N3PT|13860-66-7|(N3-pyridyl thiamine)-陌孚医药/Medlife

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N3PT (Synonyms: N3-pyridyl thiamine)

目录号: PL12403 纯度: ≥98%

CAS No. :13860-66-7

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中文名称	N3PT
中文别名	3-[(2-氨基-6-甲基-3-吡啶基)甲基]-5-(2-羟基乙基)-4-甲基噻唑鎓氯化物盐酸盐;3-[(2-氨基-6-甲基-3-吡啶基)甲基]-5-(2-羟基乙基)-4-甲基噻唑氯化物盐酸盐;转酮醇酶(TK)抑制剂(N3PT);3-((2-氨基-6-甲基吡啶-3-基)甲基)-5-(2-羟基乙基)-4-甲基-3-鎓氯盐酸盐;化合物 T12158
英文名称	N3PT
英文别名	N3PT;N3-pyridyl thiaMine;3-[(2-Amino-6-methyl-3-pyridyl)methyl]-5-(2-hydroxyethyl)-4-methylthiazolium chloride hydrochloride;N3-pyridyl thiamine
Cas No.	13860-66-7
分子式	C₁₃H₁₈N₃Os+^.Cl-^.HCl
分子量	336.28
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	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).
性状	Solid
IC50 & Target[1][2]	transketolase
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Thomas AA, et al. Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2206-10. [2]. Jeno Gyuris, May Han, Ronan C, N3-pyridyl-thiamine and its use in cancer treatments. Patent Numeber: WO2005094803 A2 [3]. Allen A. Thomas, Josh Ballard, Bryan Bernat. Potent and Selectiv

溶解度数据	In Vitro: DMSO : 2.86 mg/mL (8.50 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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