882697-00-9
882697-00-9 structure
- Name: Anle138b
- Chemical Name: Anle138b
- CAS Number: 882697-00-9
- Molecular Formula: C16H11BrN2O2
- Molecular Weight: 343.175
- Catalog: Research Areas Neurological Disease
- Create Date: 2018-06-24 14:42:14
- Modify Date: 2024-01-10 10:18:58
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Anle138b is a novel oligomer modulator.
| Name | Anle138b |
|---|---|
| Synonyms |
1H-Pyrazole, 3-(1,3-benzodioxol-5-yl)-5-(3-bromophenyl)-
3-(1,3-Benzodioxol-5-yl)-5-(3-bromophenyl)-1H-pyrazole MFCD30146410 |
| Description | Anle138b is a novel oligomer modulator. |
|---|---|
| Related Catalog | |
| In Vitro | Oligomeric aggregates are presumed to be the key neurotoxic agent. Anle138b blocksthe formation of pathological aggregates of prion protein and of α-synuclein, which is deposited in Parkinson’s disease and other synucleinopathies such as dementia with Lewy bodies and multiple system atrophy. Anle138b strongly inhibits all prion strains tested including BSE-derived and human prions. Anle138b shows structure-dependent binding to pathological aggregates and strongly inhibits formation of pathological oligomers both for prion protein and α-synuclein[1]. |
| In Vivo | Anle138b has no detectable toxicity at therapeutic doses and an excellent oral bioavailability and blood–brain-barrier penetration. In mouse models of prion disease and in three different PD mouse models, anle138b strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression[1]. Di-phenyl-pyrazole anle138b binds to aggregated tau and inhibits tau aggregation. Anle138b treatment effectively ameliorates disease symptoms, increases survival time and improves cognition of tau transgenic PS19 mice[2]. |
| Kinase Assay | Compounds (Anle138b) are diluted into the assay mixture from 10-fold stock solutions containing 10 % DMSO (v/v), resulting in a final concentration of 1 % DMSO in all samples. Experiments are started by diluting the 5-fold stock solution of fluorescently labelled α-syn in 50 mM Tris-buffer, pH 7.0, containing 1 % DMSO, 10 μM FeCl3 and compounds (Anle138b) in concentrations ranging from 1-10 μM. Aggregation is monitored at room temperature for at least 2.5 h in 3-4 independent samples for each experimental group[1]. |
| Animal Admin | Mice: During the first 2 weeks of treatment, 2 mg of anle138b dissolved in 10 μL DMSO mixed with 200 μL peanut butter are given. After 2 weeks of treatment, the dose is increased to 5 mg in 10 μL DMSO/200 μL peanut butter. At the age of 33 weeks, the dose is increased to 2×5 mg per day. All mice are monitored daily for signs of disease[1]. |
| References |
| Density | 1.6±0.1 g/cm3 |
|---|---|
| Boiling Point | 527.3±50.0 °C at 760 mmHg |
| Molecular Formula | C16H11BrN2O2 |
| Molecular Weight | 343.175 |
| Flash Point | 272.7±30.1 °C |
| Exact Mass | 342.000397 |
| LogP | 4.96 |
| Vapour Pressure | 0.0±1.3 mmHg at 25°C |
| Index of Refraction | 1.670 |
| Storage condition | 2-8℃ |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H315-H319-H335 |
| Precautionary Statements | P305 + P351 + P338 |
| RIDADR | NONH for all modes of transport |