AZD7545|252017-04-2|-陌孚医药/Medlife

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AZD7545

目录号: PL09496 纯度: ≥99%

CAS No. :252017-04-2

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中文名称	AZD7545
中文别名	4-((3-氯-4-(((2R)-3,3,3-三氟-2-羟基-2-甲基-1-氧代丙基)氨基)苯基)磺酰基)-N,N-二甲基苯甲酰胺;4-[[3-氯-4-[[(2R)-3,3,3-三氟-2-羟基-2-甲基-1-氧代丙基]氨基]苯基]磺酰基]-N,N-二甲基苯甲酰胺;AZD7545 抑制剂;(R)-4-((3-氯-4-(3,3,3-三氟-2-羟基-2-甲基丙酰胺基)苯基)磺酰基)-N,N-二甲基苯甲酰胺
英文名称	AZD7545
英文别名	(R) - N - {2 - Chloro - 4 - [4 - (N,N - dimethylcarbamoyl)phenylsulphonyl]phenyl} - 2 - hydroxy - 2 - methyl - 3,3,3 - trifluoropropanamide;(2,4-Dihydroxy-5-isopropylphenyl){5-[(4-methyl-1-piperazinyl)meth yl]-1,3-dihydro-2H-isoindol-2-yl}methanone;(R) - N - {2 - Chloro - 4 - [4 - (N,N - dimethylcarbamoyl)phenylsulphonyl]phenyl} - 2 - hydroxy - 2 - methyl - 3,3,3 - triflu;AZD7545;AZD-7545;4-[(3-Chloro-4-{[(2r)-3,3,3-Trifluoro-2-Hydroxy-2-Methylpropanoyl]amino}phenyl)sulfonyl]-N,N-Dimethylbenzamide;4-{3-chloro-4-[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanamido]benzenesulfonyl}-N,N-dimethylbenzamide;DTDZLJHKVNTQGZ-GOSISDBHSA-N;AZD 7545;2q8g;Azd4575;C19H18ClF3N2O5S;GTPL9362;AOB6866;BCP07524;4-[3-chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino]phenyl]sulfonyl-N,N-dimethylbenzamide;E
Cas No.	252017-04-2
分子式	C₁₉H₁₈ClF₃N₂O₅S
分子量	478.87
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	AZD7545 是一种有效，竞争性和选择性的 PDHK2 抑制剂，对 PDHK1 和 PDHK2 的 IC₅₀ 分别为 36.8 nM 和 6.4 nM。
生物活性	AZD7545 is a potent, competitive, selective PDHK2 (pyruvate dehydrogenase kinase 2) inhibitor with IC 50 s of 36.8 nM, 6.4 nM for PDHK1 and PDHK2, respectively.
性状	Solid
IC50 & Target[1][2]	IC50: 6.4 nM (PDHK2), 36.8 nM (PDHK1)
体外研究(In Vitro)	AZD7545 (10 μM; 90 hours for BRAF human melanoma cells and 120 hours for NRAS human melanoma cells) specifically suppresses growth of cells harboring BRAF and NRAS mutations as well as in inhibitor-resistant human melanoma. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(In Vivo)	A single dose of AZD7545 (Oral administration; 10 mg/kg once a day (08:00 h) or Twice a day (08:00 and 18:00 h); for 7 days) to Wistar rats increases the proportion of liver PDH in its active, dephosphorylated form in a dose-related manner. A single dose of 10 mg/kg also significantly elevates muscle PDH activity in obese Zucker (fa/fa) rats. has not independently confirmed the accuracy of these methods. They are for reference only.
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
参考文献	[1]. Morrell JA, et al. AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2. Biochem Soc Trans. 2003 Dec;31(Pt 6):1168-70. [2]. Mayers RM, et al. AZD7545, a novel inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2), activates pyruvate dehydrogenase in vivo and improves blood glucose control in obese (fa/fa) Zucker rats. Biochem Soc Trans. 2003 Dec;31(Pt 6):1165-7.

溶解度数据	In Vitro: DMSO : ≥ 46 mg/mL (96.06 mM)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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