Synonym
LSN2463359; LSN-2463359; LSN 2463359.
IUPAC/Chemical Name
N-(propan-2-yl)-5-[2-(pyridin-4-yl)ethynyl]pyridine-2-carboxamide
InChi Key
STAFRSGTRKNXHF-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H15N3O/c1-12(2)19-16(20)15-6-5-14(11-18-15)4-3-13-7-9-17-10-8-13/h5-12H,1-2H3,(H,19,20)
SMILES Code
O=C(C1=NC=C(C#CC2=CC=NC=C2)C=C1)NC(C)C
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
A brain penetrant positive allosteric modulator of the mGluR5.
In vivo activity:
In addition, LSN2463359 was found to selectively attenuate reversal learning deficits observed in the neurodevelopmental MAM E17 rat model but not in the acute phencyclidine (PCP) model.
Reference: Neuropharmacology. 2013 Jan;64:240-7. https://pubmed.ncbi.nlm.nih.gov/22884612/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMF |
30.0 |
113.07 |
| DMSO |
30.0 |
113.07 |
| Ethanol |
30.0 |
113.07 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
265.32
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Gastambide F, Gilmour G, Robbins TW, Tricklebank MD. The mGlu₅ positive allosteric modulator LSN2463359 differentially modulates motor, instrumental and cognitive effects of NMDA receptor antagonists in the rat. Neuropharmacology. 2013 Jan;64:240-7. doi: 10.1016/j.neuropharm.2012.07.039. Epub 2012 Aug 1. PMID: 22884612.
2. Gilmour G, Broad LM, Wafford KA, Britton T, Colvin EM, Fivush A, Gastambide F, Getman B, Heinz BA, McCarthy AP, Prieto L, Shanks E, Smith JW, Taboada L, Edgar DM, Tricklebank MD. In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat. Neuropharmacology. 2013 Jan;64:224-39. doi: 10.1016/j.neuropharm.2012.07.030. Epub 2012 Aug 1. PMID: 22884720.
In vivo protocol:
1. Gastambide F, Gilmour G, Robbins TW, Tricklebank MD. The mGlu₅ positive allosteric modulator LSN2463359 differentially modulates motor, instrumental and cognitive effects of NMDA receptor antagonists in the rat. Neuropharmacology. 2013 Jan;64:240-7. doi: 10.1016/j.neuropharm.2012.07.039. Epub 2012 Aug 1. PMID: 22884612.
2. Gilmour G, Broad LM, Wafford KA, Britton T, Colvin EM, Fivush A, Gastambide F, Getman B, Heinz BA, McCarthy AP, Prieto L, Shanks E, Smith JW, Taboada L, Edgar DM, Tricklebank MD. In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat. Neuropharmacology. 2013 Jan;64:224-39. doi: 10.1016/j.neuropharm.2012.07.030. Epub 2012 Aug 1. PMID: 22884720.
1: Gilmour G, Broad LM, Wafford KA, Britton T, Colvin EM, Fivush A, Gastambide F, Getman B, Heinz BA, McCarthy AP, Prieto L, Shanks E, Smith JW, Taboada L, Edgar DM, Tricklebank MD. In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat. Neuropharmacology. 2013 Jan;64:224-39. doi: 10.1016/j.neuropharm.2012.07.030. PubMed PMID: 22884720.
2: Gastambide F, Gilmour G, Robbins TW, Tricklebank MD. The mGlu₅ positive allosteric modulator LSN2463359 differentially modulates motor, instrumental and cognitive effects of NMDA receptor antagonists in the rat. Neuropharmacology. 2013 Jan;64:240-7. doi: 10.1016/j.neuropharm.2012.07.039. PubMed PMID: 22884612.
3: Gastambide F, Cotel MC, Gilmour G, O'Neill MJ, Robbins TW, Tricklebank MD. Selective remediation of reversal learning deficits in the neurodevelopmental MAM model of schizophrenia by a novel mGlu5 positive allosteric modulator. Neuropsychopharmacology. 2012 Mar;37(4):1057-66. doi: 10.1038/npp.2011.298. PubMed PMID: 22129780; PubMed Central PMCID: PMC3280638.
