LY2934747
LY2934747 is a selective and blood-brain barrier-permeable dual mGlu2/mGlu3 receptor agonist, with Ki values of 260 nM and 177 nM, and EC50 values of 8.4 nM and 62.4 nM against human receptors, respectively. LY2934747 exhibits antipsychotic and analgesic activities in in vivo animal models. LY2934747 can be used in studies related to psychosis and pain.
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- CAS No.: 1448707-43-4
- Formule: C10H13NO4
- Masse moléculaire:211.22
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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mGlu2 Receptor |
mGluR3R |
LY2934747 has high aqueous and DMSO solubility, low MDCK permeability, minimal hepatic metabolism, no significant Cyp isoform inhibition, and high plasma unbound fraction across multiple species[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-24 | Cmax | Tmax | T1/2 | Bioavailability | C0 | CL | Vdss |
|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 5 mg/kg | i.v. | 33661 nM·h | / | / | 3.6 h | / | 76749 nM | 11.8 mL/min/kg | 0.57 L/kg |
| Rat[1] | 5 mg/kg | p.o. | 2826 nM·h | 530 nM | 2 h | 3.8 h | 8 % | / | / | / |
| Rat[1] | 1 mg/kg | i.p. | 3050 nM·h | 3580 nM | 0.5 h | 1.1 h | 45 % | / | / | / |
| Rat[1] | 3 mg/kg | i.p. | 7310 nM·h | 10300 nM | 0.5 h | 0.4 h | 36 % | / | / | / |
| Rat[1] | 10 mg/kg | i.p. | 48500 nM·h | 59000 nM | 0.4 h | 1.5 h | 72 % | / | / | / |
LY2934747 (0.3-10 mg/kg; i.p.; single dose) dose-dependently inhibits formalin-induced nociceptive responses in rats, with an ED50 of 0.7 mg/kg[1].
LY2934747 (0.3-10 mg/kg; intraperitoneal injection; single dose) induces motor incoordination in rats at the dose of 10 mg/kg, while this effect is not observed at the dose of 3 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 175-250 g)[1]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:i.p.; single dose (4 hours prior to PCP challenge)
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Result:Produced a dose-related reduction in horizontal ambulations.
Achieved statistically significant effects (p < 0.05) at 3 mg/kg and 10 mg/kg.
Reached a calculated ED50 of 1.5 mg/kg.
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Animal Model:Sprague-Dawley (male, 200-240 g)[1]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:i.p.; single dose (60 minutes prior to formalin injection)
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Result:Produced a dose-related decrease in nociceptive responses in both the early (0-5 minutes) and late (11-40 minutes) phases.
Achieved statistically significant effects at 1 mg/kg, 3 mg/kg, and 10 mg/kg.
Reached a calculated ED50 of 0.7 mg/kg.
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Animal Model:Sprague-Dawley (male)[1]
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Dosage:3 mg/kg; 10 mg/kg
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Administration:i.p.; single dose (1, 2, or 3 hours prior to testing)
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Result:Produced statistically significant locomotor impairment at 10 mg/kg when tested 1, 2, and 3 hours post-administration.
Caused no impairment at the 3 mg/kg dose at any time point.
Chemical Information
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CAS No. 1448707-43-4
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Masse moléculaire 211.22
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Formule C10H13NO4
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SMILES
C(O)(=O)[C@H]1[C@@]2(C3(C[C@](C(O)=O)(N)[C@@]21[H])CC3)[H]
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Monn JA, et al. Synthesis and pharmacological characterization of C4-disubstituted analogs of 1S,2S,5R,6S-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylate: identification of a potent, selective metabotropic glutamate receptor agonist and determination of agonist-bound human mGlu2 and mGlu3 amino terminal domain structures. J Med Chem. 2015 Feb 26;58(4):1776-94. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LY2934747 Related Classifications
HY-131288 Related Classifications
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