhibit NC-37 cells by 50%
Cytotoxic concentration required to inhibit NC-37 cells by 50%
10.1016/S0960-894X(01)80146-3
PC-3 EC50
> 100 μM
Compound: 4; IDU
Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 27032331]
PRK IC50
0.1 μg/mL
Compound: 5-I-2'-d Urd
Concentration required to reduce HSV-1 induced cytopathogenicity by 50% in primary rabbit kidney (PRK) cells
Concentration required to reduce HSV-1 induced cytopathogenicity by 50% in primary rabbit kidney (PRK) cells
[PMID: 6267280]
PRK IC50
0.2 μg/mL
Compound: 5-I-2'-d Urd
Concentration required to reduce HSV-2 induced cytopathogenicity by 50% in primary rabbit kidney (PRK) cells; 0.2-0.4
Concentration required to reduce HSV-2 induced cytopathogenicity by 50% in primary rabbit kidney (PRK) cells; 0.2-0.4
[PMID: 6267280]
PRK IC50
0.3 μg/mL
Compound: 5-I-2'-d Urd
Concentration required to inhibit incorporation of [1,'2'-3H]dUrd into DNA of primary rabbit kidney (PRK) cells by 50%
Concentration required to inhibit incorporation of [1,'2'-3H]dUrd into DNA of primary rabbit kidney (PRK) cells by 50%
[PMID: 6267280]
PRK IC50
1 μg/mL
Compound: 5-I-2'-d Urd
Concentration required to inhibit incorporation of [Me-3H]-dThd into DNA of primary rabbit kidney (PRK) cells by 50%
Concentration required to inhibit incorporation of [Me-3H]-dThd into DNA of primary rabbit kidney (PRK) cells by 50%
[PMID: 6267280]
PRK IC50
200 μg/mL
Compound: 5-I-2'-d Urd
Concentration required to reduce TK-HSV-1 (B2006) induced cytopathogenicity by 50% in primary rabbit kidney (PRK) cells
Concentration required to reduce TK-HSV-1 (B2006) induced cytopathogenicity by 50% in primary rabbit kidney (PRK) cells
[PMID: 6267280]
Ramos EC50
47.9 μM
Compound: 4; IDU
Cytotoxicity against human Ramos cells assessed as reduction in cell viability after 72 hrs by MTS assay
Cytotoxicity against human Ramos cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 27032331]
U-87MG ATCC EC50
> 100 μM
Compound: 4; IDU
Cytotoxicity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Cytotoxicity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 27032331]
Vero ED50
1.2 μM
Compound: IDU
In vitro antiviral activity by means of plaque-inhibition assay with monolayers of Vero cells infected with the MP strain of herpes simplex virus-1 (HSV-1)
In vitro antiviral activity by means of plaque-inhibition assay with monolayers of Vero cells infected with the MP strain of herpes simplex virus-1 (HSV-1)
[PMID: 6086926]
Vero EC50
11.2 μM
Compound: IUdR
Antiviral activity against Herpes B virus 24105 infected in african green monkey Vero cells assessed as plaque reduction after 36 to 48 hrs
Antiviral activity against Herpes B virus 24105 infected in african green monkey Vero cells assessed as plaque reduction after 36 to 48 hrs
[PMID: 17438061]
Vero EC50
2.8 μM
Compound: IUdR
Antiviral activity against Herpes simplex virus 1 F infected in african green monkey Vero cells assessed as plaque reduction after 36 to 48 hrs
Antiviral activity against Herpes simplex virus 1 F infected in african green monkey Vero cells assessed as plaque reduction after 36 to 48 hrs
[PMID: 17438061]
Vero CC50
6.8 μM
Compound: IUdR
Cytotoxicity against african green monkey Vero cells after 2 days
Cytotoxicity against african green monkey Vero cells after 2 days
[PMID: 17438061]
Vero EC50
8.5 μM
Compound: IUdR
Antiviral activity against Herpes B virus 32425 infected in african green monkey Vero cells assessed as plaque reduction after 36 to 48 hrs
Antiviral activity against Herpes B virus 32425 infected in african green monkey Vero cells assessed as plaque reduction after 36 to 48 hrs
[PMID: 17438061]
體外研究
(In Vitro)

Idoxuridine (2-10 μM,72 小時) 的 IC50 值為 4.3 μM 的抗病毒藥物[1]。

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

Cell Proliferation Assay[1]

Cell Line: Crandell-Reese feline kidney (CRFK) cells
Concentration: 2-10 μM
Incubation Time: 72 hours
Result: Showed the IC50 value of 4.3 μM.

Cell Cytotoxicity Assay[1]

Cell Line: Crandell-Reese feline kidney (CRFK) cells
Concentration: 5-50 μM
Incubation Time: 72 hours
Result: Reduced by 10.8% relatively in CRFK cells.
體內(nèi)研究
(In Vivo)

Idoxuridine (腹腔注射,50 -200 mg/kg,3 次,間隔 3 小時) 可刺激 C3HeB/FeJ 雌性和雄性小鼠和 A/J 雄性小鼠[2]。

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

Animal Model: C3HeB/FeJ female and male mice and A/J male mice, aged 2 to 4 months[2]
Dosage: 50-200 mg/kg
Administration: Intraperitoneal injection, 3 times, 3 hours interval
Result: Stimulated the production of hemolysin plaque-forming cells (HPFC) to sheep red blood cells (SRBC) in the dose range of 50-200 mg/kg.
Clinical Trial
分子量

354.10

Formula

C9H11IN2O5

CAS 號
性狀

固體

顏色

White to off-white

中文名稱

碘苷;碘甙;皰疹凈;碘去氧尿啶;5-碘去氧尿苷;碘脫氧尿苷

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實驗: 

DMSO 中的溶解度 : 125 mg/mL (353.01 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.8241 mL 14.1203 mL 28.2406 mL
5 mM 0.5648 mL 2.8241 mL 5.6481 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗:

請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實驗的工作液,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

    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.87 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 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

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

    Solubility: ≥ 2.08 mg/mL (5.87 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 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。
動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動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。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,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,請謹(jǐn)慎選擇該方案。
請確保第一步儲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

純度: 99.95%

參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(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 2.8241 mL 14.1203 mL 28.2406 mL 70.6015 mL
5 mM 0.5648 mL 2.8241 mL 5.6481 mL 14.1203 mL
10 mM 0.2824 mL 1.4120 mL 2.8241 mL 7.0602 mL
15 mM 0.1883 mL 0.9414 mL 1.8827 mL 4.7068 mL
20 mM 0.1412 mL 0.7060 mL 1.4120 mL 3.5301 mL
25 mM 0.1130 mL 0.5648 mL 1.1296 mL 2.8241 mL
30 mM 0.0941 mL 0.4707 mL 0.9414 mL 2.3534 mL
40 mM 0.0706 mL 0.3530 mL 0.7060 mL 1.7650 mL
50 mM 0.0565 mL 0.2824 mL 0.5648 mL 1.4120 mL
60 mM 0.0471 mL 0.2353 mL 0.4707 mL 1.1767 mL
80 mM 0.0353 mL 0.1765 mL 0.3530 mL 0.8825 mL
100 mM 0.0282 mL 0.1412 mL 0.2824 mL 0.7060 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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產(chǎn)品名稱:
Idoxuridine
目錄號:
HY-B0307
需求量: