VU0255035 | CAS#1135243-19-4 | M1 Receptor Antagonist

MedKoo Cat#: 532900 | Name: VU0255035

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

VU0255035 is a highly selective antagonist of the muscarinic acetylcholine receptor subtype 1 (M1 mAChR), with a Ki value of 14.87 nM, exhibiting over 75-fold selectivity compared to other muscarinic receptor subtypes.In vivo studies have demonstrated that VU0255035 effectively reduces pilocarpine-induced seizures in mice without impairing contextual learning, suggesting its potential as a therapeutic agent for seizure management. Additionally, VU0255035 has been shown to delay the onset of status epilepticus following organophosphate exposure and prevent hyperexcitability in the basolateral amygdala, indicating its relevance in neuroprotection.

Chemical Structure

VU0255035

CAS#1135243-19-4

Theoretical Analysis

MedKoo Cat#: 532900

Name: VU0255035

CAS#: 1135243-19-4

Chemical Formula: C18H20N6O3S2

Exact Mass: 432.1038

Molecular Weight: 432.52

Elemental Analysis: C, 49.99; H, 4.66; N, 19.43; O, 11.10; S, 14.82

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 400.00	2 Weeks
25mg	USD 850.00	2 Weeks

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Related CAS #

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Synonym

VU0255035, VU 0255035, VU-0255035

IUPAC/Chemical Name

N-[3-oxo-3-(4-pyridin-4-ylpiperazin-1-yl)propyl]-2,1,3-benzothiadiazole-7-sulfonamide

InChi Key

WXDHQWPQLKGANZ-UHFFFAOYSA-N

InChi Code

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

SMILES Code

O=S(C1=CC=CC2=NSN=C21)(NCCC(N3CCN(C4=CC=NC=C4)CC3)=O)=O

Appearance

Light yellow to yellow solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

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 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
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Zhu Z, Wang W, Gu C, Wang M, Yan Y. The M1 muscarinic acetylcholine receptor regulates the surface expression of the AMPA receptor subunit GluA2 via PICK1. Psychopharmacology (Berl). 2023 Jan;240(1):239-248. doi: 10.1007/s00213-022-06304-4. Epub 2022 Dec 23. PMID: 36564670. 2: Crans RAJ, Wouters E, Valle-León M, Taura J, Massari CM, Fernández-Dueñas V, Stove CP, Ciruela F. Corrigendum: Striatal dopamine D2-muscarinic acetylcholine M1 receptor-receptor interaction in a model of movement disorders. Front Pharmacol. 2022 Nov 18;13:1075433. doi: 10.3389/fphar.2022.1075433. Erratum for: Front Pharmacol. 2020 Mar 13;11:194. doi: 10.3389/fphar.2020.00194. PMID: 36467044; PMCID: PMC9716621. 3: Athnaiel O, Job GA, Ocampo R, Teneqexhi P, Messer WS, Ragozzino ME. Effects of the Partial M1 Muscarinic Cholinergic Receptor Agonist CDD-0102A on Stereotyped Motor Behaviors and Reversal Learning in the BTBR Mouse Model of Autism. Int J Neuropsychopharmacol. 2022 Jan 12;25(1):64-74. doi: 10.1093/ijnp/pyab079. PMID: 34791301; PMCID: PMC8756088. 4: Rahman MA, Tanaka N, Nuruzzaman M, DebNath S, Kawahara S. Blockade of the M1 muscarinic acetylcholine receptors impairs eyeblink serial feature-positive discrimination learning in mice. PLoS One. 2020 Aug 13;15(8):e0237451. doi: 10.1371/journal.pone.0237451. PMID: 32790748; PMCID: PMC7425847. 5: Crans RAJ, Wouters E, Valle-León M, Taura J, Massari CM, Fernández-Dueñas V, Stove CP, Ciruela F. Striatal Dopamine D2-Muscarinic Acetylcholine M1 Receptor-Receptor Interaction in a Model of Movement Disorders. Front Pharmacol. 2020 Mar 13;11:194. doi: 10.3389/fphar.2020.00194. Erratum in: Front Pharmacol. 2022 Nov 18;13:1075433. doi: 10.3389/fphar.2022.1075433. PMID: 32231561; PMCID: PMC7083216. 6: Inoue M, Harada K, Matsui M, Matsuoka H. Differences among muscarinic agonists in M1 receptor-mediated nonselective cation channel activation and TASK1 channel inhibition in adrenal medullary cells. Eur J Pharmacol. 2019 Jan 15;843:104-112. doi: 10.1016/j.ejphar.2018.11.021. Epub 2018 Nov 17. PMID: 30452911. 7: Miyauchi M, Neugebauer NM, Sato T, Ardehali H, Meltzer HY. Muscarinic receptor signaling contributes to atypical antipsychotic drug reversal of the phencyclidine-induced deficit in novel object recognition in rats. J Psychopharmacol. 2017 Dec;31(12):1588-1604. doi: 10.1177/0269881117731278. Epub 2017 Sep 25. PMID: 28946779. 8: Lv X, Dickerson JW, Rook JM, Lindsley CW, Conn PJ, Xiang Z. M1 muscarinic activation induces long-lasting increase in intrinsic excitability of striatal projection neurons. Neuropharmacology. 2017 May 15;118:209-222. doi: 10.1016/j.neuropharm.2017.03.017. Epub 2017 Mar 20. PMID: 28336323; PMCID: PMC5501169. 9: Calcutt NA, Smith DR, Frizzi K, Sabbir MG, Chowdhury SK, Mixcoatl-Zecuatl T, Saleh A, Muttalib N, Van der Ploeg R, Ochoa J, Gopaul A, Tessler L, Wess J, Jolivalt CG, Fernyhough P. Selective antagonism of muscarinic receptors is neuroprotective in peripheral neuropathy. J Clin Invest. 2017 Feb 1;127(2):608-622. doi: 10.1172/JCI88321. Epub 2017 Jan 17. PMID: 28094765; PMCID: PMC5272197. 10: Miller SL, Aroniadou-Anderjaska V, Pidoplichko VI, Figueiredo TH, Apland JP, Krishnan JK, Braga MF. The M1 Muscarinic Receptor Antagonist VU0255035 Delays the Development of Status Epilepticus after Organophosphate Exposure and Prevents Hyperexcitability in the Basolateral Amygdala. J Pharmacol Exp Ther. 2017 Jan;360(1):23-32. doi: 10.1124/jpet.116.236125. Epub 2016 Oct 31. PMID: 27799295; PMCID: PMC5193080. 11: Jadeja RN, Urrunaga NH, Ahmad D, Khurana S. Data regarding M1 muscarinic receptor-mediated modulation of hepatic catalase activity in response to oxidative stress. Data Brief. 2015 Dec 18;6:405-9. doi: 10.1016/j.dib.2015.12.025. PMID: 26862589; PMCID: PMC4707288. 12: de Vin F, Choi SM, Bolognesi ML, Lefebvre RA. Presynaptic M3 muscarinic cholinoceptors mediate inhibition of excitatory synaptic transmission in area CA1 of rat hippocampus. Brain Res. 2015 Dec 10;1629:260-9. doi: 10.1016/j.brainres.2015.10.031. Epub 2015 Oct 23. PMID: 26505913. 13: Navarria A, Wohleb ES, Voleti B, Ota KT, Dutheil S, Lepack AE, Dwyer JM, Fuchikami M, Becker A, Drago F, Duman RS. Rapid antidepressant actions of scopolamine: Role of medial prefrontal cortex and M1-subtype muscarinic acetylcholine receptors. Neurobiol Dis. 2015 Oct;82:254-261. doi: 10.1016/j.nbd.2015.06.012. Epub 2015 Jun 21. PMID: 26102021; PMCID: PMC4640941. 14: Urrunaga NH, Jadeja RN, Rachakonda V, Ahmad D, McLean LP, Cheng K, Shah V, Twaddell WS, Raufman JP, Khurana S. M1 muscarinic receptors modify oxidative stress response to acetaminophen-induced acute liver injury. Free Radic Biol Med. 2015 Jan;78:66-81. doi: 10.1016/j.freeradbiomed.2014.09.032. Epub 2014 Oct 31. PMID: 25452146; PMCID: PMC4392405. 15: Harada K, Matsuoka H, Miyata H, Matsui M, Inoue M. Identification of muscarinic receptor subtypes involved in catecholamine secretion in adrenal medullary chromaffin cells by genetic deletion. Br J Pharmacol. 2015 Mar;172(5):1348-59. doi: 10.1111/bph.13011. Epub 2015 Jan 8. PMID: 25393049; PMCID: PMC4337706. 16: Maltese M, Martella G, Madeo G, Fagiolo I, Tassone A, Ponterio G, Sciamanna G, Burbaud P, Conn PJ, Bonsi P, Pisani A. Anticholinergic drugs rescue synaptic plasticity in DYT1 dystonia: role of M1 muscarinic receptors. Mov Disord. 2014 Nov;29(13):1655-65. doi: 10.1002/mds.26009. Epub 2014 Sep 4. PMID: 25195914; PMCID: PMC4216601. 17: Witkin JM, Overshiner C, Li X, Catlow JT, Wishart GN, Schober DA, Heinz BA, Nikolayev A, Tolstikov VV, Anderson WH, Higgs RE, Kuo MS, Felder CC. M1 and m2 muscarinic receptor subtypes regulate antidepressant-like effects of the rapidly acting antidepressant scopolamine. J Pharmacol Exp Ther. 2014 Nov;351(2):448-56. doi: 10.1124/jpet.114.216804. Epub 2014 Sep 3. PMID: 25187432. 18: Menozzi A, Pozzoli C, Poli E, Delvescovo B, Serventi P, Bertini S. Pharmacological characterization of muscarinic receptors in the contractions of isolated bronchi in the horse. J Vet Pharmacol Ther. 2014 Aug;37(4):325-31. doi: 10.1111/jvp.12108. Epub 2014 Mar 7. PMID: 24602109. 19: Barrett SG, Chapman CA. Contribution of muscarinic M1 receptors to the cholinergic suppression of synaptic responses in layer II of the entorhinal cortex. Neurosci Lett. 2013 Oct 25;554:11-5. doi: 10.1016/j.neulet.2013.08.050. Epub 2013 Sep 5. PMID: 24012918. 20: Xiang Z, Thompson AD, Jones CK, Lindsley CW, Conn PJ. Roles of the M1 muscarinic acetylcholine receptor subtype in the regulation of basal ganglia function and implications for the treatment of Parkinson's disease. J Pharmacol Exp Ther. 2012 Mar;340(3):595-603. doi: 10.1124/jpet.111.187856. Epub 2011 Dec 1. PMID: 22135383; PMCID: PMC3286317.