123441-03-2
Rivastigmine
CAS: 123441-03-2
Molecular Formula: C14H22N2O2
123441-03-2 - Names and Identifiers
123441-03-2 - Physico-chemical Properties
| Molecular Formula | C14H22N2O2 |
| Molar Mass | 250.34 |
| Density | 1.038±0.06 g/cm3(Predicted) |
| Boling Point | 316.2±34.0 °C(Predicted) |
| Specific Rotation(α) | D20 -32.1° (c = 5 in ethanol) |
| Flash Point | 145℃ |
| Vapor Presure | 0.000416mmHg at 25°C |
| pKa | pKa 8.99 (Uncertain) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| Sensitive | Sensitive to light |
| Refractive Index | 1.518 |
| Use | This product is for scientific research only and shall not be used for other purposes. |
| In vitro study | Rivastigmine (S-Rivastigmine; 1 µM; 24 hours) reduces LPS (2.5 µg/ml)-induced TNF-α and IL-6 by 50% and 46% combined with carbachol (10 µM), respectively and does not cause any significant reduction in pro-inflammatory cytokines . Rivastigmine (1 µM), carbachol (10 µM), or a combination of both drugs, does not have a cytotoxic effect on activated cells. |
| In vivo study | In its peripheral inhibitory action, Rivastigmine is selective for the central nervous system. It can slow down the memory impairment in rats with anterior brain injury. The drug is rapidly absorbed by the oral route. Its bioavailability is 0.355 and its protein binding rate is low. Its elimination half-life is less than 2 hours, and rivastigmine is converted to its inactive metabolite by bypassing the hepatic metabolic pathway. Rivastigmine also inhibits AChE in a concentration-dependent manner. |
123441-03-2 - Risk and Safety
| UN IDs | UN 2810 6.1 / PGIII |
| HS Code | 2924296000 |
123441-03-2 - Reference
| Reference Show more | 1. [IF=1.965] Zhang Xiao-Zhong et al."Synthesis, in vitro assays, molecular docking, theoretical ADMET prediction, and evaluation of 4-methoxy-phenylthiazole-2-amine derivatives as acetylcholinesterase inhibitors."Med Chem Res. 2019 Oct;28(10):1683-1693 |
123441-03-2 - Introduction
Rivastigmine tartrate is a cholinesterase inhibitor, IC50 is 5.5 uM, and it can also inhibit butyrylcholinesterase and acetylcholinesterase.
Last Update：2022-10-16 17:12:55
123441-03-2 - Reference Information
| introduction | livantigmine (rivastigmine) is a new drug for the treatment of mild to moderate Alzheimer's disease (AD) and belongs to the 2nd generation acetylcholinesterase inhibitor. Previously, the largest clinical trial (Phase III) has proved its safety and effectiveness, and the daily life (ADL), behavior and cognitive function of patients taking the drug have been significantly improved. |
| Indications | Listigmine is a second-generation cholinesterase inhibitor, and its inhibitory effect on central AchE is greater than that of peripheral acetylcholinesterase (AchE) Strong inhibitory effect. At the same time, it can inhibit butyrylcholinesterase. It is effective for patients with mild and moderate AD, especially for patients with heart, liver and kidney diseases. Liss's effect on improving cognitive abilities such as memory, attention and sense of location is significant. |
| Biological activity | Rivastigmine (SDZ-ENA 713, Exelon) is an inhibitor of cholinesterase with an IC50 of 5.5 μM. It inhibits acetylcholinesterase (IC50=4.15 µM) and butyrylcholinesterase (IC50=37 nM). |
| Target | Value |
Last Update：2024-04-10 22:29:15
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