| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Schistosoma and helminth species. As an inactive control for JMJD3/UTX, GSK-J5 does not significantly inhibit these histone demethylases. Its primary biological activity is against parasitic worms.
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|---|---|
| ln Vitro |
Blood-sucking worms are inhibited by GSK-J5 (30 μM; 24-96 h); helminths are likewise inhibited by 5 μM and 20 μM; 24 h); modest changes in worm movement are promoted [1].
GSK-J5 increases schistosomula mortality and adult worm viability and mortality, and egg production in a dose- and time-dependent manner. It has demonstrated potent anthelmintic activity against schistosomes and other parasitic worms. |
| ln Vivo |
In vivo activity data for GSK-J5 is not extensively detailed in standard references. As an anthelmintic agent, it is expected to show efficacy in animal models of schistosomiasis and other helminth infections. Its cell-permeable nature suggests it may have good tissue penetration.
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| Enzyme Assay |
In vitro enzyme assays for histone demethylase activity are performed using recombinant JMJD3 or UTX and a histone peptide substrate. The demethylation reaction is monitored by mass spectrometry or ELISA. GSK-J5 is used as a negative control in these assays to confirm the specificity of GSK-J4.
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| Cell Assay |
In vitro anthelmintic activity is assessed using schistosomula or adult worms in culture. Worms are treated with various concentrations of GSK-J5, and mortality is assessed by microscopic observation. Egg production is quantified. Cytotoxicity against mammalian cells is evaluated using standard cell viability assays.
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| Animal Protocol |
In vivo efficacy studies are performed in mouse models of schistosomiasis. Mice are infected with cercariae, and after the infection is established, GSK-J5 is administered orally or intraperitoneally. Worm burden and egg production are assessed at necropsy. Liver and intestinal pathology are evaluated.
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| ADME/Pharmacokinetics |
GSK-J5 has a molecular weight of 417.5 and is soluble in DMSO (21 mg/mL). It is a cell-permeable compound. It is typically stored at -20°C. Detailed pharmacokinetic parameters such as oral bioavailability and half-life are available from specialized databases.
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| Toxicity/Toxicokinetics |
Detailed toxicological profiles of GSK-J5 are not extensively reported. As an anthelmintic agent, it is expected to have a manageable safety profile at therapeutic doses. Cytotoxicity against mammalian cells is assessed in parallel with anthelmintic activity to determine the selectivity index.
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| References | |
| Additional Infomation |
GSK-J5 is a research compound used as an inactive control for histone demethylase studies and as an anthelmintic agent. It is not approved for clinical use. Its molecular formula is C24H27N5O2 and its molecular weight is 417.5.
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| Molecular Formula |
C24H27N5O2
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|---|---|
| Molecular Weight |
417.5
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| Exact Mass |
417.216
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| CAS # |
1394854-51-3
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| Related CAS # |
GSK-J1;1373422-53-7;GSK-J2;1394854-52-4;GSK-J4;1373423-53-0;GSK-J1 lithium salt;GSK-J5 hydrochloride;1797983-32-4
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| PubChem CID |
78243729
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| Appearance |
Light brown to brown ointment
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
581.2±50.0 °C at 760 mmHg
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| Flash Point |
305.3±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.615
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| LogP |
3.75
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
31
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| Complexity |
546
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(OCC)CCNC1=NC(C2=CC=CN=C2)=NC(N3CCC4=CC=CC=C4CC3)=C1
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| InChi Key |
QQHQMHJAOKADED-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H27N5O2.ClH/c1-2-31-23(30)9-13-26-21-16-22(28-24(27-21)20-8-5-12-25-17-20)29-14-10-18-6-3-4-7-19(18)11-15-29/h3-8,12,16-17H,2,9-11,13-15H2,1H3,(H,26,27,28)1H
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| Chemical Name |
N-[2-(3-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine ethyl ester hydrochloride
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| Synonyms |
GSK J5 HClGSK-J-5 HClGSK-J5 HCl
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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 (~299.40 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3952 mL | 11.9760 mL | 23.9521 mL | |
| 5 mM | 0.4790 mL | 2.3952 mL | 4.7904 mL | |
| 10 mM | 0.2395 mL | 1.1976 mL | 2.3952 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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