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nAChR agonist1

Product Name
nAChR agonist1
CAS No.
1394371-75-5
Chemical Name
nAChR agonist1
Synonyms
DUN71755;nAChR agonist1;nAChR agonist 1(DUN71755);nAChR agonist 1, 10 mM in DMSO;4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide;4-[5-(4-chlorophenyl)-4-methyl-2-propanoylthiophen-3-yl]benzene-1-sulfonamide;Benzenesulfonamide, 4-[5-(4-chlorophenyl)-4-methyl-2-(1-oxopropyl)-3-thienyl]-;nAChR agonist1,nAChR agonist-1,Inhibitor,brain-permeable,oral,disease,nAChR,inhibit,nAChR agonist 1,cells,neuroblastoma,Alzheimer’s,deficits,cognitive,Nicotinic acetylcholine receptors
CBNumber
CB56171370
Molecular Formula
C20H18ClNO3S2
Formula Weight
419.94
MOL File
1394371-75-5.mol
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nAChR agonist1 Property

Boiling point:
575.2±60.0 °C(Predicted)
Density 
1.334±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO : 125 mg/mL (297.66 mM; Need ultrasonic)
pka
9.93±0.10(Predicted)
form 
Solid
color 
Off-white to yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0109394
Product name
nAChRagonist1
Purity
98.02%
Packaging
5mg
Price
$450
Updated
2021/12/16
ChemScene
Product number
CS-0109394
Product name
nAChRagonist1
Purity
98.02%
Packaging
10mg
Price
$800
Updated
2021/12/16
ChemScene
Product number
CS-0109394
Product name
nAChRagonist1
Purity
98.02%
Packaging
25mg
Price
$1650
Updated
2021/12/16
ChemScene
Product number
CS-0109394
Product name
nAChRagonist1
Purity
98.02%
Packaging
50mg
Price
$2550
Updated
2021/12/16
DC Chemicals
Product number
012753
Product name
nAChRagonist1(DUN71755)
Packaging
001
Price
$1000
Updated
2021/12/16
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nAChR agonist1 Chemical Properties,Usage,Production

Uses

nAChR agonist 1 is a potent,?brain-permeable, and?orally?efficacious positive?allosteric?modulator?of α7?nicotinic?acetylcholine?receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 μM in a Ca2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease[1].

in vivo

Acute (single-dose) oral administration of nAChR agonist 1 (compound 28) prior to memory acquisition, significantly increased the discrimination index in both time-delay and scopolamine-induced 8 amnesia at 1 and 3 mg/kg dose levels in male Wistar rats.nAChR agonist 1 also significantly improved the discrimination index in the memory consolidation paradigm, when administered immediately after the memory acquisition trial[1].
nAChR agonist 1 treatment (10 mg/kg; p.o.) shows that the AUC, Cmax, and F values are 63 h μM, 2.3 μM, 63%, respectively[1].
nAChR agonist 1 (1 mg/kg; i.v.) treatment shows that the AUC, Cmax,T1/2, CL, and Vss are 1.3 h μM, 0.9 μM, 1.4 hours, 31 mL/min/kg, 3 L/kg, respectively[1].

Animal Model:Male BALB/c mice[1]
Dosage:10 mg/kg
Administration:p.o.(Pharmacokinetic?Analysis)
Result:The AUC, Cmax, and F values are 63 h μM, 2.3 μM, 63%, respectively.

References

[1] Sinha N, et al.Discovery?of?Novel,?Potent,?Brain-Permeable, and?Orally?Efficacious?Positive?Allosteric?Modulator?of α7?Nicotinic?Acetylcholine?Receptor?[4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide]: Structure-Activity Relationship and Preclinical Characterization. J Med Chem.?2020 Feb 13;63(3):944-960. DOI:10.1021/acs.jmedchem.9b01569

nAChR agonist1 Preparation Products And Raw materials

Raw materials

Preparation Products

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nAChR agonist1 Suppliers

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1394371-75-5, nAChR agonist1Related Search:


  • nAChR agonist1
  • Benzenesulfonamide, 4-[5-(4-chlorophenyl)-4-methyl-2-(1-oxopropyl)-3-thienyl]-
  • nAChR agonist 1(DUN71755)
  • DUN71755
  • 4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide
  • nAChR agonist1,nAChR agonist-1,Inhibitor,brain-permeable,oral,disease,nAChR,inhibit,nAChR agonist 1,cells,neuroblastoma,Alzheimer’s,deficits,cognitive,Nicotinic acetylcholine receptors
  • 4-[5-(4-chlorophenyl)-4-methyl-2-propanoylthiophen-3-yl]benzene-1-sulfonamide
  • nAChR agonist 1, 10 mM in DMSO
  • 1394371-75-5