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BT-13 {[allProObj[0].p_purity_real_show]}

货号:A1177143

BT-13是一种选择性 GDNF 受体 RET 激动剂,独立于 GDNF 配体发挥作用,能够促进体外感觉神经元神经突生长,同时减轻大鼠神经病变的发生。

BT-13 化学结构 CAS号:924537-98-4
BT-13 化学结构
CAS号:924537-98-4
BT-13 3D分子结构
CAS号:924537-98-4
BT-13 化学结构 CAS号:924537-98-4
BT-13 3D分子结构 CAS号:924537-98-4
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BT-13 纯度/质量文件 产品仅供科研

货号:A1177143 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 c-RET 其他靶点 纯度
Regorafenib +++

RET, IC50: 1.5 nM

98%
TG101209 ++

RET, IC50: 17 nM

FLT3 99%+
Danusertib +

RET, IC50: 31 nM

99%+
AD80 ++++

RET V804M, IC50: 0.6 nM

RET wt, IC50: 1.3 nM

Raf,Src 99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

BT-13 细胞实验

Cell Line
Concentration Treated Time Description References
Adult rat dorsal root ganglion (DRG) sensory neurons 100 ng/ml 24–30 h BT13 promoted neurite growth from peptidergic sensory neurons but did not affect neurite initiation Front Pharmacol. 2017 Jun 21;8:365
MG87RET murine fibroblasts 0.1–50 µM BT13 dose-dependently activated luciferase with EC50=17.4 µM, inducing an 11.6-fold increase in luciferase activity Front Pharmacol. 2017 Jun 21;8:365
RET-knockout embryonic midbrain dopamine neurons 0.1 μM, 1 μM 5 days To assess the effect of BT13 on the survival of RET-knockout dopamine neurons. BT13 failed to influence the survival of RET-knockout embryonic midbrain dopamine neurons. Mov Disord. 2020 Feb;35(2):245-255
Wild-type embryonic midbrain dopamine neurons 0.1 μM, 1 μM 5 days To assess the effect of BT13 on the survival of cultured dopamine neurons. BT13 significantly increased the number of surviving wild-type embryonic midbrain dopamine neurons. Mov Disord. 2020 Feb;35(2):245-255
MG87RET cells 25 μM To evaluate the ability of BT13 to activate RET and signal via GFL receptors. BT13 significantly increased the phosphorylation level of RET in cells expressing GFR α1/RET and GFR α2/RET. Mov Disord. 2020 Feb;35(2):245-255

BT-13 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Spinal nerve ligation (SNL)-induced experimental neuropathy Subcutaneous injection 20 and 25 mg/kg Administered on post-surgical days 1, 3, 5, 8, 10, and 12 BT13 attenuated mechanical hypersensitivity and reversed injury-induced changes in the expression of sensory neuron markers in dorsal root ganglia Front Pharmacol. 2017 Jun 21;8:365
Mice Not specified Stereotactic injection into the striatum 103.5 μg, 207 μg, 517.5 μg, 776.25 μg Single injection To evaluate the ability of BT13 to activate intracellular signaling cascades in the mouse striatum. BT13 at the dose of 750μg significantly increased phosphorylation of ERK and S6. Mov Disord. 2020 Feb;35(2):245-255

BT-13 参考文献

[1]Ivanova L, Tammiku-Taul J, García-Sosa AT, Sidorova Y, Saarma M, Karelson M. Molecular Dynamics Simulations of the Interactions between Glial Cell Line-Derived Neurotrophic Factor Family Receptor GFRα1 and Small-Molecule Ligands. ACS Omega. 2018 Sep 30;3(9):11407-11414. doi: 10.1021/acsomega.8b01524. Epub 2018 Sep 19. PMID: 30320260; PMCID: PMC6173496.

[2]Sidorova YA, Bespalov MM, Wong AW, Kambur O, Jokinen V, Lilius TO, Suleymanova I, Karelson G, Rauhala PV, Karelson M, Osborne PB, Keast JR, Kalso EA, Saarma M. A Novel Small Molecule GDNF Receptor RET Agonist, BT13, Promotes Neurite Growth from Sensory Neurons in Vitro and Attenuates Experimental Neuropathy in the Rat. Front Pharmacol. 2017 Jun 21;8:365. doi: 10.3389/fphar.2017.00365. PMID: 28680400; PMCID: PMC5478727.

BT-13 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.66mL

1.93mL

0.97mL

19.32mL

3.86mL

1.93mL

BT-13 技术信息

CAS号924537-98-4
分子式C23H27F4N3O4S
分子量 517.54
SMILES Code FC(F)(F)C1=C(C=CC(F)=C1)C(N(CC2)CCN2C3=C(C=CC(S(=O)(N(CC)CC)=O)=C3)OC)=O
MDL No. MFCD19950448
别名
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

DMSO: 25 mg/mL(48.31 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
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