| Identification | Back Directory | [Name]
nAChR agonist1 | [CAS]
1394371-75-5 | [Synonyms]
nAChR agonist1
nAChR agonist 1(DUN71755)
Benzenesulfonamide, 4-[5-(4-chlorophenyl)-4-methyl-2-(1-oxopropyl)-3-thienyl]- | [Molecular Formula]
C20H18ClNO3S2 | [MDL Number]
MFCD32671353 | [MOL File]
1394371-75-5.mol | [Molecular Weight]
419.94 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
9.93±0.10(Predicted) | [color ]
Off-white to yellow |
| Hazard Information | Back Directory | [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 |
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| Company Name: |
InvivoChem
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| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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