1. GPCR/G Protein Immunology/Inflammation Anti-infection
  2. CXCR HIV
  3. IT1t dihydrochloride

IT1t dihydrochloride 

目录号: HY-101458A 纯度: 99.89%
COA 产品使用指南

IT1t dihydrochloride是高效的CXCR4拮抗剂;抑制CXCL12/CXCR4相互作用的IC50值为2.1 nM。

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IT1t dihydrochloride Chemical Structure

IT1t dihydrochloride Chemical Structure

CAS No. : 1092776-63-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥935
In-stock
1 mg ¥386
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5 mg ¥850
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10 mg ¥1500
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25 mg ¥3000
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50 mg ¥5400
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100 mg ¥9400
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200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of IT1t dihydrochloride:

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.

IC50 & Target

CXCL12/CXCR4

2.1 nM (IC50)

HIV-1 (X4)

14.2 nM (IC50, in MT-4 cells)

HIV-1 (X4)

19 nM (IC50, in PBMCs)

体外研究
(In Vitro)

The CXCR4 is involved in chemotaxis and serves as a coreceptor for T-tropic HIV-1 viral entry and in cancer metastasis. IT1t is a small, drug-like, isothiourea derivative. IT1t shows very potent and dose-dependent inhibition of the CXCL12/CXCR4 interaction with an IC50 of 2.1 nM. This calcium flux is also inhibited by IT1t with an IC50 of 23.1[1]. Strong electron density is observed for IT1t in the binding cavity of both subunits of the CXCR4 homodimer. In dimers of CXCR4 bound to IT1t, the monomers interact only at the extracellular side of helices V and VI, leaving at least a 4 Å gap between the intracellular regions, which is presumably filled by lipids. The IT1t compound and CVX15 peptide have both been characterized as competitive inhibitors of CXCL12, and many of the receptor-ligand contacts in the co-crystal structures presented are important for CXCL12 binding, including the acidic Asp187, Glu2887.39 and Asp972.63. The binding site of IT1t may point to the major anchor region for this domain[2].

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

体内研究
(In Vivo)

IT1t reduces the formation of TNBC early metastases in the zebrafish xenograft model. Tumor cell invasion at the metastatic site is effectively reduced upon CXCR4 silencing (Fig. 7B), similar to the antagonist IT1t [3].

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

分子量

479.57

Formula

C21H36Cl2N4S2

CAS 号
性状

固体

颜色

White to off-white

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: 

H2O 中的溶解度 : 50 mg/mL (104.26 mM; 超声助溶)

DMSO 中的溶解度 : ≥ 30 mg/mL (62.56 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0852 mL 10.4260 mL 20.8520 mL
5 mM 0.4170 mL 2.0852 mL 4.1704 mL
查看完整储备液配制表

* 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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

  • 方案 一

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

    Solubility: ≥ 1.67 mg/mL (3.48 mM); 澄清溶液

    此方案可获得 ≥ 1.67 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

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

    Solubility: ≥ 1.67 mg/mL (3.48 mM); 澄清溶液

    此方案可获得 ≥ 1.67 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 16.7 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。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (208.52 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献
Cell Assay
[1]

Jurkat cells are incubated with serial dilutions (0.001, 0.01, 0.1, 1, 10, 100, 1000 μM) of IT1t at room temperature for two hours. Cytotoxicity of IT1t is also evaluated at 37°C over a longer period of time in MT-4 cells and PHA-stimulated PBMCs (ten day incubation) because these cell types are used in anti-HIV activity assays which last up to ten days. Cytotoxicity is evaluated microscopically and viability is assessed using the a kit[1].

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

参考文献

IT1t dihydrochloride 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.0852 mL 10.4260 mL 20.8520 mL 52.1300 mL
5 mM 0.4170 mL 2.0852 mL 4.1704 mL 10.4260 mL
10 mM 0.2085 mL 1.0426 mL 2.0852 mL 5.2130 mL
15 mM 0.1390 mL 0.6951 mL 1.3901 mL 3.4753 mL
20 mM 0.1043 mL 0.5213 mL 1.0426 mL 2.6065 mL
25 mM 0.0834 mL 0.4170 mL 0.8341 mL 2.0852 mL
30 mM 0.0695 mL 0.3475 mL 0.6951 mL 1.7377 mL
40 mM 0.0521 mL 0.2607 mL 0.5213 mL 1.3033 mL
50 mM 0.0417 mL 0.2085 mL 0.4170 mL 1.0426 mL
60 mM 0.0348 mL 0.1738 mL 0.3475 mL 0.8688 mL
H2O 80 mM 0.0261 mL 0.1303 mL 0.2607 mL 0.6516 mL
100 mM 0.0209 mL 0.1043 mL 0.2085 mL 0.5213 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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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产品名称:
IT1t dihydrochloride
目录号:
HY-101458A
需求量: