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Purity: ≥98%
Anle138b is a novel oligomer modulator for disease-modifying therapy of neurodegenerative diseases such as prion and Parkinson's disease.. Anle138b blocks the activity of conducting Aβ pores without changing the membrane embedded Aβ-oligomer structure, at the mechanistic level. Anle138b blocks interpeptide main chain interactions and impedes the spontaneous formation of ordered β-sheet structures, in particular those with out-of-register antiparallel β-strands.
| ln Vitro |
It is believed that low aggregates are important neurotoxicants. Emrusolmin strongly inhibits all prion strains examined, mixing BSE derivatives and human prions. Emrusolmin swells the formation of pathogenic aggregates of prion proteins and alpha-synuclein, which form dead deposits in Parkinson's disease and other synucleinopathies (e.g. Louis Emrusolmin). Alpha-synuclein and prion protein pathological oligomers are severely inhibited by emusolmin, which exhibits structural reliance on pathological aggregation [1].
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| ln Vivo |
Emrusolmin has been demonstrated to bind structurally binding to pathological aggregates and strongly suppresses the production of prion protein and alpha-synapsin nuclear pathological oligomers in vitro and in the chamber [1]. Emrusolmin (0.6-2 g/kg; Oral
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| Animal Protocol |
Animal/Disease Models: Two-month-old PLP-hαSyn mice [3]
Doses: 0.6 and 2 g/kg Route of Administration: Oral Experimental Results: Prevention of motor deficits and neurodegeneration PLP-hαSyn mice. |
| References |
[1]. Wagner J, et al. Anle138b: a novel oligomer modulator for disease-modifying therapy of neurodegenerative diseases such as prion and Parkinson's disease. Acta Neuropathol. 2013 Jun;125(6):795-813.
[2]. Martinez Hernandez A, et al. The diphenylpyrazole compound anle138b blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology. EMBO Mol Med. 2018;10(1):32-47. [3]. Heras-Garvin A, et al. Anle138b modulates α-synuclein oligomerization and prevents motor decline and neurodegeneration in a mouse model of multiple system atrophy. Mov Disord. 2019;34(2):255-263. |
| Molecular Formula |
C16H11BRN2O2
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|---|---|
| Molecular Weight |
343.18
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| Exact Mass |
342.0004
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| CAS # |
882697-00-9
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| Related CAS # |
882697-00-9
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| SMILES |
BrC1=CC(C2=NNC(C3=CC=C(OCO4)C4=C3)=C2)=CC=C1
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| Chemical Name |
5-(1,3-Benzodioxol-5-yl)-3-(3-bromophenyl)-1H-pyrazole
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| Synonyms |
Anle 138b Anle-138bAnle138b
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~145.70 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9139 mL | 14.5696 mL | 29.1392 mL | |
| 5 mM | 0.5828 mL | 2.9139 mL | 5.8278 mL | |
| 10 mM | 0.2914 mL | 1.4570 mL | 2.9139 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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