妥布特罗

生物活性靶点体外研究体内研究妥布特罗试剂级价格

妥布特罗

CAS号:41570-61-0
英文名:Tulobuterol
中文名:妥布特罗
CBNumber:CB8320201
分子式:C12H18ClNO
分子量:227.73
MOL File:41570-61-0.mol

妥布特罗化学性质

熔点 :89-91°C
沸点 :338.2±27.0 °C(Predicted)
密度 :1.098±0.06 g/cm3(Predicted)
RTECS号 :DA4734170
储存条件 :-20°C Freezer
溶解度 :DMSO (Slightly), Methanol (Slightly)
酸度系数(pKa) :13.62±0.20(Predicted)
形态 :Solid
颜色 :White to Off-White
CAS 数据库 :41570-61-0(CAS DataBase Reference)

安全信息

安全说明 :24/25
海关编码 :29214990
毒性 :LD50 in male mice, rats, rabbits (mg/kg): 305, 850, 563 orally; 170, 417, 164 s.c. (Kubo, 1975)

妥布特罗性质、用途与生产工艺

生物活性 Tulobuterol (C-78 free base) 是一种长效的 β2 肾上腺素受体 (β2-adrenoceptor) 激动剂，可减少慢性阻塞性肺疾病和支气管哮喘的发作频率。Tulobuterol 也是一种拟交感神经药，用作透皮贴剂，可增加正常的横膈膜肌肉力量。
靶点

β2-adrenoceptor

体外研究

Tulobuterol (0.1 μM; 24 hours or 72 hours; human tracheal epithelial cells) treatment decreases the RV14 RNA levels at 1 day and at 3 days after infection. The concentrations of sICAM-1 in the supernatants of the cells treated with tulobutero are significantly lower than those in the cells treated with vehicle before RV14 infection. Treatment with Tulobuterol reduces the number of acidic endosomes with green fluorescence in the cells and the fluorescence intensity of acidic endosomes in the cells. Also reduces the RV14 infection-induced secretion of IL-1β, IL-6, and IL-8. Tulobuterol treatment produces a small but significant reduction in the amount of p50, p65, and c-Rel of NF-κB induced by RV14 infection.

RT-PCR

Cell Line:	Human tracheal epithelial cells infected with RV14
Concentration:	0.1 μM
Incubation Time:	24 hours or 72 hours
Result:	Decreased the RV14 RNA levels at 1 day and at 3 days after infection. The concentrations of sICAM-1 in the supernatants of the cells were significantly lower. Reduced the number of acidic endosomes with green fluorescence in the cells and the fluorescence intensity of acidic endosomes in the cells. Also reduced the RV14 infection-induced secretion of IL-1β, IL-6, and IL-8. And produced a small but significant reduction in the amount of p50, p65, and c-Rel of NF-κB induced by RV14 infection.

体内研究

In vivo effect of Tulobuterol is examined the on the contractility of diaphragm muscles prepared from mice (BALBs/c mice; 21.7 ± 0.2 g) treated with Endotoxin. Contractile parameters of force-frequency curves and twitch kinetics using untreated or treated diaphragm muscles at 0 (E0) and 4 (E4) hours after E. coli endotoxin (20 mg/kg) administration are measured. E0 and E4 diaphragm muscles are analyzed at 0, 12, and 24 h after transdermal Tulobuterol treatment. The force-frequency curves of E0 and E4 diaphragm muscles at three time points are not significantly changed each other, indicating that Tulobuterol patch restores the muscle contractility. Thus, diaphragm muscle contractility is maintained during 4 h of endotoxin administration with Tulobuterol patch for over 24 h.