| Description | Ropivacaine hydrochloride monohydrate (LEA-103 HCl) is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly. |
| In vitro | 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. |
| Target activity | TREK1 (COS-7 cell membrane):402.7 μM (IC50) |
| Synonyms | Ropivacaine HCl, Ropivacaine HCl monohydrate, LEA 103, 盐酸罗哌卡因, 盐酸罗哌卡因一水合物, LEA-103 HCl |
| molecular weight | 328.88 |
| Molecular formula | C17H29ClN2O2 |
| CAS | 132112-35-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 65 mg/mL (197.64 mM), Sonication is recommended. H2O: 46 mg/mL (147.97 mM) |
| References | 1. Simpson D, et al. Drugs, 2005, 65(18), 2675-2717. |
Ropivacaine hydrochloride monohydrate
CAS No.: 132112-35-7
Ropivacaine hydrochloride monohydrate (LEA-103 HCl) is an anaesthetic agent and blocks impulse conduction in nerve fibre
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