| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
The half-life of AMG PERK 44 against cellular pPERK is 84 nM [1].
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|---|---|
| ln Vivo |
In this assay, AMG PERK 44 (oral; 3-100 mg/kg) maintains >50% Target coverage was sustained for 24 hours in a time-course PD assay when administered at 100 mg/kg po. It also potently inhibits PERK autophosphorylation (ED50=3 mg/kg; 4-hour time point ED90=60 mg/kg) [1]. In male CD-1 mice and Sprague-Dawley rats, AMG PERK 44 (iv; 1 mg/kg) has an MRT of 2.3 hours, a CL of 1.6 L/h·kg, and a Vss of 3.6 L/kg [1].
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| Animal Protocol |
Animal/Disease Models: SD (SD (Sprague-Dawley)) rats and male CD-1 mice [1]
Doses: 1 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: intravenous (iv) (iv)injection Experimental Results: CL is 1.6 L/h·kg, Vss is 3.6 L/kg, 2.3 hrs (hrs (hours)) on the subway. |
| References |
|
| Molecular Formula |
C34H29CLN4O2
|
|---|---|
| Molecular Weight |
561.072666883469
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| Exact Mass |
560.197
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| CAS # |
1883548-84-2
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| PubChem CID |
121513867
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
41
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| Complexity |
967
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl.O=C1C(C(C2C=CC(C)=C(C3C=CC4C(=CC=C(C)N=4)C=3)C=2N)=O)=C(C2C=CC=CC=2)N(C)N1C1C=CC=CC=1
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| InChi Key |
RNAKBTDDCHJCMT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C34H28N4O2.ClH/c1-21-14-18-27(31(35)29(21)25-17-19-28-24(20-25)16-15-22(2)36-28)33(39)30-32(23-10-6-4-7-11-23)37(3)38(34(30)40)26-12-8-5-9-13-26;/h4-20H,35H2,1-3H3;1H
|
| Chemical Name |
4-[2-amino-4-methyl-3-(2-methylquinolin-6-yl)benzoyl]-1-methyl-2,5-diphenylpyrazol-3-one;hydrochloride
|
| 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. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~44.56 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.71 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 (3.71 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 20.8 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: ≥ 2.08 mg/mL (3.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7823 mL | 8.9115 mL | 17.8231 mL | |
| 5 mM | 0.3565 mL | 1.7823 mL | 3.5646 mL | |
| 10 mM | 0.1782 mL | 0.8912 mL | 1.7823 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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