| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 100mg |
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nAChR agonist 1 is a novel, brain-permeable, and orally bioavailable positive allosteric modulator (PAM) 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.
| ln Vivo |
Acute (single dose) oral treatment of compound 28, a nAChR agonist, before memory acquisition greatly exacerbated the latency and scopolamine-induced 8 amnesia in male Wistar rats at dose levels of 1 and 3 mg/kg. When given right after memory acquisition trials, nAChR agonist 1 also markedly increased discrimination index in memory consolidation paradigms [1]. AUC, Cmax, and F values for nAChR agonist 1 therapy (10 mg/kg; oral) were 63 h μM, 2.3 μM, and 63%, respectively [1]. AUC, Cmax, T1/2, CL, and Vss for nAChR agonist 1 (1 mg/kg; IV) treatment were 1.3 h μM, 0.9 μM, 1.4 h, 31 mL/min/kg, and 3 L/kg, respectively. [1].
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| Animal Protocol |
Animal/Disease Models: Male balb/c (Bagg ALBino) mouse [1]
Doses: 10 mg/kg Route of Administration: PO (pharmacokinetic/PK/PK analysis) Experimental Results: AUC, Cmax, and F values were 63 h μM, 2.3 μM, and 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 Relati
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| Molecular Formula |
C20H18CLNO3S2
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|---|---|
| Molecular Weight |
419.938
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| Exact Mass |
419.0417
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| Elemental Analysis |
C, 57.20 H, 4.32 Cl, 8.44 N, 3.34 O, 11.43 S, 15.27
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| CAS # |
1394371-75-5
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| Related CAS # |
1394371-75-5;
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| SMILES |
NS(C1=CC=C(C2=C(C(CC)=O)SC(C3=CC=C(Cl)C=C3)=C2C)C=C1)(=O)=O
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| InChi Key |
DYIIYIJHDMIABW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H18ClNO3S2/c1-3-17(23)20-18(13-6-10-16(11-7-13)27(22,24)25)12(2)19(26-20)14-4-8-15(21)9-5-14/h4-11H,3H2,1-2H3,(H2,22,24,25)
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| Chemical Name |
4-(5-(4-chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide
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| Synonyms |
nAChR agonist 1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~297.66 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.95 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3813 mL | 11.9065 mL | 23.8129 mL | |
| 5 mM | 0.4763 mL | 2.3813 mL | 4.7626 mL | |
| 10 mM | 0.2381 mL | 1.1906 mL | 2.3813 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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