VU-0357121


Catalog No. size PriceQuantity
M6526-2 2mg solid $110
M6526-10 10mg solid $452

Description

Cas:433967-28-3

Product Information:

VU0357121 is a positive allosteric modulator of mGlu5 receptors (EC50 = 33 nM). Mutagenesis studies indicate that VU0357121 and related analogues bind to a yet uncharacterized allosteric site on mGlu(5), distinct from CPPHA, yet share a functional interaction with the MPEP site.

 

Chemical Formula: C17H17F2NO2

 

Exact Mass: 305.1227

 

Molecular Weight: 305.3248

 

Elemental Analysis: C, 66.88; H, 5.61; F, 12.44; N, 4.59; O, 10.48

 

Synonym:

 

VU-0357121

VU0357121

VU 0357121

 

Chemical Name:

4-Butoxy-N-(2,4-difluorophenyl)benzamide

 

InChi Key:

AHCYOTLTLQTPSU-UHFFFAOYSA-N

 

InChi Code:

InChI=1S/C17H17F2NO2/c1-2-3-10-22-14-7-4-12(5-8-14)17(21)20-16-9-6-13(18)11-15(16)19/h4-9,11H,2-3,10H2,1H3,(H,20,21)

 

Smiles Code:

O=C(NC1=CC=C(F)C=C1F)C2=CC=C(OCCCC)C=C2

 

 

Technical Data:

 

Appearance: White to off-white 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

 

In Vitro:

VU 0357121 has the ability to enhance glutamate sensitivity of mGlu5 is likely due to the interaction at a site on the receptor distinct from the MPEP binding site. VU 0357121 does not bind at the MPEP allosteric site of mGlu5, thus does not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU 0357121 to shift the glutamate concentration response curve, whereas the response to VU 0357121 is not altered by the F585I/rmGlu5 mutation. VU 0357121 shows weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line.

 

 

References:

  1. Rodriguez AL, Tarr JC, Zhou Y, Williams R, Gregory KJ, Bridges TM, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR. Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu(5). 2012 Dec 17 [updated 2013 Mar 22]. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. Available from http://www.ncbi.nlm.nih.gov/books/NBK154499/ PubMed PMID: 24027804.

 

  1. Hammond AS, Rodriguez AL, Townsend SD, Niswender CM, Gregory KJ, Lindsley CW, Conn PJ. Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology. ACS Chem Neurosci. 2010 Oct 20;1(10):702-716. Epub 2010 Aug 19. PubMed PMID: 20981342; PubMed Central PMCID: PMC2957851.

 

Products are for research use only. Not for human use.

Payment & Security

American Express Apple Pay Diners Club Discover Elo Google Pay JCB Mastercard PayPal Shop Pay Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed