| Size | Price | Stock | Qty |
|---|---|---|---|
| 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 vitro, Th2 cells are resistant to factor-induced apoptosis when exposed to GS143 (10 μM or 20 μM), but not Th1 cells. In a dose-dependent manner, GS143 strongly suppresses the Th2 pathway's ability to produce IL-4 [1]. TNFα-induced NF-κB regulation is inhibited by GS143, with an average IC50 value of 10.5 μM. With an IC50 value of 6.1 μM, GS143 also suppresses TNFα-induced ICAM-1 expression in HT-29 circulation. LPS-activated THP-1 cells showed inhibited production of TNFα and IL-1β, with IC50 values of 2.1 μM and 5.3 μM, respectively. p53 and β-catenin are not inhibited by GS143[2].
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|---|---|
| ln Vivo |
Intranasal scent administered once to BALB/c mice containing 16–32 μg/body of GS143 causes transcription factor receptors to become activated by NF-κB. Additionally, GS143 therapy causes the development of Th2 cytokines and eotaxin in the airways, as well as transcription factor activation of eosinophils and eosinophils into the airways [1].
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| Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse (7-8 weeks) injected with ovalbumin [1]
Doses: 16 μg/body or 32 μg/body Route of Administration: intranasal administration; primary Experimental Results:inhibition of lungs of sensitized mice Antigen-induced NF-κB activation. |
| References |
| Molecular Formula |
C28H19FN2O4
|
|---|---|
| Molecular Weight |
466.459870576859
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| Exact Mass |
466.132
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| CAS # |
916232-21-8
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| PubChem CID |
121513876
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| Appearance |
Pink to red solid powder
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| LogP |
5.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
35
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| Complexity |
844
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=CC(N2C(=O)C(=CC3=CC=C(C4C(F)=CC=CC=4)O3)C(CC3C=CC=CC=3)=N2)=CC=1)O
|
| InChi Key |
IZPMWFSVTDOCDI-HAVVHWLPSA-N
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| InChi Code |
InChI=1S/C28H19FN2O4/c29-24-9-5-4-8-22(24)26-15-14-21(35-26)17-23-25(16-18-6-2-1-3-7-18)30-31(27(23)32)20-12-10-19(11-13-20)28(33)34/h1-15,17H,16H2,(H,33,34)/b23-17+
|
| Chemical Name |
4-[(4E)-3-benzyl-4-[[5-(2-fluorophenyl)furan-2-yl]methylidene]-5-oxopyrazol-1-yl]benzoic acid
|
| Synonyms |
GS143; GS 143; GS-143
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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 : ~37.5 mg/mL (~80.39 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.46 mM) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 1.88 mg/mL (4.03 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 18.8 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1438 mL | 10.7190 mL | 21.4381 mL | |
| 5 mM | 0.4288 mL | 2.1438 mL | 4.2876 mL | |
| 10 mM | 0.2144 mL | 1.0719 mL | 2.1438 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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