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2mg |
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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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Purity: ≥98%
LY2119620 (LY 2119620; LY-2119620) is a novel, potent, specific, high-affinity and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors, the so called positive allosteric modulator (PAM). LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms. In [35S]GTPγS-binding experiments, LY2119620 exhibited a modest allosteric agonism of 23.2% and 16.8% at the M2 and M4 receptors, respectively. LY2119620 and ACh binding caused cooperativity factor α of 79.4 and 19.5 for the M4 receptor and the M2 receptor, respectively.
ln Vitro |
At the M2 and M4 receptors, LY2119620 exhibits a modest allosteric agonism of 23.2±2.18% and 16.8±5.01%, respectively. For LY2119620, there is very little allosteric agonism (<20%) at the M1, M3, and M5 receptors. It is consistently found that the variable KB of LY2119620 for the allosteric binding site on the unoccupied receptor ranges from approximately 1.9 to 3.4 µM. The addition of 10 µM LY2119620 resulted in an increase in Bmax at the M2 receptor of 793±1.95 fmol/mg to 2850±162 fmol/mg and approximately a 5-fold increase at the M4 receptor of 284±18.3 fmol/mg to 1340±42.2 fmol/mg[1].
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ln Vivo |
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Animal Protocol |
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References |
Molecular Formula |
C19H24CLN5O3S
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Molecular Weight |
437.94
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Exact Mass |
437.129
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CAS # |
886047-22-9
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Related CAS # |
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PubChem CID |
57664406
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Appearance |
White to light yellow solid powder
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Density |
1.46±0.1 g/cm3
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LogP |
2.733
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Hydrogen Bond Donor Count |
2
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Hydrogen Bond Acceptor Count |
7
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Rotatable Bond Count |
5
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Heavy Atom Count |
29
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Complexity |
631
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Defined Atom Stereocenter Count |
0
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InChi Key |
TYTGOXSAAQWLPJ-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C19H24ClN5O3S/c1-10-13-15(21)16(17(27)22-11-3-4-11)29-19(13)23-18(14(10)20)28-9-12(26)25-7-5-24(2)6-8-25/h11H,3-9,21H2,1-2H3,(H,22,27)
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Chemical Name |
3-amino-5-chloro-N-cyclopropyl-4-methyl-6-[2-(4-methyl-1-piperazinyl)-2-oxoethoxy]-thieno[2,3-b]pyridine-2-carboxamide
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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 |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.71 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 (5.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2834 mL | 11.4171 mL | 22.8342 mL | |
5 mM | 0.4567 mL | 2.2834 mL | 4.5668 mL | |
10 mM | 0.2283 mL | 1.1417 mL | 2.2834 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.