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GPCR&G protein

VU0357121 (433967-28-3)

VU0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes.

Not Intended for Therapeutic Use. For research use only.

CAS: 433967-28-3 Category

VU0357121 (433967-28-3) Description

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.

VU0357121 (433967-28-3) Specifications

Product Name VU0357121
Synonyms VU-0357121, VU0357121, VU 0357121
Chemical Names VU 0357121; 433967-28-3; 4-butoxy-N-(2,4-difluorophenyl)benzamide; VU0357121; CHEMBL2151790; D02VFF
Purity >98%
CAS Number 433967-28-3
Molecular Formula C17H17F2NO2
Molecular Weight 305.325 g/mol
Monoisotopic Mass 305.123 g/mol
InChIKey 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 O=C(NC1=CC=C(F)C=C1F)C2=CC=C(OCCCC)C=C2
Form Powder
Color white
Solubility  may be formulated in DMSO
Storage Temp.  −20°C
Shelf life >2 years if stored properly.
Handling Dry, dark
Application  a novel positive allosteric modulator

 


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RIDADR NONH for all modes of transport

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.
  • 2: 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.
  • 3: Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5. Rodriguez AL, Tarr JC, Zhou Y, Williams R, Gregory KJ, Bridges TM, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2012 Dec 17 [updated 2013 Mar 22]. PMID: 24027804
  • 4. Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology. Hammond AS, Rodriguez AL, Townsend SD, Niswender CM, Gregory KJ, Lindsley CW, Conn PJ. ACS Chem Neurosci. 2010 Oct 20;1(10):702-716. Epub 2010 Aug 19. PMID: 20981342

1 review for VU0357121 (433967-28-3)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The VU0357121 (433967-28-3) is high purity,also customer service is pretty nice !gotta try!!

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