VU 0650786

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MedKoo CAT#: 571267

CAS#: NONE

Description: VU 0650786 is a mGlu3 negative allosteric modulator. VU 0650786 has an mGlu2 IC50 of greater than 30 uM and mGlu3 IC50 of 392 nM, suggesting that it is highly selective for mGlu2 and mGlu3.

Chemical Structure

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VU 0650786
CAS# NONE
Instruction

Theoretical Analysis

MedKoo Cat#: 571267
Name: VU 0650786
CAS#: NONE
Chemical Formula: C18H15ClFN5O2
Exact Mass: 387.09
Molecular Weight: 387.800
Elemental Analysis: C, 55.75; H, 3.90; Cl, 9.14; F, 4.90; N, 18.06; O, 8.25

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: VU 0650786; VU-0650786; VU0650786

IUPAC/Chemical Name: (R)-2-(((5-chloropyridin-2-yl)oxy)methyl)-5-(2-fluoropyridin-3-yl)-7-methyl-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one

InChi Key: RXRVCJFGSOVYLG-LLVKDONJSA-N

InChi Code: InChI=1S/C18H15ClFN5O2/c1-11-9-24(14-3-2-6-21-17(14)20)18(26)15-7-13(23-25(11)15)10-27-16-5-4-12(19)8-22-16/h2-8,11H,9-10H2,1H3/t11-/m1/s1

SMILES Code: ClC1=CC=C(OCC2=NN([C@H](C)CN(C3=C(F)N=CC=C3)C4=O)C4=C2)N=C1

Appearance: Solid powder

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

More Info: Negative allosteric modulators (NAM) are molecules of interest in treating depression-related behaviors, as potentially novel antidepressants.

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 387.80 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.

Recalculate based on batch purity %
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:
In vitro protocol:
In vivo protocol:

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1: Engers JL, Bollinger KA; Weiner RL, Rodriguez AL, Long MF, Breiner MM, Chang S, Bollinger SR, Bubser M, Jones CK, Morrison RD, Bridges TM, Blobaum AL, Niswender CM, Conn JP, Emmitte KA, Lindsley CW. Design and Synthesis of N‑Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs. ACS Med Chem. 2017 Aug 15. doi: 10.1021/acsmedchemlett.7b00249. [Epub ahead of print].

2: Engers JL, Rodriguez AL, Konkol LC, Morrison RD, Thompson AD, Byers FW, Blobaum AL, Chang S, Venable DF, Loch MT, Niswender CM, Daniels JS, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents. J Med Chem. 2015 Sep 24;58(18):7485-500. doi: 10.1021/acs.jmedchem.5b01005. Epub 2015 Sep 10. PubMed PMID: 26335039; PubMed Central PMCID: PMC4809247.

3: Walker AG, Sheffler DJ, Lewis AS, Dickerson JW, Foster DJ, Senter RK, Moehle MS, Lv X, Stansley BJ, Xiang Z, Rook JM, Emmitte KA, Lindsley CW, Conn PJ. Co-Activation of Metabotropic Glutamate Receptor 3 and Beta Adrenergic Receptors Modulates Cyclic-AMP, Long-Term Potentiation, and Disrupts Memory Reconsolidation. Neuropsychopharmacology. 2017 Jun 30. doi: 10.1038/npp.2017.136. [Epub ahead of print] PubMed PMID: 28664928.