盐酸罗哌卡因一水合物 T6645

Product Introduction
Bioactivity


英文名: Ropivacaine hydrochloride monohydrate

描述: Ropivacaine hydrochloride monohydrate (LEA-103 HCl) 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。

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 62 mg/mL (199.44 mM)
H2O : 46 mg/mL (147.97 mM)


关键字: LEA-103 | Potassium Channel | hypertension | Na channels | pain | K(2P) | neuropathic | Inhibitor | vasoconstrictive | KcsA | Ropivacaine hydrochloride Monohydrate | Na+ channels | Ropivacaine HCl Monohydrate | potassium | Ropivacaine hydrochloride monohydrate | Ropivacaine Hydrochloride | TREK-1 | Sodium Channel | inhibit | conduction | Ropivacaine hydrochloride | LEA103 | channel | neuronal

相关产品: Linopirdine | RY785 | TASK-1-IN-1 | DMP-543 | ICA-069673 | 20(S)-Ginsenoside Rg3 | Senicapoc | P-1075 | ML365 | Potassium Channel Activator 1

相关库: Drug Repurposing Compound Library | Approved Drug Library | Potassium Channel Blocker Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途