JNJ 16259685
Tocris Bioscience, part of Bio-Techne | Catalog # 2333
Highly potent, mGlu1-selective non-competitive antagonist
Key Product Details
Description
Highly potent, mGlu1-selective non-competitive antagonist
Product Description
JNJ 16259685 is a sub-nanomolar potent, non-competitive mGlu1 antagonist (Ki = 0.34 nM). Inhibits glutamate-induced Ca2+ response at the human mGlu1 receptor with an IC50 value of 0.55 nM. Selective over mGlu5 (> 400-fold) and displays no activity at mGlu2, mGlu3, mGlu4, mGlu6, AMPA or NMDA receptors (IC50 > 10 μM). Centrally active following systemic administration.Product Specifications
Molecular Weight
325.41
Formula
C20H23NO3
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
(3,4-Dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-(cis-4-methoxycyclohexyl)-methanone
CAS Number
409345-29-5
PubChem ID
11313361
InChI Key
QOTAQTRFJWLFCR-UHFFFAOYSA-N
SMILES
O=[C@@]([C@@H]4CC[C@H](OC)CC4)C(C=C3)=CC1=C3N=C(OCCC2)C2=C1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 8.14 | 25 | |
| Ethanol | 32.54 | 100 |
Preparing Stock Solutions
for JNJ 16259685
The following data is based on the product molecular weight 325.41
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.07 mL | 15.37 mL | 30.73 mL |
| 5 mM | 0.61 mL | 3.07 mL | 6.15 mL |
| 10 mM | 0.31 mL | 1.54 mL | 3.07 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.61 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Xie Effects of mGluR1 antagonism in the dorsal hippocampus on drug context-induced reinstatement of cocaine-seeking behavior in rats. Psychopharmacology (Berl). 2010 PMID: 19847405
- Mabire Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists. J.Med.Chem. 2005 PMID: 15771457
- Steckler Metabotropic glutamate receptor 1 blockade impairs acquisition and retention in a spatial water maze task. Behav.Brain Res. 2005 PMID: 16043241
- Lavreysen JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist. Neuropharmacology 2004 PMID: 15555631
Product Specific Notices for JNJ 16259685
For research use only
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