VU0255035 - ≥98%, high purity , CAS No.1135243-19-4, Antagonist of M 1 receptor;Antagonist of M 2 receptor;Antagonist of M 3 receptor;Antagonist of M 4 receptor;Antagonist of M 5 receptor

Item Number
V275278
Grouped product items
SKUSizeAvailabilityPrice Qty
V275278-2mg
2mg
In stock
$42.90
V275278-5mg
5mg
In stock
$88.90
V275278-10mg
10mg
In stock
$147.90
V275278-25mg
25mg
In stock
$310.90
V275278-50mg
50mg
In stock
$559.90
V275278-100mg
100mg
In stock
$1,007.90
V275278-250mg
250mg
In stock
$2,267.90

Highly selective, competitive muscarinic M 1 antagonist

Basic Description

SynonymsAKOS024457774 | A894354 | N-[3-oxo-3-(4-pyridin-4-ylpiperazin-1-yl)propyl]-2,1,3-benzothiadiazole-4-sulfonamide | VU0255035 hydrate | CS-0027615 | N-{3-oxo-3-[4-(pyridin-4-yl)piperazin-1-yl]propyl}-2,1,3-benzothiadiazole-4-sulfonamide | VU0255035 | BRD-K5
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsHighly selective, competitive muscarinic M 1 antagonist (K i = 14.87 nM). 75-fold selectivity over other receptor subtypes for orthosteric site. Blood-brain barrier permeable.
Storage TempStore at -20°C,Desiccated
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionAntagonist of M 1 receptor;Antagonist of M 2 receptor;Antagonist of M 3 receptor;Antagonist of M 4 receptor;Antagonist of M 5 receptor
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

VU 0255035 is a highly selective, competitive and brain penetrant muscarinic M1 receptor antagonist with an IC50 of 130 nM. VU 0255035 reduces pilocarpine-induced seizures in mice. VU0255035 is used to examine the role of the M1 receptor in diverse situations  

Associated Targets(Human)

CHRM5 Tclin Muscarinic acetylcholine receptor M5 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CHRM3 Tclin Muscarinic acetylcholine receptor M3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CHRM4 Tclin Muscarinic acetylcholine receptor M4 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptors; M1 & M2 (498 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name N-[3-oxo-3-(4-pyridin-4-ylpiperazin-1-yl)propyl]-2,1,3-benzothiadiazole-4-sulfonamide
INCHI InChI=1S/C18H20N6O3S2/c25-17(24-12-10-23(11-13-24)14-4-7-19-8-5-14)6-9-20-29(26,27)16-3-1-2-15-18(16)22-28-21-15/h1-5,7-8,20H,6,9-13H2
InChi Key WXDHQWPQLKGANZ-UHFFFAOYSA-N
Canonical SMILES C1CN(CCN1C2=CC=NC=C2)C(=O)CCNS(=O)(=O)C3=CC=CC4=NSN=C43
Isomeric SMILES C1CN(CCN1C2=CC=NC=C2)C(=O)CCNS(=O)(=O)C3=CC=CC4=NSN=C43
PubChem CID 24768606
Molecular Weight 432.51

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

14 results found

Lot NumberCertificate TypeDateItem
F23061542Certificate of AnalysisJun 12, 2024 V275278
F23062010Certificate of AnalysisMay 10, 2024 V275278
F23061981Certificate of AnalysisMay 10, 2024 V275278
F23061980Certificate of AnalysisMay 10, 2024 V275278
F23061632Certificate of AnalysisMay 10, 2024 V275278
F23061568Certificate of AnalysisMay 10, 2024 V275278
F23061549Certificate of AnalysisMay 10, 2024 V275278
F23061565Certificate of AnalysisMar 21, 2024 V275278
F23061959Certificate of AnalysisMar 21, 2024 V275278
F23061978Certificate of AnalysisMar 21, 2024 V275278
F23062006Certificate of AnalysisMar 21, 2024 V275278
F23062008Certificate of AnalysisMar 21, 2024 V275278
F23062009Certificate of AnalysisMar 21, 2024 V275278
F23062051Certificate of AnalysisMar 21, 2024 V275278

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Chemical and Physical Properties

SolubilitySoluble in DMSO to 50mM

Safety and Hazards(GHS)

Pictogram(s) GHS07
Signal Warning
Hazard Statements

H315:Causes skin irritation

H319:Causes serious eye irritation

H335:May cause respiratory irritation

H302:Harmful if swallowed

Precautionary Statements

P261:Avoid breathing dust/fume/gas/mist/vapors/spray.

P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

P280:Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352:IF ON SKIN: wash with plenty of water.

P321:Specific treatment (see ... on this label).

P405:Store locked up.

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P271:Use only outdoors or in a well-ventilated area.

P270:Do not eat, drink or smoke when using this product.

P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing.

P403+P233:Store in a well-ventilated place. Keep container tightly closed.

P362+P364:Take off contaminated clothing and wash it before reuse.

P330:Rinse mouth.

P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes.

P301+P317:IF SWALLOWED: Get medical help.

P337+P317:If eye irritation persists: Get medical help.

P332+P317:If skin irritation occurs: Get medical help.

P319:Get medical help if you feel unwell.

Related Documents

Solution Calculators