GSK1795091
Based on 1 Customer Validation
GSK1795091 (CRX-601), an immunologic stimulator, is a synthetic TLR4 agonist. Antitumor activity. GSK1795091 can be used as a vaccine adjuvant to enhance both mucosal and systemic immunity to influenza virus vaccines. Not only, GSK1795091 inhibits tumor growth and increases the survival in mice model, but results in long term survival in influenza challenge model in mice.
For research use only. We do not sell to patients.
- Purity: 94.48%
- CAS No.: 1233589-81-5
- Formula: C81H157N2O16P
- Molecular Weight:1446.09
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
GSK1795091 (25 μg/mouse; iv; once weekly for 3 doses) inhibits tumor growth and results in long term survival in tumor model in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice primed with H3N2[1]
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Dosage:0.1 μg /mouse
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Administration:Intranasal administration
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Result:As an adjuvant combined with detergent split-influenza antigen (H3N2) generated strong local and systemic immunity against co-administered influenza antigens while exhibiting high efficacy against two heterotypic influenza challenges.
Mice receiving adjuvanted vaccines had significantly higher IgA titers than non-adjuvanted (vehicle) controls in an adjuvant dose-dependent manner.
Adjuvanted vaccines promoted antigen-specific IgG and IgA antibody responses and the generation of polyfunctional antigen-specific Th17 cells.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1233589-81-5
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Appearance Solid
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Molecular Weight 1446.09
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Formula C81H157N2O16P
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Color White to off-white
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SMILES
O=C(C[C@H](OCCCCCCCCCC)CCCCCCCCCCC)O[C@@H]([C@@H]([C@H]1CO)O[P](O)(O)=O)[C@H]([C@@H](O1)OC[C@@H](C(O)=O)NC(C[C@H](OCCCCCCCCCC)CCCCCCCCCCC)=O)NC(C[C@H](OCCCCCCCCCC)CCCCCCCCCCC)=O
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Synonyms
CRX-601
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (17.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (1.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Hug BA, et al. Safety, Pharmacokinetics, and Pharmacodynamics of the TLR4 Agonist GSK1795091 in Healthy Individuals: Results from a Randomized, Double-blind, Placebo-controlled, Ascending Dose Study. Clin Ther. 2020;42(8):1519-1534.e33. [Content Brief]
[2]. Maroof A, et.al. Intranasal vaccination promotes detrimental Th17-mediated immunity against influenza infection. PLoS Pathog. 2014 Jan;10(1):e1003875. [Content Brief]
[3]. Cebada J, et al. OX40 agonists for cancer treatment: a patent review. Expert Opin Ther Pat. 2021 Jan;31(1):81-90. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.6915 mL | 3.4576 mL | 6.9152 mL | 17.2880 mL |
| 5 mM | 0.1383 mL | 0.6915 mL | 1.3830 mL | 3.4576 mL | |
| 10 mM | 0.0692 mL | 0.3458 mL | 0.6915 mL | 1.7288 mL | |
| 15 mM | 0.0461 mL | 0.2305 mL | 0.4610 mL | 1.1525 mL |
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