N3PT N3-pyridyl thiamine|cas:13860-66-7|西域试剂

N3PT N3-pyridyl thiamine,98.98%

产品编号：Bellancom-16339| CAS NO：13860-66-7| 分子式：C₁₃H₁₉Cl₂N₃OS| 分子量：336.28

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货号	价格	库存与货期
Bellancom-16339	￥2325.00	杭州北京（现货）
Bellancom-16339	￥3534.00	杭州北京（现货）
Bellancom-16339	￥8370.00	杭州北京（现货）
Bellancom-16339	￥13020.00	杭州北京（现货）

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N3PT N3-pyridyl thiamine

产品介绍

N3PT (N3-pyridyl thiamine) 是转酮醇酶 (transketolase) 抑制剂。N3PT 通过焦磷酸化来结合转酮醇酶，对缺少结合型硫胺素转酮酶 (Apo-TK) 的 K_d 为 22 nM。

生物活性

N3PT (N3-pyridyl thiamine) is a potent and selective transketolase inhibitor. N3PT is pyrophosphorylated and then binds to transketolase with an K_d value of 22 nM (Apo-TK, transketolase lacking bound thiamine).

体外研究

Transketolase is a key enzyme in pentose phosphate pathway of tumor cells.
N3PT (compound 1) shows an average EC₅₀ value of 26 nM against human transketolase in HCT-116 cells.
N3PT (1 ppM or 5 ppM) inhibits thiamine-utilizing enzymes activity dramatically without reducing NADPH-containing glucose-6-phosphate dehydrogenase (G6PD) activity.

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

体内研究

N3PT (compound 1) (100 mg/kg; i.v.; twice a day; 2 weeks) shows inhibitory effect on transketolase activity without significantly anti-tumor activity in HCT-116 tumor-bearing nude mice.

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

Animal Model:	HCT-116 tumor-bearing nude mice
Dosage:	100 mg/kg
Administration:	Intravenous injection; twice a day; 2 weeks
Result:	Decreased the activity of transketolase with no apparent effect on tumor size. Indicated that there were alternative pathways to generate ribose for DNA synthesis that were operating in these tumor cell lines.

体内研究

N3PT (compound 1) (100 mg/kg; i.v.; twice a day; 2 weeks) shows inhibitory effect on transketolase activity without significantly anti-tumor activity in HCT-116 tumor-bearing nude mice.

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

Animal Model:	HCT-116 tumor-bearing nude mice
Dosage:	100 mg/kg
Administration:	Intravenous injection; twice a day; 2 weeks
Result:	Decreased the activity of transketolase with no apparent effect on tumor size. Indicated that there were alternative pathways to generate ribose for DNA synthesis that were operating in these tumor cell lines.

性状

Solid

溶解性数据

In Vitro:

DMSO : 2.86 mg/mL (8.50 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9737 mL	14.8686 mL	29.7371 mL
5 mM	0.5947 mL	2.9737 mL	5.9474 mL
10 mM	---	---	---

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。

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