Chemical Name: 3-[4-(Hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methylpyridine oxalate
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Functionally selective muscarinic M1 receptor agonist (EC50 values are 0.3, 5, 42, 52 and 92.5 nM at M1, M3, M5, M4 and M2 receptors respectively). Displays a complex pharmacological profile: reversible and wash-resistant binding, resulting in full agonist activity at M1; delayed wash-resistant partial agonist activity at M2; and delayed wash-resistant full agonist activity at M4. Exhibits antipsychotic activity, and improves cognitive deficits and behavioral disturbances in Alzheimer's disease and schizophrenia.
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Technical Data
M. Wt
371.46
Formula
C14H23N3OS.C2H2O4
Storage
Desiccate at +4°C
Purity
≥98% (HPLC)
CAS Number
141064-23-5
PubChem ID
18920248
InChI Key
ZJOUESNWCLASJP-UHFFFAOYSA-N
Smiles
CCCCCCOC1=NSN=C1C2=CCCN(C)C2.OC(C(O)=O)=O
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
37.15
100
ethanol
9.29
25
water
3.71
10mM with gentle warming
Preparing Stock Solutions
The following data is based on the product molecular weight 371.46. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.69 mL
13.46 mL
26.92 mL
5 mM
0.54 mL
2.69 mL
5.38 mL
10 mM
0.27 mL
1.35 mL
2.69 mL
50 mM
0.05 mL
0.27 mL
0.54 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
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References
References are publications that support the products' biological activity.
Jakubiket al (2008) Importance and prospects for design of selective muscarinic agonists. Physiol.Res. 57 S39 PMID: 18481916
Heinrichet al (2009) Pharmacological comparison of muscarinic ligands: historical versus more recent muscarinic M1-preferring receptor agonists. Eur.J.Pharmacol. 605 53 PMID: 19168056
Stanhopeet al (2001) The muscarinic receptor agonist xanomeline has an antipsychotic-like profile in the rat. J.Pharmacol.Exp.Ther. 299 782 PMID: