LY2389575 hydrochloride
Based on 1 Customer Validation
LY2389575 hydrochloride is a selective and noncompetitive mGlu3 negative allosteric modulator (NAM), with an IC50 value of 190 nM. LY2389575 hydrochloride induces an increase in Mrc1 levels. LY2389575 hydrochloride also independently amplifies Amyloid beta (Aβ) toxicity and can be used in study of Alzheimer's disease.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.93%
- CAS. Nr.: 885104-09-6
- Formel: C15H16BrCl3N4
- Molecular Weight:438.58
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
-
HY-103565
AMN082mGluR7 Agonist -
HY-110122
AZ 12216052mGluR8 PAM -
HY-16636
ML337mGlu3 Modulator -
HY-107507
Ro 01-6128mGluR Modulator -
HY-W015546
β-N-methylamino-L-alanine hydrochlorideNeurotoxin -
HY-102095
SIB-1757mGluR5 antagonist -
HY-11095
NPS 2390CaSR/mGluR1/5 Allosteric Antagonist -
HY-W011417
Cinnabarinic acidmGlu4 Agonist -
HY-14609
MPEP HydrochloridemGlu5 Receptor Antagonist -
HY-100786
DL-AP3mGluR1 Antagonist -
HY-102095R
SIB-1757 (Standard)Reference Standard -
HY-100804
L-Cysteinesulfinic acidmGluR Agonist
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
mGluR3 190 nM (IC50) |
In Vitro
LY2389575 hydrochloride (5 μM; 1 h) induces an increase in Mrc1 levels in microglial cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:Microglial cells
-
Concentration:5 μM
-
Incubation Time:1 h
-
Result:Increased levels of Mrc1.
Chemical Information
-
CAS. Nr. 885104-09-6
-
Appearance Solid
-
Molecular Weight 438.58
-
Formel C15H16BrCl3N4
-
Color White to light yellow
-
SMILES
ClC1=CC=C(CN[C@@H]2CN(C3=NC=C(Br)C=N3)CC2)C(Cl)=C1.[H]Cl
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (228.01 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Methanol : 8.33 mg/mL (18.99 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Amyloid: Congo Red Amyloid Staining
Congo red amyloid staining is a histochemical method used to detect extracellular amyloid deposits in tissue sections based on the affinity of Congo red dye for β-pleated sheet-rich protein aggregates. When bound to amyloid, Congo red produces characteristic apple-green birefringence under polarized light microscopy, which is widely regarded as a diagnostic feature of amyloid deposition in histopathology. The diagnostic principle relies on the combination of dye binding (congophilia) and optical anisotropy under polarized illumination, which distinguishes amyloid from most non-amyloid eosinophilic extracellular deposits in routine histological evaluation. Amyloid identification by Congo red staining remains a cornerstone in diagnostic pathology despite the availability of adjunct methods such as immunohistochemistry and mass spectrometry, particularly because of its ability to localize deposits directly within tissue architecture. The specificity of Congo red-positive deposits is incre
-
Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Reinheit & Dokumentation
-
Data Sheet (273 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
Verweise
[1]. Caraci F, et al. Targeting group II metabotropic glutamate (mGlu) receptors for the treatment of psychosis associated with Alzheimer's disease: selective activation of mGlu2 receptors amplifies beta-amyloid toxicity in cultured neurons, whereas dual activation of mGlu2 and mGlu3 receptors is neuroprotective. Mol Pharmacol. 2011 Mar;79(3):618-26. [Content Brief]
[2]. Zinni M, et al. mGlu3 receptor regulates microglial cell reactivity in neonatal rats. J Neuroinflammation. 2021 Jan 6;18(1):13. [Content Brief]
[3]. Srivastava A, et al. Metabotropic Glutamate Receptors in Alzheimer's Disease Synaptic Dysfunction: Therapeutic Opportunities and Hope for the Future. J Alzheimers Dis. 2020;78(4):1345-1361. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Methanol / DMSO | 1 mM | 2.2801 mL | 11.4004 mL | 22.8009 mL | 57.0021 mL |
| 5 mM | 0.4560 mL | 2.2801 mL | 4.5602 mL | 11.4004 mL | |
| 10 mM | 0.2280 mL | 1.1400 mL | 2.2801 mL | 5.7002 mL | |
| 15 mM | 0.1520 mL | 0.7600 mL | 1.5201 mL | 3.8001 mL | |
| DMSO | 20 mM | 0.1140 mL | 0.5700 mL | 1.1400 mL | 2.8501 mL |
| 25 mM | 0.0912 mL | 0.4560 mL | 0.9120 mL | 2.2801 mL | |
| 30 mM | 0.0760 mL | 0.3800 mL | 0.7600 mL | 1.9001 mL | |
| 40 mM | 0.0570 mL | 0.2850 mL | 0.5700 mL | 1.4251 mL | |
| 50 mM | 0.0456 mL | 0.2280 mL | 0.4560 mL | 1.1400 mL | |
| 60 mM | 0.0380 mL | 0.1900 mL | 0.3800 mL | 0.9500 mL | |
| 80 mM | 0.0285 mL | 0.1425 mL | 0.2850 mL | 0.7125 mL | |
| 100 mM | 0.0228 mL | 0.1140 mL | 0.2280 mL | 0.5700 mL |
LY2389575 hydrochloride Related Classifications
HY-107509 Related Classifications
Powered by Bioz