JNJ 16259685CAS: 409345-29-5
MF: C20H23NO3
MW: 325.4
A non-compeitive antagonist at the mGluR-1.

JNJ 16259685 (CAS 409345-29-5)

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Synonym: (3,4-Dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-(cis-4-methoxycyclohexyl)-methanone
Application: A non-compeitive antagonist at the mGluR-1
CAS Number: 409345-29-5
Purity: ≥98%
Molecular Weight: 325.4
Molecular Formula: C20H23NO3
* Refer to Certificate of Analysis for lot specific data (including water content).
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JNJ 16259685 is a sub-nanomolar potent, non-competitive mGluR-1 antagonist (Ki=0.34nM). Inhibits glutamate-induced Ca2+ response at the human mGluR-1 (IC50=0.55nM). Selective over mGluR-5 (>400-fold). Displays no activity at mGluR-2, mGluR-3, mGluR-4, mGluR-6, AMPA or NMDA receptors (IC50 > 10 μM). JNJ 16259685 is an inhibitor of mGluR-1a and mGluR-1b.


References

1. Lavreysen, H., et al. 2004. Neuropharmacology. 47: 961-972. PMID: 15555631
2. Steckler, T., et al. 2005. Psychopharmacology. 179: 198-206. PMID: 15821950
3. Steckler, T., et al. 2005. Behav. Brain. Res. 164: 52-60. PMID: 16043241
4. Mabire, D., et al. 2005. J. Med. Chem. 48: 2134-2153. PMID: 15771457
5. Fukunaga, I., et al. 2007. Br. J. Pharmacol. 151: 870-876. PMID: 17502847
6. Knöpfel, T., 2007. Br. J. Pharmacol. 151: 723-724. PMID: 17502846

Physical State :
Solid
Solubility :
Soluble in ethanol (100 mM), and DMSO (25 mM).
Storage :
Store at 4° C
Boiling Point :
~502.51° C at 760 mmHg (Predicted)
Density :
~1.21 g/cm3 (Predicted)
Refractive Index :
n20D 1.60 (Predicted)
IC50 :
mGluR-1a: IC50 = 0.55 nM (human); Metabotropic glutamate receptor 1: IC50 = 3 nM (rat); human: IC50 = 73 nM
Ki Data :
mGlu1: Ki= 0.34 nM
pK Values :
pKb: 2.6 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
11313361
MDL Number :
MFCD08690525
SMILES :
COC1CCC(CC1)C(=O)C2=CC3=CC4=C(N=C3C=C2)OCCC4

Download SDS (MSDS)

Certificate of Analysis

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