Gardiquimod diTFA

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Gardiquimod diTFA  纯度: 99.77%

Gardiquimod diTFA,一种咪唑啉类似物,TLR7/8 激动剂。Gardiquimod diTFA 可抑制巨噬细胞和活化外周血单个核细胞 (PBMCs) 的 HIV-1 感染。当浓度低于 10 μM 时,Gardiquimod diTFA 特别激活 TLR7。

Gardiquimod diTFA

Gardiquimod diTFA Chemical Structure

CAS No. : 1159840-61-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥655 In-stock
5 mg ¥550 In-stock
10 mg ¥880 In-stock
25 mg ¥1950 In-stock
50 mg ¥3300 In-stock
100 mg ¥5600 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Gardiquimod diTFA 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Antiviral Compound Library
  • Small Molecule Immuno-Oncology Compound Library
  • Antioxidants Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Pyroptosis Compound Library

生物活性

Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 μM[1][2].

IC50 & Target[1]

TLR7

 

TLR8

 

HIV-1

 

体外研究
(In Vitro)

Gardiquimod diTFA (6-60 μM ) significantly inhibits cDNA synthesis by HIV-1 reverse transcriptase[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Dendritic cells (DCs) in combination with Gardiquimod (1 mg/kg per mouse; i.p.; daily for 7 days) improves the anti-tumor effects of NK cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male athymic nude mice (Balb-nu/nu, 5 weeks old) (bearing human HepG2 liver carcinoma xenografts)[2]
Dosage: 1 mg/kg per mouse
Administration: i.p.; daily for 7 days
Result: Significantly suppressed the growth of human HepG2 liver carcinoma xenografts.

分子量

541.44

Formula

C21H25F6N5O5

CAS 号

1159840-61-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 50 mg/mL (92.35 mM; Need ultrasonic)

H2O : 25 mg/mL (46.17 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8469 mL 9.2346 mL 18.4693 mL
5 mM 0.3694 mL 1.8469 mL 3.6939 mL
10 mM 0.1847 mL 0.9235 mL 1.8469 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 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: PBS

    Solubility: 50 mg/mL (92.35 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.62 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 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.62 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 μL 20% 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
  • 4.

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

    Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.62 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Buitendijk M, et al. Gardiquimod: a Toll-like receptor-7 agonist that inhibits HIV type 1 infection of human macrophages and activated T cells. AIDS Res Hum Retroviruses. 2013 Jun;29(6):907-18.

    [2]. Ma F, et al. The TLR7 agonists imiquimod and gardiquimod improve DC-based immunotherapy for melanoma in mice. Cell Mol Immunol. 2010 Sep;7(5):381-8.

    [3]. Zhou Z, et al. TLR7/8 agonists promote NK-DC cross-talk to enhance NK cell anti-tumor effects in hepatocellular carcinoma. Cancer Lett. 2015 Dec 28;369(2):298-306.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

FTI-2148 diTFA

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

FTI-2148 diTFA 

FTI-2148 diTFA 是 RAS C 末端修饰的法呢基转移酶 (FT-1) 和香叶基转移酶 1 (GGT-1) 的抑制剂,抑制 FT-1 和 GGT-1 的 IC50 分别为 1.4 nM 和 1.7 μM。

FTI-2148 diTFA

FTI-2148 diTFA Chemical Structure

CAS No. : 817586-01-9

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

FTI-2148 diTFA is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively[1].

IC50 & Target

IC50: 1.4 nM (FT-1); 1.7 μM (GGT-1)[1]

体外研究
(In Vitro)

FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells[1].
FTI-2148 diTFA is against P. falciparum PFT, Mammalian PFT and Mammalian PGGT-I with IC50 values of 15 nM; 0.82 nM and 1700 nM, respectively. PFT:protein farnesyltransferase; PGGT-I geranylgeranyltransferase-I[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: KRAS HRAS, and NRAS-transformed NIH3T3 cells 
Concentration: 30 μM
Incubation Time:
Result: Inhibited the prenylation of KRAS and NRAS.

体内研究
(In Vivo)

FTI-2148 (intraperitoneal injection; 25 or 50 mpk/day with a mini-pump; started on day 15 and stopped on day 45 and restarted day 53-83) inhibits the tumor growth by 91% in human lung adenocarcinoma A-549 cells induced mouse model[1].
FTI-2148 (subcutaneous injection; 25 mpk/day with a mini-pump; 14 days) inhibits tumor growth by 77%by the end of the 2-week treatment in Human Xenograft Nude Mouse Model[1].
FTI-2148 (subcutaneous injection; 100 mg/kg/day; 14 days) results in breast tumor regression in a ras transgenic mouse model[3].
FTI-2148 (subcutaneous injection; 100 mg/kg/day; 4 days) results in 85–88% inhibition of FTase with no inhibition of GGTase I enzymatic activity in breast tumors from mice in vivo settings[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Ras transgenic mouse model[3]
Dosage: 100 mg/kg/day
Administration: Subcutaneous injection; 100 mg/kg/day; 14 days
Result: Reduced regression by 87 ± 3% of mammary carcinomas in mice.

分子量

680.62

Formula

C28H30F6N4O7S

CAS 号

817586-01-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
In Vitro: 

Ethanol : 5 mg/mL (7.35 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4692 mL 7.3462 mL 14.6925 mL
5 mM 0.2938 mL 1.4692 mL 2.9385 mL
10 mM

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% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.5 mg/mL (0.73 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.73 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 5.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.5 mg/mL (0.73 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.73 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 5.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 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
  • 3.

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

    Solubility: ≥ 0.5 mg/mL (0.73 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.73 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 5.0 mg/mL 的澄清 EtOH 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Sun J, et al. Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine.Cancer Res. 1999 Oct 1;59(19):4919-26.

    [2]. Carrico D, et al.In vitro and in vivo antimalarial activity of peptidomimetic protein farnesyltransferase inhibitors with improved membrane permeability.Bioorg Med Chem. 2004 Dec 15;12(24):6517-26.

    [3]. 3. Sun J, et al. Geranylgeranyltransferase I inhibitor GGTI-2154 induces breast carcinoma apoptosis and tumor regression in H-Ras transgenic mice.Cancer Res. 2003 Dec 15;63(24):8922-9.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务