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Fig. 1 · Structure
Cat. No.
A14330
CAS No.
1254977-87-1
Formula
C22H23F3N4
Mol. Weight
400.187

Documents & Downloads

JNJ 42153605

Cat. No. A14330 CAS 1254977-87-1

mGluR-2 modulator

JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 receptor.

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Biological Activity

Target & Activity

Target Activity Value
mGluR2 EC50 17 nM

Cellular Effect

Cell Line Activity Value Description Reference
CHO IC50 15 nM Binding affinity to human mGlu2R expressed in CHO cells by radioligand binding assay [PMID: 23072213]
CHO EC50 17 nM Positive allosteric modulator activity at human mGlu2R expressed in CHO cells incubated for 30 mins by [35S]GTPgammaS binding assay [PMID: 23072213]
CHO EC50 17 nM Positive allosteric modulation of human mGlu2 receptor expressed in CHO cell membranes assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method [PMID: 27579727]
CHO-K1 EC50 > 10000 nM Positive allosteric modulation at human mGlu2 receptor W773A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting metho [PMID: 27579727]
CHO-K1 EC50 23.6 nM Positive allosteric modulation at human mGlu2 receptor F776A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting metho [PMID: 27579727]
CHO-K1 EC50 27 nM Positive allosteric modulation at human mGlu2 receptor N735D mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting metho [PMID: 27579727]
CHO-K1 EC50 385 nM Positive allosteric modulation at human mGlu2 receptor F643A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting metho [PMID: 27579727]
CHO-K1 EC50 4.8 nM Positive allosteric modulation of wild-type human mGlu2 receptor expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method [PMID: 27579727]
CHO-K1 EC50 46.4 nM Positive allosteric modulation at wild type human mGlu2 receptor L732A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect preincubated for 30 mins prior to glutamate challenge measured after 30 mins by [35S]GTP-gammaS bi [PMID: 27579727]

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Specifications

Manufacturer Adooq Bioscience
Actions Modulator
CAS Number 1254977-87-1
Applications mGluR-2 modulator
Formula C22H23F3N4
Molecular Weight 400.187
SMILES
FC(c1c(ccn2c1nnc2CC1CC1)N1CCC(CC1)c1ccccc1)(F)F

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 4 mg/mL (9.98 mM)
Water Insoluble
Ethanol 10 mg/mL (24.97 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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