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Submit ReviewVU 0255035
Description: Highly selective M1 antagonist
Chemical Name: N-[3-Oxo-3-[4-(4-pyridinyl)-1-piperazinyl]propyl]-2,1,3-benzothiadiazole-4-sulfonamide
Purity: ≥99% (HPLC)
Biological Activity for VU 0255035
VU 0255035 is a highly selective muscarinic M1 antagonist (Ki = 14.87 nM). Targets the M1 orthosteric site with greater than 75-fold selectivity over the other receptor subtypes. Reduces pilocarpine-induced seizures in mice. Brain penetrant.
Technical Data for VU 0255035
| M. Wt | 432.52 |
| Formula | C18H20N6O3S2 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1135243-19-4 |
| PubChem ID | 24768606 |
| InChI Key | WXDHQWPQLKGANZ-UHFFFAOYSA-N |
| Smiles | O=C(CCNS(C4=CC=CC3=NSN=C34)(=O)=O)N(CC2)CCN2C1=CC=NC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for VU 0255035
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 8.65 | 20 |
Preparing Stock Solutions for VU 0255035
The following data is based on the product molecular weight 432.52. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 11.56 mL | 57.8 mL | 115.6 mL |
| 1 mM | 2.31 mL | 11.56 mL | 23.12 mL |
| 2 mM | 1.16 mL | 5.78 mL | 11.56 mL |
| 10 mM | 0.23 mL | 1.16 mL | 2.31 mL |
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Product Datasheets for VU 0255035
References for VU 0255035
References are publications that support the biological activity of the product.
Sheffler et al (2009) A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning. Mol.Pharmacol. 76 356 PMID: 19407080
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Keywords: VU 0255035, VU 0255035 supplier, selective, muscarinic, receptors, M1, antagonists, mAChR, acetylcholine, ACh, VU0255035, Receptors, 3727, Tocris Bioscience
6 Citations for VU 0255035
Citations are publications that use Tocris products. Selected citations for VU 0255035 include:
James M et al (2022) Cholinergic control of striatal GABAergic microcircuits. Cell Rep 41 111531 PMID: 36288709
Urrunaga et al (2015) M1 muscarinic receptors modify oxidative stress response to acetaminophen-induced acute liver injury. Proc Natl Acad Sci U S A 78 66 PMID: 25452146
Shin et al (2015) Muscarinic regulation of DA and glutamate transmission in the nucleus accumbens. Front Cell Neurosci 112 8124 PMID: 26080439
Martin et al (2015) Endocannabinoids Mediate Muscarinic Acetylcholine Receptor-Dependent Long-Term Depression in the Adult Medial Prefrontal Cortex. Mar Drugs 9 457 PMID: 26648844
Zhu et al (2017) Impairments of spatial memory in an Alzheimer's disease model via degeneration of hippocampal cholinergic synapses. Nat Commun 8 1676 PMID: 29162816
Rachakonda et al (2015) M1 Muscarinic Receptor Deficiency Attenuates Azoxymethane-Induced Chronic Liver Injury in Mice. Sci Rep 5 14110 PMID: 26374068
Do you know of a great paper that uses VU 0255035 from Tocris? Please let us know.
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