LY 2389575 hydrochloride |
| Katalog-Nr.GC14722 |
negative allosteric modulator of mGlu3
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 885104-09-6
Sample solution is provided at 25 µL, 10mM.
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LY2389575 is described here instead of LY2389575 hydrochloride. LY2389575 is a selective negative allosteric modulator (NAM) of metabotropic glutamate receptor 3 (mGlu3) with an IC50 value of 4.2 μM [1].
The metabotropic glutamate receptors (mGlus) are members of the GPCR family C. They are characterized by a large extracellular amino-terminal domain for binding agonist. Eight mGlus had been found and were assigned to three groups based on their pharmacology, sequence homology, and mechanisms to couple to effector. They are Group I: mGlu1 and mGlu5; Group II: mGlu2 and mGlu3; Group III: mGlu4,6,7,8 [1].
In mixed neuronal cultures, LY2389575 abolished the protective activity of 1 μM LY379268 (the orthosteric mGlu2/3 receptor agonist) in the concentration range of 0.1 to 1 μM and amplified Aβ toxicity on its own at the highest concentration. In the absence of Aβ, LY2389575 at these concentrations was not toxic (numbers of dead neurons in control cultures and in cultures treated with 1 μM LY2389575 were 41 ± 3, and 42 ± 1, respectively). Further data indicated that LY2389575 was able to amplify Aβ toxicity and abolish the neuroprotective activity of LY379268 only in cultures containing wild-type astrocytes. In the FLIPR assay system, LY2389575 behaved as a noncompetitive mGlu3 receptor antagonist with an efficacy of 100 ± 0.68% and an IC50 value of 190 ± 26 nM. LY2389575 failed in affecting responses mediated by all other mGlu receptor subtypes or GABAB receptors [2].
No in vivo data for the application of this drug had been found.
References:
[1]. Sheffler DJ, Wenthur CJ, Bruner JA, et al. Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM[J]. Bioorganic & medicinal chemistry letters, 2012, 22(12): 3921-3925.
[2]. Caraci F, Molinaro G, Battaglia G, 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 β-Amyloid Toxicity in Cultured Neurons, Whereas Dual Activation of mGlu2 and mGlu3 Receptors Is Neuroprotective[J]. Molecular pharmacology, 2011, 79(3): 618-626.
| Cas No. | 885104-09-6 | SDF | |
| Chemical Name | (S)-1-(5-bromopyrimidin-2-yl)-N-(2,4-dichlorobenzyl)pyrrolidin-3-amine hydrochloride | ||
| Canonical SMILES | BrC1=CN=C(N2CC[C@@](NCC3=C(Cl)C=C(Cl)C=C3)([H])C2)N=C1.Cl | ||
| Formula | C15H15BrCl2N4.HCl | M.Wt | 438.58 |
| Löslichkeit | <8.77mg/ml in DMSO | Storage | Desiccate at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2801 mL | 11.4004 mL | 22.8009 mL |
| 5 mM | 0.456 mL | 2.2801 mL | 4.5602 mL |
| 10 mM | 0.228 mL | 1.14 mL | 2.2801 mL |
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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