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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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VU0467154 (VU-0467154) is a novel and potent M4 PAM (positive allosteric modulator) with the potential to be used as a novel approach for the treatment of psychotic symptoms associated with schizophrenia and other neuropsychiatric disorders. Acting on muscarinic acetylcholine receptor (mAChR). VU0467154 exhibits robust APD-like and cognitive enhancing activity in rodents. Selective M4 PAMs could provide a therapeutic strategy for the treatment of HD.
ln Vitro |
VU0467154 is a muscarinic acetylcholine receptor (mAChR) positive allosteric modulator that has pEC50s of 7.75, 6.2, and 6.2 for rat, human, and cynomolgus monkey (cyno) M4 receptors, respectively. It can greatly increase the responsiveness to ACh. 6. In rats and humans, VU0467154 did not increase ACh responses in M1, M2, M3, or M5 [1].
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ln Vivo |
Rats' amphetamine-induced hyperlocomotion is reversed by VU0467154 (1–56.6 mg/kg, oral or intraperitoneal injection). In wild-type mice, VU0467154 (0.3-30 mg/kg, ip) reverses the hyperlocomotion caused by amphetamine and MK-801, but not in M4 KO mice. In wild-type mice, VU0467154 alone also improves the learning of context- and cue-mediated fear conditioning [1].
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References |
[1]. Bubser M, et al. Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents. ACS Chem Neurosci. 2014 Oct 15;5(10):920-42
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Molecular Formula |
C17H15F3N4O3S2
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Molecular Weight |
444.451211214066
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CAS # |
1451993-15-9
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Related CAS # |
1451993-15-9;
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SMILES |
C12SC(C(NCC3=CC=C(S(C(F)(F)F)(=O)=O)C=C3)=O)=C(N)C1=C(C)C(C)=NN=2
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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 : ~13.89 mg/mL (~31.25 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 1.39 mg/mL (3.13 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 13.9 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2500 mL | 11.2499 mL | 22.4997 mL | |
5 mM | 0.4500 mL | 2.2500 mL | 4.4999 mL | |
10 mM | 0.2250 mL | 1.1250 mL | 2.2500 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.