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Purity: ≥98%
VU0357017 HCI (formerly CID-25010775) is a potent and highly selective M1 agonists that appear to act at an allosteric site to activate the receptor with EC50 of 477 ± 172 nM and pEC50 of 6.37 ± 0.15). VU0357017 is a highly selective M1 agonist implies that these substances are more likely to function as allosteric agonists rather than at the highly conserved orthosteric site on M1.In a rodent model of contextual fear conditioning, optimized compounds like VU0357017 have strong in vivo efficacy in reversing scopolamine-induced deficits and offer excellent brain exposure following systemic dosing.
| Targets |
M1 mAChR ( IC50 = 477 nM ); M1 mAChR ( Ki = 9.91 μM )
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| ln Vitro |
In vitroactivity: VU0357017 is an M1-selective agonist that acts at an allosteric site to appear to activate M1. Based on competition binding experiment, the Ki values of VU0357017 are 9.91 (rM1), 21.4 (rM2), 55.3 (rM3), 35 (rM4), and 50 (rM5), in that order. Being a highly selective M1 agonist, VU0357017 indicates that these substances are more likely to function as allosteric agonists than at the highly conserved orthosteric site on M1.
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| ln Vivo |
VU0357017 significantly enhances hippocampal-dependent learning in rats. In rats, VU0357017 improves contextual fear conditioning and Morris water maze performance.
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| Animal Protocol |
Male Sprague−Dawley rats (380-420 g) were pretreated with scopolamine
1, 3, 10 mg/kg A single i.p. |
| References |
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| Molecular Formula |
C18H28CLN3O3
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| Molecular Weight |
369.89
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| Exact Mass |
369.18
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| Elemental Analysis |
C, 58.45; H, 7.63; Cl, 9.58; N, 11.36; O, 12.98
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| CAS # |
1135242-13-5
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| Related CAS # |
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| Appearance |
White to off-white solid powder
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| SMILES |
CCOC(=O)N1CCC(CC1)NCCNC(=O)C2=CC=CC=C2C.Cl
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| InChi Key |
XKJQVUIXSBOCPP-UHFFFAOYSA-N
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| 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
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| Chemical Name |
ethyl 4-[2-[(2-methylbenzoyl)amino]ethylamino]piperidine-1-carboxylate;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25~38 mg/mL (67.6~102.7 mM)
Water: ~10 mg/mL Ethanol: ~2 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 33.33 mg/mL (90.11 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7035 mL | 13.5175 mL | 27.0351 mL | |
| 5 mM | 0.5407 mL | 2.7035 mL | 5.4070 mL | |
| 10 mM | 0.2704 mL | 1.3518 mL | 2.7035 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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