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VU0483605

Product Name
VU0483605
CAS No.
1623101-11-0
Chemical Name
VU0483605
Synonyms
VU0483605;VU0483605, 10 mM in DMSO;3-Chloro-N-(3-chloro-4-(4-chloro-1,3-dioxoisoindolin-2-yl)phenyl)picolinamide;3-chloro-N-[3-chloro-4-(4-chloro-1,3-dioxoisoindol-2-yl)phenyl]pyridine-2-carboxamide;2-Chloro-N-[3-chloro-4-(4-chloro-1,3-dioxo-1,3-dihydro-isoindol-2-yl)phenyl]nicotinamide;3-Chloro-N-[3-chloro-4-(4-chloro-1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)phenyl]-2-pyridinecarboxamide;3-chloro-N-[3-chloro-4-(4-chloro-1,3-dioxo-2,3-dihydro-1H-isoindol-2-yl)phenyl]pyridine-2-carboxamide;2-Pyridinecarboxamide, 3-chloro-N-[3-chloro-4-(4-chloro-1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)phenyl]-;Inhibitor,inhibit,VU0483605,Metabotropic glutamate receptors,allosteric modulator,brain penetrant,metabotropic glutamate,VU 0483605,mGluR,VU-0483605
CBNumber
CB63067594
Molecular Formula
C20H10Cl3N3O3
Formula Weight
446.67
MOL File
1623101-11-0.mol
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VU0483605 Property

Density 
1.625±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
≤20mg/ml in DMSO;20mg/ml in dimethyl formamide
form 
crystalline solid
pka
9.39±0.70(Predicted)
color 
Light yellow to orange
InChI
InChI=1S/C20H10Cl3N3O3/c21-12-4-1-3-11-16(12)20(29)26(19(11)28)15-7-6-10(9-14(15)23)25-18(27)17-13(22)5-2-8-24-17/h1-9H,(H,25,27)
InChIKey
HJQXPBKPTGWZCF-UHFFFAOYSA-N
SMILES
C1(C(NC2=CC=C(N3C(=O)C4=C(C3=O)C=CC=C4Cl)C(Cl)=C2)=O)=NC=CC=C1Cl
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
16941
Product name
VU0483605
Purity
≥98%
Packaging
1mg
Price
$49
Updated
2024/03/01
Cayman Chemical
Product number
16941
Product name
VU0483605
Purity
≥98%
Packaging
5mg
Price
$96
Updated
2024/03/01
Cayman Chemical
Product number
16941
Product name
VU0483605
Purity
≥98%
Packaging
10mg
Price
$143
Updated
2024/03/01
TRC
Product number
V787575
Product name
VU0483605
Packaging
50mg
Price
$550
Updated
2021/12/16
ApexBio Technology
Product number
C5611
Product name
VU0483605
Packaging
10mg
Price
$171
Updated
2021/12/16
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VU0483605 Chemical Properties,Usage,Production

Uses

VU 0483605 is a positive allosteric modulator of metabotropic glutamate receptors (mGluRs) that preferentially binds mGlu1 over mGlu4 (1,2). VU 0483605 is a mGlu1 antagonist and has potential therapeutic properties for treating schizophrenia.

Biological Activity

vu0483605 is a selective positive allosteric modulator (pam) of mglur1 [1].the metabotropic glutamate receptors (mglurs), members of g-protein-coupled receptors, have been involved in a variety of functions in the central and peripheral nervous systems, such as learning, memory, anxiety, and the perception of pain. the mglurs exist in pre- and postsynaptic neurons in synapses of the hippocampus, cerebellum, the cerebral cortex, as well as other parts of the brain and in peripheral tissues. mice deficient in mglur1 showed severe motor coordination and spatial learning deficient [2].vu0483605 is a selective positive allosteric modulator (pam) of mglur1. vu0483605 displayed ec50 values of 0.39 and 0.36 μm at human and rat mglur1 receptors, respectively. vu0483605 showed no activity against mglu4 pam with the ec50 of >10 μm. vu0483605 potentiated the response to glutamate in cells stably expressing mglu1 and partially restored the reduction in glutamate-mediated calcium signaling in a mutant cell model of schizophrenia [1].

IC 50

Human mGluR1: 390 nM (EC50); rat mGluR1: 356 nM (EC50); Human mGlu4: >10 μM (EC50)

References

[1] cho h p, garcia-barrantes p m, brogan j t, et al. chemical modulation of mutant mglu1 receptors derived from deleterious grm1 mutations found in schizophrenics[j]. acs chemical biology, 2014, 9(10): 2334-2346.
[2] conquet f, bashir z i, davies c h, et al. motor deficit and impairment of synaptic plasticity in mice lacking mglur1[j]. nature, 1994, 372(6503): 237.

VU0483605 Preparation Products And Raw materials

Raw materials

Preparation Products

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VU0483605 Suppliers

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1623101-11-0, VU0483605Related Search:


  • VU0483605
  • 2-Chloro-N-[3-chloro-4-(4-chloro-1,3-dioxo-1,3-dihydro-isoindol-2-yl)phenyl]nicotinamide
  • 3-Chloro-N-(3-chloro-4-(4-chloro-1,3-dioxoisoindolin-2-yl)phenyl)picolinamide
  • 3-Chloro-N-[3-chloro-4-(4-chloro-1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)phenyl]-2-pyridinecarboxamide
  • 2-Pyridinecarboxamide, 3-chloro-N-[3-chloro-4-(4-chloro-1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)phenyl]-
  • 3-chloro-N-[3-chloro-4-(4-chloro-1,3-dioxo-2,3-dihydro-1H-isoindol-2-yl)phenyl]pyridine-2-carboxamide
  • 3-chloro-N-[3-chloro-4-(4-chloro-1,3-dioxoisoindol-2-yl)phenyl]pyridine-2-carboxamide
  • Inhibitor,inhibit,VU0483605,Metabotropic glutamate receptors,allosteric modulator,brain penetrant,metabotropic glutamate,VU 0483605,mGluR,VU-0483605
  • VU0483605, 10 mM in DMSO
  • 1623101-11-0
  • C20H10Cl3N3O3