OP-5244 sodium|西域试剂

OP-5244 sodium,98.28%

产品编号：Bellancom-136978A| 分子式：C₁₉H₂₈ClN₅NaO₉P| 分子量：559.87

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货号	价格	库存与货期
Bellancom-136978A	￥8500.00	杭州北京（现货）
Bellancom-136978A	￥14000.00	杭州北京（现货）
Bellancom-136978A	￥29500.00	杭州北京（现货）

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OP-5244 sodium

产品介绍

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。

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.

体外研究

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

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

体内研究

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.
OP-5244 (150 mg/kg; p.o. twice daily for 16 d) increases CD8⁺ T cells infiltration and reverses immunosuppression in mice.
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).
OP-5244 (10 mg/kg; p.o.) exhibits C_max (rat 0.82, dog 1.25, cyno 1.72 μM) and AUC (rat 1.96, dog 1.75, cyno 14.2 µM•h) .

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

Animal Model:	BALB/c mice with breast cancer
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.

体内研究

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

Animal Model:	BALB/c mice with breast cancer
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (59.53 mM; ultrasonic and warming and heat to 60°C)

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
10 mM	0.1786 mL	0.8931 mL	1.7861 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 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。

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)

参考文献