Ropivacaine HCl monohydrate 是钠通道阻断剂,通过可逆地抑制钠离子内流从而引起神经纤维脉冲传导阻滞。Ropivacaine HCl monohydrate 也是 K2P(双孔钾通道)TREK-1的抑制剂。在动物实验模型中,Ropivacaine HCl monohydrate可用于神经性疼痛的缓解。
产品描述
Ropivacaine HCl is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.
体外活性
Raltitrexed induces double-stranded DNA breaks in a concentration-dependent manner. In Lovo cells and LS174T cell lines containing wild-type p53, Raltitrexed increases the levels of the Bax protein up to 5-fold. In human colon cancer cells, Raltitrexed is actively absorbed into cells and is then rapidly and extensively metabolized into a series of polyglutamates, which results in the effective inhibition of thymidylate synthase. Raltitrexed is delivered to the brain very quickly and can be detected in all brain tissues within 5 minutes. In human colon cancer cells, the combination of Raltitrexed and SN-38 results in a synergistic cytotoxic effect within a range of concentrations. Raltitrexed is a specific folate-based inhibitor of thymidylate synthase. The effect on the activity of advanced rectal cancer is similar to fluorouracil (5-fluorouracil) plus leucovorin. Raltitrexed produces activity by rapid cell entry and glutamination. The glutaminated derivatives are more than 100 times more active than the parent compound. In the HCT-8 cell line, Raltitrexed results in an increase in intracellular phosphoribosyl pyrophosphate (PRPD) indicating that the cytotoxic effect of Raltitrexed in combination with 5-FU is due to increased nucleotide formation of 5-FU. Combinations of Raltitrexed and folinic acid (5FU-FA) show a combination of mode-dependent, synergistic inhibition of proliferation, which is determined by measuring the combination series. Raltitrexed combined with Vorinostat produced significant synergistic effects of cell cycle perturbation and S-phase arrest.
Cas No.
132112-35-7
分子式
C17H29ClN2O2
分子量
328.88
别名
Ropivacaine HCl monohydrate;盐酸罗哌卡因;盐酸罗哌卡因一水合物;LEA 103;Ropivacaine HCl;LEA-103 HCl
储存和溶解度
Ethanol:<1 mgml
DMSO:62 mg/mL (199.44 mM)
H2O:46 mg/mL (147.97 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years