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GPCR&G protein

VU0357017 hydrochloride (1135242-13-5)

VU0357017, also known as CID 25010775, is a subtype-selective M1 muscarinic acetylcholine allosteric agonist.

Not Intended for Therapeutic Use. For research use only.

CAS: 1135242-13-5 Category

VU0357017 hydrochloride (1135242-13-5) Description

VU0357017 is a subtype-selective M1 muscarinic acetylcholine allosteric agonist. VU0357017 has a potency of 200 nM and Achmax of 81% and had no activity at M2-M5 up to the highest concentrations tested and also had little or no detectable antagonist activity at any other mAChR subtype at concentrations over 2 orders of magnitude higher than those required to activate M1 or activity at a large panel of GPCRs, ion channels, and transporters. In contrast, TBPB inhibited responses to ACh at each of the other mAChR subtypes. VU0357017 was active in reversing cognitive deficits induced by Scopolamine (S200000) in a preclinical rodent model.

VU0357017 HCL (1135242-13-5) Specifications

Product Name VU0357017 hydrochloride
Synonyms VU0357017, VU-0357017, VU 0357017, CID 25010775, CID25010775, CID-25010775
Chemical Names VU 0357017 Hydrochloride; 1135242-13-5; VU0357017; Vu0357017 hydrochloride; VU0357017 (hydrochloride); Ethyl 4-(2-(2-methylbenzamido)ethylamino)piperidine-1-carboxylate hydrochloride
Purity >98%
CAS Number 1135242-13-5
Molecular Formula C18H28ClN3O3
Molecular Weight 369.89 g/mol
Monoisotopic Mass 369.182 g/mol
InChIKey XKJQVUIXSBOCPP-UHFFFAOYSA-N
InChi Code InChI=1S/C18H27N3O3.ClH/c1-3-24-18(23)21-12-8-15(9-13-21)19-10-11-20-17(22)16-7-5-4-6-14(16)2;/h4-7,15,19H,3,8-13H2,1-2H3,(H,20,22);1H
SMILES O=C(N1CCC(NCCNC(C2=CC=CC=C2C)=O)CC1)OCC.[H]Cl
Form Powder
Color White
Solubility  Soluble in DMSO
Storage Temp.  −20°C
Shelf life >2 years if stored properly.
Handling Dry, dark
Application a subtype-selective M1 muscarinic

 


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RIDADR NONH for all modes of transport

References:

  • 1: 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. PubMed PMID: 26862589; PubMed Central PMCID: PMC4707288.
  • 2: Digby GJ, Utley TJ, Lamsal A, Sevel C, Sheffler DJ, Lebois EP, Bridges TM, Wood MR, Niswender CM, Lindsley CW, Conn PJ. Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode. ACS Chem Neurosci. 2012 Dec 19;3(12):1025-36. doi: 10.1021/cn300103e. PubMed PMID: 23259038; PubMed Central PMCID: PMC3526969.
  • 3: Sheffler DJ, Sevel C, Le U, Lovell KM, Tarr JC, Carrington SJ, Cho HP, Digby GJ, Niswender CM, Conn PJ, Hopkins CR, Wood MR, Lindsley CW. Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism. Bioorg Med Chem Lett. 2013 Jan 1;23(1):223-7. doi: 10.1016/j.bmcl.2012.10.132. PubMed PMID: 23200253; PubMed Central PMCID: PMC3525729.
  • 4: Digby GJ, Noetzel MJ, Bubser M, Utley TJ, Walker AG, Byun NE, Lebois EP, Xiang Z, Sheffler DJ, Cho HP, Davis AA, Nemirovsky NE, Mennenga SE, Camp BW, Bimonte-Nelson HA, Bode J, Italiano K, Morrison R, Daniels JS, Niswender CM, Olive MF, Lindsley CW, Jones CK, Conn PJ. Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models. J Neurosci. 2012 Jun 20;32(25):8532-44. doi: 10.1523/JNEUROSCI.0337-12.2012. PubMed PMID: 22723693; PubMed Central PMCID: PMC3398407.
  • 5: Thomsen M, Lindsley CW, Conn PJ, Wessell JE, Fulton BS, Wess J, Caine SB. Contribution of both M1 and M4 receptors to muscarinic agonist-mediated attenuation of the cocaine discriminative stimulus in mice. Psychopharmacology (Berl). 2012 Apr;220(4):673-85. doi: 10.1007/s00213-011-2516-9. PubMed PMID: 21964721; PubMed Central PMCID: PMC3314162.
  • 6: Lebois EP, Bridges TM, Lewis LM, Dawson ES, Kane AS, Xiang Z, Jadhav SB, Yin H, Kennedy JP, Meiler J, Niswender CM, Jones CK, Conn PJ, Weaver CD, Lindsley CW. Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system. ACS Chem Neurosci. 2010;1(2):104-121. PubMed PMID: 21961051; PubMed Central PMCID: PMC3180826.

1 review for VU0357017 hydrochloride (1135242-13-5)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The VU0357017 hydrochloride (1135242-13-5) is high purity,also customer service is pretty nice !gotta try!!

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