Size | Price | Stock | Qty |
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5mg |
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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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ln Vitro |
Applying M1 PAM VU0453595 (3 μM) causes medium spiny neurons (MSNs) to become temporarily more excitable[3].
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ln Vivo |
VU0453595 increases the intensity of M1-mediated muscarinic long-term depression (mLTD)[1].
VU0453595 (1-10 mg/kg; i.p.) restores behavioral deficiencies brought on by phencyclidine (PCP) administration repeated[1]. |
Animal Protocol |
Male C57BL6/J mice (8-9 weeks old)
1, 3, or 10 mg/kg Intraperitoneal (i.p.); 10 mL/kg; administered 30 min before the social interaction test |
References |
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Molecular Formula |
C18H15FN4O
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Molecular Weight |
322.336306810379
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Exact Mass |
322.12
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Elemental Analysis |
C, 67.07; H, 4.69; F, 5.89; N, 17.38; O, 4.96
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CAS # |
1432436-13-9
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Appearance |
Solid powder
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SMILES |
CN1C=C(C=N1)C2=CC(=C(C=C2)CN3CC4=C(C3=O)C=CC=N4)F
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InChi Key |
LIZQOZALTSDKFU-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C18H15FN4O/c1-22-9-14(8-21-22)12-4-5-13(16(19)7-12)10-23-11-17-15(18(23)24)3-2-6-20-17/h2-9H,10-11H2,1H3
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Chemical Name |
6-[[2-fluoro-4-(1-methylpyrazol-4-yl)phenyl]methyl]-7H-pyrrolo[3,4-b]pyridin-5-one
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Synonyms |
VU-0453595; VU0453595; VU 0453595
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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 |
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: ~100 mg/mL (~310.2 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.76 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 (7.76 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.1023 mL | 15.5116 mL | 31.0231 mL | |
5 mM | 0.6205 mL | 3.1023 mL | 6.2046 mL | |
10 mM | 0.3102 mL | 1.5512 mL | 3.1023 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.
M1 PAM VU0453595 potentiates the effect of submaximal optical stimulation of striatal cholinergic system on MSN excitability. Neuropharmacology . 2017 May 15:118:209-222. td> |
M1 PAM VU0453595 enhances cue-dependent non-spatial learning. Neuropharmacology . 2017 May 15:118:209-222. td> |
VU0453595 and VU0550164 lack significant agonist activity and are potent PAMs in M1-expressing CHO cells. Neuropsychopharmacology . 2018 Jul;43(8):1763-1771. td> |
The M1 PAM VU0453595 potentiates muscarinic LTD by activating M1 receptors. Neuropsychopharmacology . 2016 Jan;41(2):598-610. td> |
Muscarinic LTD is compromised following repeated PCP treatment but can be rescued by the M1 PAM VU0453595. Neuropsychopharmacology . 2016 Jan;41(2):598-610. td> |