Tolebrutinib|1971920-73-6|(SAR442168; PRN2246)-陌孚医药/Medlife

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Tolebrutinib (Synonyms: SAR442168; PRN2246)

目录号: PL01786 纯度: ≥98%

CAS No. :1971920-73-6

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中文名称	Tolebrutinib
英文名称	Tolebrutinib
英文别名	Tolebrutinib;c]pyridin-2-one;8CZ82ZYY9X;4-amino-3-(4-phenoxyphenyl)-1-[(3R)-1-(prop-2-;enoyl)piperidin-3-yl]-1,3-dihydro-2H-imidazo[4,5-;(R)-1-(1-Acryloylpiperidin-3-yl)-4-amino-3-(4-phenoxyphenyl)-1H-imidazo[4,5-c]pyridin-2(3H)-one;4-amino-3-(4-phenoxyphenyl)-1-[(3R)-1-prop-2-enoylpiperidin-3-yl]imidazo[4,5-c]pyridin-2-one;Tolebrutinib [INN];GTPL10625;BTK'168;PRN2246;SAR442168;example 3 [WO2016196840A1];2H-Imidazo(4,5-C)pyridin-2-on
Cas No.	1971920-73-6
分子式	C₂₆H₂₅N₅O₃
分子量	455.51
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Tolebrutinib (SAR442168) 是一种有效的，选择性，具有口服活性和可透过血脑屏障的布鲁顿氏酪氨酸激酶 (BTK) 抑制剂，在 Ramos B 细胞和 HMC 小胶质细胞中的 IC₅₀ 值分别为 0.4 和 0.7 nM。Tolebrutinib 对中枢神经系统免疫具有功效。Tolebrutinib 可用于多发性硬化症 (MS) 的研究。

生物活性

Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC 50 s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).

性状

Solid

IC50 & Target[1][2]

IC50: 0.7 nM (BTK; in HMC microglia cells)

体外研究(In Vitro)

PRN2246 blocks the BCR-mediated activation (IC50=10 nM) and Fc receptor activation (IC50=166 and 9.6 nM for FcεR and FcγR, repectively) of immune cells.
PRN2246 inhibits microglial FcγR activation through durable occupancy of BTK, with an IC50 of 157 nM. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

PRN2246 (1-5 mg/kg; p.o. q.d. for 28 d) produces dose-dependent protection from in myelin oligodendrocyte glycoprotein (MOG)-induced experimental autoimmune encephalomyelitis (EAE) model. 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

ClinicalTrial

参考文献

[1]. Dahl K, et, al. Radiosynthesis of a Brutons tyrosine kinase inhibitor, [ 11 C]Tolebrutinib, via palladium-NiXantphos-mediated carbonylation. J Labelled Comp Radiopharm. 2020 Sep;63(11):482-487.
[2]. Francesco MR, et, al. PRN2246, a potent and selective blood brain barrier penetrating BTK inhibitor, exhibits efficacy in central nervous system immunity. Multiple Sclerosis Journal. 2017;Poster Session 2:P989.

溶解度数据	In Vitro: DMSO : 100 mg/mL (219.53 mM; Need ultrasonic)配制储备液

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Data Sheet

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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