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Anle138b 

Cat. No.: HY-101855 Purity: >98.0%
Data Sheet SDS Handling Instructions

Anle138b is a novel oligomer modulator.

For research use only. We do not sell to patients.
Anle138b Chemical Structure

Anle138b Chemical Structure

CAS No. : 882697-00-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $66 In-stock
5 mg $60 In-stock
10 mg $100 In-stock
25 mg $220 In-stock
50 mg $390 In-stock
100 mg $690 In-stock
200 mg $1200 In-stock
500 mg   Get quote  
1 g   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Anle138b is a novel oligomer modulator.

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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.9140 mL 14.5700 mL 29.1401 mL
5 mM 0.5828 mL 2.9140 mL 5.8280 mL
10 mM 0.2914 mL 1.4570 mL 2.9140 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Anle138b is prepared in DMSO/peanut butter.

Mouse: 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

343.17

Formula

C₁₆H₁₁BrN₂O₂

CAS No.

882697-00-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Anle138b
Cat. No.:
HY-101855
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