VU 0357017 hydrochloridePositive allosteric modulator of M1 receptors CAS# 1135242-13-5 |
- FLAG tag Peptide
Catalog No.:BCC2562
CAS No.:98849-88-8
Quality Control & MSDS
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Chemical structure
3D structure
Cas No. | 1135242-13-5 | SDF | Download SDF |
PubChem ID | 25010775 | Appearance | Powder |
Formula | C18H28ClN3O3 | M.Wt | 369.89 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Synonyms | CID-25010775 | ||
Solubility | DMSO : 25 mg/mL (67.59 mM; Need ultrasonic) | ||
Chemical Name | ethyl 4-[2-[(2-methylbenzoyl)amino]ethylamino]piperidine-1-carboxylate;hydrochloride | ||
SMILES | CCOC(=O)N1CCC(CC1)NCCNC(=O)C2=CC=CC=C2C.Cl | ||
Standard InChIKey | XKJQVUIXSBOCPP-UHFFFAOYSA-N | ||
Standard InChI | 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 | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | Positive allosteric modulator of muscarinic M1 receptors (EC50 = 198 nM). Displays no activity at M2-M5 at concentrations up to 30 μM. Potentiates NMDA receptor currents in hippocampal neurons; activity reverses cognitive decifits in a rodent model of hippocampal-dependent memory. CNS penetrant. |
VU 0357017 hydrochloride Dilution Calculator
VU 0357017 hydrochloride Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.7035 mL | 13.5175 mL | 27.0351 mL | 54.0701 mL | 67.5877 mL |
5 mM | 0.5407 mL | 2.7035 mL | 5.407 mL | 10.814 mL | 13.5175 mL |
10 mM | 0.2704 mL | 1.3518 mL | 2.7035 mL | 5.407 mL | 6.7588 mL |
50 mM | 0.0541 mL | 0.2704 mL | 0.5407 mL | 1.0814 mL | 1.3518 mL |
100 mM | 0.027 mL | 0.1352 mL | 0.2704 mL | 0.5407 mL | 0.6759 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15). IC50 value: 477 ± 172 nM (EC50) [1] Target: M1 in vitro: VU0357017 is a M1-selective agonists that appear to activate M1 through actions at an allosteric site. Ki values of VU0357017 derived from competition binding experiment is 9.91(rM1), 21.4 (rM2), 55.3 (rM3), 35 (rM4), and 50 (rM5), respectively. [1] VU0357017 is a potent and efficacious M1 agonist, selective versus M2 M5 family members and allosteric agonist. VU0357017 is a highly selective M1 agonist suggests that these compounds are unlikely to act at the highly conserved orthosteric site on M1 and are more likely to act as allosteric agonists. [2] VU0357017 has robust effects on M1-activation of calcium mobilization and ERK1/2 phosphorylation but have little effect on β-arrestin recruitment. VU0357017 induces calcium release and ERK phosphorylation but is without effects on β-arrestin recruitment. VU0357017 significantly enhances threshold Θ-burst LTP and VU0364572 induces LTD at the Schaffer collateral-CA1 synapse of rodent hippocampal slices. [3] in vivo: VU0357017 has robust efficacy in improving hippocampal-dependent learning in rats. VU0357017 enhances performance in Morris water maze and contextual fear conditioning in rats. [3]
References:
[1]. Digby GJ, et al. 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.
[2]. Lebois EP, et al. 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.
[3]. Digby GJ, et al. 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.
[4]. Sheffler DJ, et al. Further exploration of M? allosteric agonists: subtle structural changes abolish M? allosteric agonism and result in pan-mAChR orthosteric antagonism. Bioorg Med Chem Lett. 2013 Jan 1;23(1):223-7.
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Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM.[Pubmed:20156687]
Bioorg Med Chem Lett. 2010 Mar 15;20(6):1972-5.
This Letter describes a chemical lead optimization campaign directed at VU0119498, a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) with the goal of developing a selective M(1) PAM. An iterative library synthesis approach delivered a potent (M(1) EC(50)=830 nM) and highly selective M(1) PAM (>30 microM vs M(2)-M(5)).