SPHINX31,99.12%

产品编号:Bellancom-117661| CAS NO:1818389-84-2| 分子式:C27H24F3N5O2| 分子量:507.51

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-117661
900.00 杭州 北京(现货)
Bellancom-117661
1200.00 杭州 北京(现货)
Bellancom-117661
3500.00 杭州 北京(现货)
Bellancom-117661
5500.00 杭州 北京(现货)

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SPHINX31

产品介绍 SPHINX31 是一种有效的、丝氨酸/富含精氨酸的蛋白激酶1 (SRPK1) 的选择性抑制剂,其IC50 值为 5.9 nM。SPHINX31 能够抑制富丝氨酸/精氨酸剪接因子 1 (SRSF1) 的磷酸化。SPHINX31 还能降低促血管生成基因 VEGF-A165a 亚型的 mRNA 表达。SPHINX31 可用于研究新生血管性眼病。
生物活性

SPHINX31 is a potent and selective SRPK1 inhibitor, with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 also decreases the mRNA expression of pro-angiogenic VEGF-A165a isoform. SPHINX31 can be used to research neovascular eye disease.

体外研究

SPHINX31 (0.3-10 μM; 24 h) significantly down-regulates the expression of VEGF-A165a mRNA.
SPHINX31 (0.3 μM; 24 h) suppresses SRSF1 phosphorylation and nuclear localization.
SPHINX31 (0.3-10 μM; 24 h) decreases pre-tube formation and the rate of migration for human umbilical vein endothelial cells (HUVECs).

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

RT-PCR

Cell Line: HuCCA-1 cells
Concentration: 0.3, 1, 3 and 10 μM
Incubation Time: 24 h
Result: Significantly down-regulated about 60% of the expression of VEGF-A165a mRNA compared with the control cells.

Immunofluorescence

Cell Line: HuCCA-1 cells
Concentration: 0.3 μM
Incubation Time: 24 h
Result: Suppressed SRSF1 phosphorylation and nuclear localization, which thereby induced less expression of pro-angiogenic VEGF-A165a in HuCCA-1 cells.

Cell Migration Assay

Cell Line: HuCCA-1 cells
Concentration: 0.3, 1, 3 and 10 μM
Incubation Time: 24 h
Result: Decreased pre-tube formation of the cells network area to about 50% of the control group.
Decreased the rate of migration for HUVECs.
体内研究
(In Vivo)

SPHINX31 (200 μg/mL; twice daily topical eye drops) protects the retinal endothelial permeability barrier from diabetes-associated loss of integrity.

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

Animal Model: Norway Brown rats (intraperitoneally injected with 50 mg/kg Streptozotocin (HY-10219) to induce type I diabetes)
Dosage: 200 μg/mL
Administration: Twice daily topical eye drops
Result: Reduced retinal permeability in the diabetics (7.92 ± 1.65 × 10-4 cms-1) less than before induction of diabetes (8.15 ± 2.33 × 10-4 cms-1), and less than the control group (8.85 ± 1.29 × 10-4 cms-1), while the diabetes group was 12.67 ± 1.09 × 10-4 cms-1.
体内研究

SPHINX31 (200 μg/mL; twice daily topical eye drops) protects the retinal endothelial permeability barrier from diabetes-associated loss of integrity.

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

Animal Model: Norway Brown rats (intraperitoneally injected with 50 mg/kg Streptozotocin (HY-10219) to induce type I diabetes)
Dosage: 200 μg/mL
Administration: Twice daily topical eye drops
Result: Reduced retinal permeability in the diabetics (7.92 ± 1.65 × 10-4 cms-1) less than before induction of diabetes (8.15 ± 2.33 × 10-4 cms-1), and less than the control group (8.85 ± 1.29 × 10-4 cms-1), while the diabetes group was 12.67 ± 1.09 × 10-4 cms-1.
体内研究

SPHINX31 (200 μg/mL; twice daily topical eye drops) protects the retinal endothelial permeability barrier from diabetes-associated loss of integrity.

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

Animal Model: Norway Brown rats (intraperitoneally injected with 50 mg/kg Streptozotocin (HY-10219) to induce type I diabetes)
Dosage: 200 μg/mL
Administration: Twice daily topical eye drops
Result: Reduced retinal permeability in the diabetics (7.92 ± 1.65 × 10-4 cms-1) less than before induction of diabetes (8.15 ± 2.33 × 10-4 cms-1), and less than the control group (8.85 ± 1.29 × 10-4 cms-1), while the diabetes group was 12.67 ± 1.09 × 10-4 cms-1.
性状Solid
溶解性数据
In Vitro: 

DMSO : 17.33 mg/mL (34.15 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9704 mL 9.8520 mL 19.7040 mL
5 mM 0.3941 mL 1.9704 mL 3.9408 mL
10 mM 0.1970 mL 0.9852 mL 1.9704 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。-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: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2 mg/mL (3.94 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (3.94 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.0 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
  • 2.

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

    Solubility: ≥ 2 mg/mL (3.94 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (3.94 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 20.0 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 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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