| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
In human medulloblastoma TE-671 cells expressing L-PGDS, AT-56 (1-30 μM; 10 min) dose-dependently suppresses PGD2 synthesis with an IC50 of roughly 3 μM [1].
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|---|---|
| ln Vivo |
AT-56 (1-30 mg/kg; oral) reduces PGD2 production in the stab-injured brain [1]. AT-56 (1-10 mg/kg; oral) suppresses L-PGDS-mediated allergic airway inflammation in mice [1]. AT-56 (10 mg/kg; oral) has a Cmax (2.15 μg/ml), half-life (1.71 hours), and excellent oral bioavailability (82%) [1].
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| Animal Protocol |
Animal/Disease Models: H-PGDS KO mice with stab brain injury (14-16 weeks, 25-30 g, C57BL/6 strain) [1]
Doses: 0, 1, 3, 10, 30 mg/kg administered Method: Po 1 hour before stabbing Experimental Results:Inhibited L-PGDS response in the brain. Using 30 mg/kg AT-56 diminished the total amount of PGD2 in the brain to 40%. Animal/Disease Models: Human L-PGDS overexpressing TG mice (male, 14-16 weeks, 25-30 g) [1] Doses: 0, 1, 10 mg/kg Route of Administration: 1 hour before and 24 hrs (hrs (hours)) after antigen exposure Hourly oral Experimental Results: Prevention of eosinophil infiltration by inhibition of transgenic human L-PGDS. Animal/Disease Models: Male C57BL/6 mice (7 weeks, 22-26 g) [1] Doses: 10 mg/kg orally, 2 mg/kg intravenously (iv) (iv)(iv) (pharmacokinetic/PK/PK analysis) Dosing methods: oral and intravenous (iv) (iv)injection Experimental Results: Oral bioavailability (82%); Cmax (2.15 μg/ml); T1/2 (1.71 hrs (hrs (hours)), oral); T1/2 (2.35 hrs (hrs (hours)), intravenous (iv) (iv)injection). |
| References |
| Exact Mass |
397.226
|
|---|---|
| Elemental Analysis |
C, 75.54; H, 6.85; N, 17.62
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| CAS # |
162640-98-4
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| PubChem CID |
11741525
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
620.4±65.0 °C at 760 mmHg
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| Flash Point |
329.0±34.3 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.646
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| LogP |
5.84
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
|
| Heavy Atom Count |
30
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| Complexity |
591
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LQNGMDUIRLSESZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C25H27N5/c1-3-9-22-19(7-1)12-13-20-8-2-4-10-23(20)25(22)21-14-17-30(18-15-21)16-6-5-11-24-26-28-29-27-24/h1-4,7-10,12-13H,5-6,11,14-18H2,(H,26,27,28,29)
|
| Chemical Name |
1-[4-(2H-tetrazol-5-yl)butyl]-4-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,9,11,13-heptaenylidene)piperidine
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| Synonyms |
AT-56 AT56 AT 56
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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 (~251.56 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.29 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 (6.29 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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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