VU 0255035

Pricing Availability   Qty
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)
Datasheet
Citations (6)
Reviews
Literature (1)

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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:

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

James M et al (2022) Cholinergic control of striatal GABAergic microcircuits. Cell Rep 41 111531 PMID: 36288709

Rachakonda et al (2015) M1 Muscarinic Receptor Deficiency Attenuates Azoxymethane-Induced Chronic Liver Injury in Mice. Sci Rep 5 14110 PMID: 26374068

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


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Literature in this Area

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