1. Immunology/Inflammation
  2. CD73
  3. OP-5244 sodium

OP-5244 sodium 是一种有效和具有口服活性的 CD73 抑制剂,IC50 值为 0.25 nM。OP-5244 sodium 通过阻断腺苷的产生来逆转免疫抑制作用,具有进行癌症研究的潜力。

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OP-5244 sodium Chemical Structure

OP-5244 sodium Chemical Structure

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1 mg ¥3400
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5 mg ¥8500
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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

OP-5244 sodium is a potent and orally active inhibitor of CD73, with an IC50 of 0.25 nM. OP-5244 sodium reverses immunosuppression through blocking of adenosine production, and has the potential for the cancer research[1].

IC50 & Target

IC50: 0.25 nM (CD73)[1]

体外研究
(In Vitro)

OP-5244 inhibits the production of adenosine (ADO), with an EC50 of 0.79±0.38 nM in H1568 (NSCLC) cells[1].
OP-5244 inhibits AMP hydrolysis to ADO in peripheral blood derived CD8+ T cells with an EC50 of 0.22 nM[1].
OP-5244 (4.1-1000 nM; 96 h) rescues AMP-suppressed CD8+ T cells proliferation and cytokine production[1].
OP-5244 (0.01 nM-10 μM) inhibits ADO production completely in human and murine cancer cell lines (H1568 and EMT6, respectively)[1].

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

体内研究
(In Vivo)

OP-5244 (15 mg/kg/day; s.c. for 13 d) exhibits anti-tumor effects as a single agent as shown by the tumor growth inhibition in mice[1].
OP-5244 (150 mg/kg; p.o. twice daily for 16 d) increases CD8+ T cells infiltration and reverses immunosuppression in mice[1].
OP-5244 (0.2 mg/kg; i.v.) exhibits terminal elimination half-lives (rat 8.5, dog 0.82, cyno 4.6 h) due to moderate plasma clearance (rat 0.18, dog 1.22, cyno 0.05 L/kg/h) and low steady-state volume of distribution (rat 0.22, dog 0.29, cyno 0.10 L/kg/h)[1].
OP-5244 (10 mg/kg; p.o.) exhibits Cmax (rat 0.82, dog 1.25, cyno 1.72 μM) and AUC (rat 1.96, dog 1.75, cyno 14.2 µM•h) [1].

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

Animal Model: BALB/c mice with breast cancer[1]
Dosage: 15 mg/kg/day
Administration: S.c. for 13 days
Result: Inhibited tumor growth.
Showed a 95% lower ADO/AMP ratio compared to that of the vehicle group.
分子量

559.87

Formula

C19H28ClN5NaO9P

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 and light

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

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 33.33 mg/mL (59.53 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7861 mL 8.9306 mL 17.8613 mL
5 mM 0.3572 mL 1.7861 mL 3.5723 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 and light)。-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。

  • 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

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
纯度 & 产品资料
参考文献

OP-5244 sodium 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 and light)。-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 1 mM 1.7861 mL 8.9306 mL 17.8613 mL 44.6532 mL
5 mM 0.3572 mL 1.7861 mL 3.5723 mL 8.9306 mL
10 mM 0.1786 mL 0.8931 mL 1.7861 mL 4.4653 mL
15 mM 0.1191 mL 0.5954 mL 1.1908 mL 2.9769 mL
20 mM 0.0893 mL 0.4465 mL 0.8931 mL 2.2327 mL
25 mM 0.0714 mL 0.3572 mL 0.7145 mL 1.7861 mL
30 mM 0.0595 mL 0.2977 mL 0.5954 mL 1.4884 mL
40 mM 0.0447 mL 0.2233 mL 0.4465 mL 1.1163 mL
50 mM 0.0357 mL 0.1786 mL 0.3572 mL 0.8931 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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OP-5244 sodium
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