| 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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Purity: ≥98%
AMG 579 is a novel, potent, selective, and highly efficacious phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 0.1 nM. In the in vivo LC-MS/MS target occupancy (TO) study at 10 mg/kg, AMG 579 achieved 86-91% occupancy of PDE10A in the brain. Furthermore, both CNS TO and efficacy in PCP-LMA behavioral model were observed in a dose dependent manner. With superior in vivo TO, in vivo efficacy and in vivo PK profiles in multiple preclinical species, compound 5 (AMG 579) was advanced as our PDE10A clinical candidate.
| ln Vivo |
Rats' PCP-induced behavior was demonstrated to be considerably reduced by AMG 579 in less than two hours. It was found that 0.3 mg/kg was the lowest effective dose of AMG 579 that would still have an effect in the PCP-LMA model. Five dogs have a 72% oral bioavailability, which is good [1].
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|---|---|
| References |
| Molecular Formula |
C25H23N5O3
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|---|---|
| Molecular Weight |
441.481825113297
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| Exact Mass |
441.18
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| CAS # |
1227067-61-9
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| PubChem CID |
59351313
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
690
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C1C=CC(C(C2=NC3C=CC=CC=3N2)=O)=CC=1)C1C(C2CCN(C(C)=O)CC2)=NC=CN=1
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| InChi Key |
ZNPDAYJZIRPRFQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H23N5O3/c1-16(31)30-14-10-17(11-15-30)22-25(27-13-12-26-22)33-19-8-6-18(7-9-19)23(32)24-28-20-4-2-3-5-21(20)29-24/h2-9,12-13,17H,10-11,14-15H2,1H3,(H,28,29)
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| Chemical Name |
1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethan-1-one
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| Synonyms |
AMG-579; AMG 579; AMG579; J3.339.633C
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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 : ~41.67 mg/mL (~94.39 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.71 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 20.8 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: ≥ 2.08 mg/mL (4.71 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 20.8 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 | 2.2651 mL | 11.3255 mL | 22.6511 mL | |
| 5 mM | 0.4530 mL | 2.2651 mL | 4.5302 mL | |
| 10 mM | 0.2265 mL | 1.1326 mL | 2.2651 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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