VU 0255035

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Cat.No. 3727 - VU 0255035 | C18H20N6O3S2 | CAS No. 1135243-19-4
Description: Highly selective muscarinic M1 antagonist
Chemical Name: N-[3-Oxo-3-[4-(4-pyridinyl)-1-piperazinyl]propyl]-2,1,3-benzothiadiazole-4-sulfonamide
Purity: ≥99% (HPLC)
Citations (4)

Biological Activity

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

M. Wt 432.52
Formula C18H20N6O3S2
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 1135243-19-4
PubChem ID 24768606
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 8.65 20

Preparing Stock Solutions

The following data is based on the product molecular weight 432.52. 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 2.31 mL 11.56 mL 23.12 mL
5 mM 0.46 mL 2.31 mL 4.62 mL
10 mM 0.23 mL 1.16 mL 2.31 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

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, supplier, selective, muscarinic, receptors, M1, antagonists, mAChR, acetylcholine, ACh, VU0255035, M1, Receptors, M1, Receptors, Tocris Bioscience

4 Citations for VU 0255035

Citations are publications that use Tocris products. Selected citations for VU 0255035 include:

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 dopamine 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

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? If so please let us know.

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