| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
Epac1; Epac2 ( IC50 = 5.9 µM )
HJC0197 targets the Epac1 (exchange protein activated by cAMP 1) signaling pathway. Epac1 is a guanine nucleotide exchange factor (GEF) that activates the small GTPase Rap1. By inhibiting Epac1, HJC0197 prevents the activation of Rap1, which is involved in cell adhesion, migration, and proliferation. This makes it a potential tool for studying Epac1-Rap1 signaling. |
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| ln Vitro |
HJC0197 (25 μM) likewise suppresses Rap1-GDP exchange activity mediated by Epac1 at 25 μM when cAMP concentration is equal[1].
In vitro activity of HJC0197 is assessed in cell-based assays measuring Rap1 activation. Cells are treated with the compound, and the activation of Rap1 is measured by pull-down assays using the Rap1-binding domain of RalGDS. The compound's ability to inhibit Epac1-mediated Rap1 activation is determined. |
| ln Vivo |
In vivo activity of HJC0197 has not been extensively reported. As a research compound, it may be evaluated in animal models of cancer or inflammatory diseases to assess its therapeutic potential. However, no specific in vivo data is available in the public domain.
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| Enzyme Assay |
The in vitro assay for HJC0197 typically involves a Rap1 activation assay. Cells expressing Epac1 are treated with the compound and stimulated with cAMP. The activation of Rap1 is measured using a pull-down assay with the Rap1-binding domain of RalGDS, followed by Western blotting for Rap1-GTP.
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| Cell Assay |
Cellular assays for HJC0197 involve treating cells with the compound and measuring its effects on Rap1-dependent processes, such as cell adhesion, migration, and proliferation. Cell adhesion is assessed by measuring the attachment of cells to extracellular matrix proteins. Cell migration is assessed using transwell or wound-healing assays.
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| Animal Protocol |
In vivo animal experiments for HJC0197 would typically involve administering the compound to mouse models of cancer or inflammatory diseases. Its effects on tumor growth, metastasis, or inflammation would be assessed. However, no specific in vivo data is available.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for HJC0197 is not publicly available. As a research compound, its absorption, distribution, metabolism, and excretion (ADME) properties would need to be characterized. Parameters such as oral bioavailability, half-life, and plasma protein binding would be determined to guide further development.
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| Toxicity/Toxicokinetics |
Toxicological data for HJC0197 is limited. As a research compound, it is not intended for human use. Standard safety precautions should be followed when handling. Its safety profile would need to be established through preclinical toxicology studies if it were to be developed for therapeutic applications.
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| References | |
| Additional Infomation |
HJC0197 is a research compound that inhibits the Epac1-Rap1 signaling pathway. It is used in studies of cell adhesion, migration, and cancer. The compound is available from various chemical suppliers for research purposes only.
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| Molecular Formula |
C19H21N3OS
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|---|---|
| Molecular Weight |
339.45
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| Exact Mass |
339.141
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| Elemental Analysis |
C, 67.23; H, 6.24; N, 12.38; O, 4.71; S, 9.45
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| CAS # |
1383539-73-8
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| PubChem CID |
136228204
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| Appearance |
White to off-white solid powder
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| LogP |
4.208
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
609
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(CC1C=C(C)C=CC=1C)C1NC(C(C#N)=C(C2CCCC2)N=1)=O
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| InChi Key |
QLLWRTHDHRGHQZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H21N3OS/c1-12-7-8-13(2)15(9-12)11-24-19-21-17(14-5-3-4-6-14)16(10-20)18(23)22-19/h7-9,14H,3-6,11H2,1-2H3,(H,21,22,23)
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| Chemical Name |
4-cyclopentyl-2-[(2,5-dimethylphenyl)methylsulfanyl]-6-oxo-1H-pyrimidine-5-carbonitrile
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| Synonyms |
HJC 0197; HJC-0197; HJC0197
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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: ~68 mg/mL (~200.3 mM)
Ethanol: ~14 mg/mL Water: ~8 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.36 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 (7.36 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 (7.36 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 | 2.9459 mL | 14.7297 mL | 29.4594 mL | |
| 5 mM | 0.5892 mL | 2.9459 mL | 5.8919 mL | |
| 10 mM | 0.2946 mL | 1.4730 mL | 2.9459 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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