| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
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KAG-308 is a novel, potent, selective and orally bioactive agonist of the prostaglandin E2 receptor EP4, it selectively activated EP4 and potently inhibited tumor necrosis factor-α production in peripheral whole blood and T cells, shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor. . It shows efficacy for treating ulcerative colitis and can bring about lower risk of colorectal carcinogenesis by orally bioavailable administration.
| ln Vitro |
KAG-308 is an oral active, powerful, selective EP4 receptor agonist that prevents colitis and encourages the healing of histological mucosa. Compared to human EP1 (Ki, 1410 nM; EC50, 1000 nM) and EP2 (Ki, 1540 nM; EC50, 1000 nM), KAG-308's Ki and EC50 values for the human EP4 receptor are 2.57 nM and 17 nM, respectively, making it more powerful. selectivity), IP receptors (Ki, 52.9 nM; EC50, >10000 nM), and EP3 (Ki, 32.4 nM; EC50, 160 nM). Dual-luciferase reporter tests demonstrate that KAG-308 possesses strong agonist action against both human and mouse EP4, with EC50 values of 0.15 nM and 1.0 nM, respectively [1].
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| References |
| Molecular Formula |
C24H30F2N4O3
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|---|---|
| Molecular Weight |
460.516812801361
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| Exact Mass |
460.228
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| CAS # |
1215192-68-9
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| Related CAS # |
1215192-68-9
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| PubChem CID |
67108613
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| Appearance |
White to light yellow solid powder
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| LogP |
3.5
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
33
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| Complexity |
722
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| Defined Atom Stereocenter Count |
6
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| SMILES |
FC1(/C(=C/CCCC2N=NNN=2)/O[C@H]2C[C@H]([C@H](/C=C/[C@H]([C@H](C)C3C=CC=C(C)C=3)O)[C@H]21)O)F
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| InChi Key |
KSELABKNBIUMGG-YGBAREPYSA-N
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| InChi Code |
InChI=1S/C24H30F2N4O3/c1-14-6-5-7-16(12-14)15(2)18(31)11-10-17-19(32)13-20-23(17)24(25,26)21(33-20)8-3-4-9-22-27-29-30-28-22/h5-8,10-12,15,17-20,23,31-32H,3-4,9,13H2,1-2H3,(H,27,28,29,30)/b11-10+,21-8-/t15-,17+,18-,19-,20+,23-/m1/s1
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| Chemical Name |
4-[(Z)-(1S,5R,6R,7R)-6-[(1E,3R,4R)-3-Hydroxy-4-(m-tolyl)-1-pentenyl]-7-hydroxy-4,4-difluoro-2-oxabicyclo[3.3.0]octan-3-ylidene]-1-(tetrazol-5-yl)butane
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| Synonyms |
KAG-308 KAG 308 KAG308
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), 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)
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| Solubility (In Vitro) |
DMSO : ~80 mg/mL (~173.72 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 6 mg/mL (13.03 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 60.0 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: 6 mg/mL (13.03 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 60.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1715 mL | 10.8573 mL | 21.7146 mL | |
| 5 mM | 0.4343 mL | 2.1715 mL | 4.3429 mL | |
| 10 mM | 0.2171 mL | 1.0857 mL | 2.1715 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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