924537-98-4
中文名稱
319H6
英文名稱
BT-13
CAS
924537-98-4
分子式
C23H27F4N3O4S
分子量
517.54
MOL 文件
924537-98-4.mol
更新日期
2024/12/22 16:36:05
924537-98-4 結(jié)構(gòu)式
基本信息
中文別名
化合物BT-13 英文別名
319H6BT 13 NEW
BT-13 (RET agonist BT13)
Benzenesulfonamide, N,N-diethyl-3-[4-[4-fluoro-2-(trifluoromethyl)benzoyl]-1-piperazinyl]-4-methoxy-
物理化學(xué)性質(zhì)
沸點(diǎn)637.0±65.0 °C(Predicted)
密度1.326±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 25 mg/mL (48.31 mM)
酸度系數(shù)(pKa)0.42±0.20(Predicted)
形態(tài)Solid
顏色White to off-white
常見(jiàn)問(wèn)題列表
生物活性
BT-13 是有效的、膠質(zhì)細(xì)胞源性神經(jīng)營(yíng)養(yǎng)因子 (GDNF) 受體 RET 的選擇性激動(dòng)劑 (獨(dú)立于 GDNF 配體發(fā)揮作用),促進(jìn)體外感覺(jué)神經(jīng)元神經(jīng)突生長(zhǎng),減輕大鼠神經(jīng)病變的發(fā)生。靶點(diǎn)
GDNF receptor RET.
體外研究
BT-13 stimulates phosphorylation of RET, as well as RET-dependent intracellular signaling, but activated neither NGF receptor TrkA nor BDNF receptor TrkB nor intracellular signaling in the absence of RET.
體內(nèi)研究
BT-13 (20 and 25mg/kg in rats induced by ligation of left L5 and L6 spinal nerves) has a slight antinociceptive/antihyperalgesic effect and protected DRG neurons in rats with surgery-induced neuropathy.
Animal Model: | Rats induced by ligation of left L5 and L6 spinal nerves. |
Dosage: | 5-25 mg/kg, dissolved in sesame oil containing 5% DMSO. |
Administration: | Subcutaneous injections on post-surgical day 1, 3, 5, 8, 10, and 12. |
Result: | 20 and 25mg/kg decreased mechanical hypersensitivity and normalized expression of sensory neuron markers in dorsal root ganglia. |