PF-543 Sphingosine Kinase 1 Inhibitor II|cas:1415562-82-1|西域试剂

PF-543 Sphingosine Kinase 1 Inhibitor II,98.64%

产品编号：Bellancom-15425| CAS NO：1415562-82-1| 分子式：C₂₇H₃₁NO₄S| 分子量：465.60

PF-543是新颖的可渗透细胞的SPHK1抑制剂，Ki值为4.3 nM。对SPHK1的选择性是SPHK2的100倍以上。

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	价格	库存与货期
Bellancom-15425	￥950.00	杭州北京（现货）
Bellancom-15425	￥1400.00	杭州北京（现货）
Bellancom-15425	￥3000.00	杭州北京（现货）
Bellancom-15425	￥4500.00	杭州北京（现货）
Bellancom-15425	￥6750.00	杭州北京（现货）

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PF-543 Sphingosine Kinase 1 Inhibitor II

产品介绍

PF-543 (Sphingosine Kinase 1 Inhibitor II) 是一种有效，选择性，可逆和鞘氨醇竞争性 SPHK1 抑制剂，IC₅₀ 为 2 nM，K_i 为 3.6 nM。PF-543 对 SPHK1 的选择性是 SPHK2 的 100 倍以上。PF-543 还是有效的全血中 1-磷酸鞘氨醇 (S1P) 形成的有效抑制剂，IC₅₀ 为 26.7 nM。PF-543 诱导细胞凋亡，坏死和自噬。

生物活性

PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC₅₀ of 2 nM and a K_i of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC₅₀ of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy.

体外研究

PF-543 (10-1000 nM; 24 hours; PASM cells) treatment abolishes SK1 expression at nM concentrations.
PF-543 (0.1-10 μM; 24 hours; PASM cells) treatment induces caspase-3/7 activity.
PF-543 inhibits C₁₇-S1P formation in 1483 cells with an IC₅₀ of 1.0 nM.
SphK1 inhibition by PF-543 causes a dose-dependent depletion of the intracellular level of S1P with EC₅₀ concentration of 8.4 nM and a concomitant elevation of the intracellular level of sphingosine in 1483 cells. The level of endogenous S1P in 1483 cells after a 1 h treatment with 200 nM PF-543 is decreased 10-fold, producing a proportional increase in the level of sphingosine.

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

Western Blot Analysis

Cell Line:	Human pulmonary arterial smooth muscle (PASM) cells
Concentration:	10 nM, 100 nM, 1000 nM
Incubation Time:	24 hours
Result:	Abolished SK1 expression at nM concentrations.

Apoptosis Analysis

Cell Line:	Human pulmonary arterial smooth muscle (PASM) cells
Concentration:	0.1 μM, 1 μM, 10 μM
Incubation Time:	24 hours
Result:	Induced caspase-3/7 activity in cultured human pulmonary smooth muscle cells.

体内研究
(In Vivo)

PF-543 (1 mg/kg; intraperitoneal injection; every second day; for 21 days; female C57BL/6 J mice) treatment has no effect on vascular remodelling but reduces right ventricular hypertrophy. The protection involves a reduction in the expression of p53 and an increase in the expression of anti-oxidant nuclear factor Nrf-2.
Mice are initially dosed (ip) with 10 mg/kg or 30 mg/kg of PF-543 for 24 h and the T_1/2 is 1.2 h in blood samples. Administration of 10 mg/kg PF-543 for 24 h to mice induces a decrease in SK1 expression in pulmonary vessels.

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

Animal Model:	Female C57BL/6 J mice (7-12 week-old) with hypoxic-induced pulmonary arterial hypertension
Dosage:	1 mg/kg
Administration:	Intraperitoneal injection; every second day; for 21 days
Result:	Reduced right ventricular hypertrophy. The protection involves a reduction in the expression of p53 (that promotes cardiomyocyte death) and an increase in the expression of anti-oxidant nuclear factor Nrf-2.

体内研究

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

Animal Model:	Female C57BL/6 J mice (7-12 week-old) with hypoxic-induced pulmonary arterial hypertension
Dosage:	1 mg/kg
Administration:	Intraperitoneal injection; every second day; for 21 days
Result:	Reduced right ventricular hypertrophy. The protection involves a reduction in the expression of p53 (that promotes cardiomyocyte death) and an increase in the expression of anti-oxidant nuclear factor Nrf-2.

体内研究

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

Animal Model:	Female C57BL/6 J mice (7-12 week-old) with hypoxic-induced pulmonary arterial hypertension
Dosage:	1 mg/kg
Administration:	Intraperitoneal injection; every second day; for 21 days
Result:	Reduced right ventricular hypertrophy. The protection involves a reduction in the expression of p53 (that promotes cardiomyocyte death) and an increase in the expression of anti-oxidant nuclear factor Nrf-2.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (214.78 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1478 mL	10.7388 mL	21.4777 mL
5 mM	0.4296 mL	2.1478 mL	4.2955 mL
10 mM	0.2148 mL	1.0739 mL	2.1478 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 (protect from light, stored under nitrogen)。-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

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

参考文献

. Schnute ME, et al. Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem J. 2012 May 15;444(1):79-88. [Content Brief]

. MacRitchie N, et al. Effect of the sphingosine kinase 1 selective inhibitor, PF-543 on arterial and cardiac remodelling in a hypoxic model of pulmonary arterial hypertension. Cell Signal. 2016 Aug;28(8):946-55. [Content Brief]

. Hamada M, et al. Induction of autophagy by sphingosine kinase 1 inhibitor PF-543 in head and neck squamous cell carcinoma cells. Cell Death Discov. 2017 Aug 14;3:17047. [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

1. 物质的识别

产品名：	PF-543
CAS号：	1415562-82-1
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	PF-543
分子式：	C27H31NO4S
分子量：	465.6

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。

10. 生态资料

一般注意事项：

无可用资料。

11. 废弃处置

按照所在国家，省份，县市和地方的法规处置。

12. 运输信息

正确的运输名称：	无
非危险品运输：	这种物质被视为非危险品运输。

13. 法规信息

尚未有针对此产品作出的化学安全性评估。

14. 其他信息

[1]. Schnute ME, et al. Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem J. 2012 May 15;444(1):79-88.

[2]. Wang J, et al. Crystal Structure of Sphingosine Kinase 1 with PF-543. ACS Med Chem Lett. 2014 Oct 27;5(12):1329-33.

[3]. MacRitchie N, et al. Effect of the sphingosine kinase 1 selective inhibitor, PF-543 on arterial and cardiac remodelling in a hypoxic model of pulmonary arterial hypertension. Cell Signal. 2016 Aug;28(8):946-55.

PF-543 Sphingosine Kinase 1 Inhibitor II,98.64%

PF-543 Sphingosine Kinase 1 Inhibitor II

化学品安全说明书(MSDS)

质检证书(COA)

1. 物质的识别

2. 合成/成分数据

3. 急救措施

4. 消防措施

5. 泄漏应急处理

6. 处理和储存

7. 接触控制和个人防护

8. 稳定性和反应活性

9. 毒性资料

10. 生态资料

11. 废弃处置

12. 运输信息

13. 法规信息

14. 其他信息

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