TDI-10229
目录号: PL03291 纯度: ≥99%
CAS No. :2810887-45-5
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中文名称
TDI-10229
中文别名
化合物TDI-10229
英文名称
TDI-10229
英文别名
TDI-10229;TDI 10229,TDI10229;CompoundTDI10229
Cas No.
2810887-45-5
分子式
C16H16ClN5
分子量
313.78
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
TDI-10229 是一种口服有效的可溶性腺苷酸环化酶 (sAC, ADCY10) 抑制剂 (IC50 值为 195 nM)。TDI-10229 在生化和细胞分析中都显示出对 sAC 的纳摩尔级抑制,并表现出足以保证其用作体内工具化合物的小鼠药代动力学特性。
生物活性
TDI-10229 is a potent and orally bioavailable inhibitor of soluble adenylyl cyclase (sAC, ADCY10). TDI-10229 displays nanomolar inhibition of sAC in both biochemical and cellular assays (IC 50 of 195 nM) and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound.
性状
Solid
IC50 & Target[1][2]
IC50: 195 nM (sAC).
体外研究(In Vitro)
TDI-10229 exhibits good permeability with an IC50 of 92 nM for human 4-4 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
TDI-10229 (5 mg/kg; p.o.) treatment shows the C max , AUC and MRT were 15.5 μM, 94 μg h/mL and 3.95 hours, respectively.
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
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Balbach M, et al. Soluble adenylyl cyclase inhibition prevents human sperm functions essential for fertilization [published online ahead of print, 2021 Aug 31]. Mol Hum Reprod. 2021;gaab054.
[2]. Fushimi M, et al. Discovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10). ACS Med Chem Lett. 2021;12(8):1283-1287. Published 2021 Jul 14.
溶解度数据
In Vitro: DMSO : 125 mg/mL (398.37 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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