| Name | Ropivacaine hydrochloride monohydrate |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 65 mg/mL (197.64 mM), Sonication is recommended.
H2O : 46 mg/mL (139.87 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.08 mM), Sonication is recommended.
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| Keywords | vasoconstrictive | TREK-1 | SodiumChannel | sodium ion influx | Sodium Channel | PotassiumChannel | Potassium Channel | potassium | neuropathic | LEA-103 | LEA103 | K(2P) | conduction |
| Inhibitors Related | Minoxidil sulfate | Phenytoin sodium | Procaine | Tannic acid | Lidocaine | Hydrochlorothiazide | Valproic Acid | Lidocaine hydrochloride | L-Aspartic aicd sodium | Mebeverine hydrochloride | Ursodeoxycholic acid | Indapamide |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Neuroprotective Compound Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Drug Library |
United States
