2. GPCR/G Protein Neuronal Signaling
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  4. 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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LY2934747

LY2934747 Chemical Structure

CAS No. : 1448707-43-4

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Description

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[1].

IC50 & Target[1]

mGlu2 Receptor

 

mGluR3R

 

In Vitro

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.

LY2934747 Related Antibodies
Parmacokinetics
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 % / / /
In Vivo

LY2934747 (0.3-10 mg/kg; i.p.; single dose) dose-dependently attenuates phencyclidine (PCP)-induced hyperactivity in rats[1].
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.

Animal Model: Sprague-Dawley (male, 175-250 g)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.p.; single dose (4 hours prior to PCP challenge)
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.
Animal Model: Sprague-Dawley (male, 200-240 g)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.p.; single dose (60 minutes prior to formalin injection)
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.
Animal Model: Sprague-Dawley (male)[1]
Dosage: 3 mg/kg; 10 mg/kg
Administration: i.p.; single dose (1, 2, or 3 hours prior to testing)
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.
Molecular Weight

211.22

Formula

C10H13NO4
CAS No.
SMILES

C(O)(=O)[C@H]1[C@@]2(C3(C[C@](C(O)=O)(N)[C@@]21[H])CC3)[H]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LY2934747 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LY29347471448707-43-4LY 2934747LY-2934747mGluRMetabotropic glutamate receptorsmGlu2 receptorspainmGlu receptor subtypesmGlu2 receptormGlu3 receptorCNS targetsrat cortical mGlu2/3 receptorsInhibitorinhibitorinhibit

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