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GSK2245035 (GSK-2245035) is a novel potent and selective intranasal Toll-like receptor 7 (TLR7) agonist with Type-1 interferon (IFN)-stimulating activity and the potential to be used for the treatment of asthma. Exhibits pEC50s of 9.3 and 6.5 for IFNα and TFNα. Suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures.
| ln Vitro |
In individual-derived human PBMC cells, GSK2245035 (0.01, 0.1, 1, 10, 100, 1000, and 10,000 nM; 6 days) decreases the release of Th2 cytokines, IL-5 and IL-13, in response to home dust mites or Timothy. Dose-dependent sensitization levels to certain allergens exist [1].
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| ln Vivo |
At dosages of 0.3 mg/kg and higher, GSK2245035 (in; 0.03-1 mg/kg; 6 hours) causes a dose-related rise in serum IFNα levels at the 2-hour time point that disappears at 6 hours [1]. After administering GSK2245035 (3, 30, 300, and 3000 ng/kg) for six hours, the most sensitive biomarker of target engagement, plasma IP-10, was found to be enhanced in cynomolgus monkeys at the 30 ng/kg dose and higher [1].
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| Animal Protocol |
Animal/Disease Models: Female balb/c (Bagg ALBino) mouse[1]
Doses: 0.03, 0.1, 0.3, 1 mg/kg Route of Administration: Intranasally (in); 6 hrs (hours) Experimental Results: Dose-related increases in IFNα levels in serum were detected at doses of 0.3 mg /kg and above at the 2 h time point which had subsided at 6 h. |
| References | |
| Additional Infomation |
GSK2245035 is under investigation in clinical trial NCT02833974 (Effect of the GSK2245035 on the Allergen-induced Asthmatic Response).
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| Molecular Formula |
C20H34N6O2
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|---|---|
| Molecular Weight |
390.522964000702
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| Exact Mass |
390.274
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| CAS # |
1207629-49-9
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| Related CAS # |
1207629-49-9;1325212-97-2;
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| PubChem CID |
44623937
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Index of Refraction |
1.555
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| LogP |
3.37
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
28
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| Complexity |
487
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCC[C@H](C)OC1=NC(=C2C(=N1)N(C(=O)N2)CCCCCN3CCCCC3)N
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| InChi Key |
LFMPVTVPXHNXOT-HNNXBMFYSA-N
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| InChi Code |
InChI=1S/C20H34N6O2/c1-3-10-15(2)28-19-23-17(21)16-18(24-19)26(20(27)22-16)14-9-5-8-13-25-11-6-4-7-12-25/h15H,3-14H2,1-2H3,(H,22,27)(H2,21,23,24)/t15-/m0/s1
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| Chemical Name |
6-amino-2-[(2S)-pentan-2-yl]oxy-9-(5-piperidin-1-ylpentyl)-7H-purin-8-one
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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 : ~125 mg/mL (~320.09 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.33 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 (5.33 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 (5.33 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 | 2.5607 mL | 12.8034 mL | 25.6069 mL | |
| 5 mM | 0.5121 mL | 2.5607 mL | 5.1214 mL | |
| 10 mM | 0.2561 mL | 1.2803 mL | 2.5607 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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