Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
EC50: 28.2 nM (HBsAg); 16.0 nM (HBeAg)[1]
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ln Vitro |
In the Caco-2 experiment, GST-HG131 exhibits moderate permeability; in the liver microsomal stability assay, it exhibits low clearance and low rat and human plasma protein binding[1]. In primary human hepatocytes (PHH) expressing HBV, GST-HG131 exhibits antiviral action and suppresses both HBsAg and HBeAg, two HBV antigens[1]. In a dose- and time-dependent way, GST-HG131 (500 nM) seems to suppress HBV antigens by inhibiting HBV RNAs[1]. Specific HBV inhibition is demonstrated by GST-HG131 against various viruses, including the H1N1 influenza virus, the hepatitis C virus, and herpes simplex virus type 1[1].
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ln Vivo |
Low clearance, a moderate plasma half-life (T1/2), a high plasma exposure (Cmax and AUC), and oral bioavailability are all displayed by GST-HG131[1]. In an AAV/HBV mouse model, GST-HG131 (3, 10, and 30 mg/kg; intravenous; tail vein injection; once daily for 4 weeks) exhibits HBV inhibition[1]. In a rat early toxicological investigation, GST-HG131 (100, 300, and 1000 mg/kg; po; once daily for 14 d) is well tolerated at 300 mg/kg and 100 mg/kg[1]. Note: Male C57BL/6 mice (iv/po: 0.5 mg/kg), male SD rats (iv/po: 0.5 mg/kg), and Beagle dogs (iv/po: 0.33 mg/kg) are the mice, rats, and dogs that have the PK parameter[1]. Criteria CL(iv) (mL/min/kg) Vdss(iv) (L/kg) T1/2 (h) Cmax(po) (nM) AUC0-last(po) (nM·h) Bioavailability (F%) Rat 28 1.72 2.0 659 1832 71.1 Dog 4.04 1.08 3.39 4850 26500 93.2
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Cell Assay |
Western Blot Analysis[1]
Cell Types: Northern-Blot Tested Concentrations: 500, 166.67, 55.56, 18.52, 6.17, 2.06, 0.68, 0.23, and 0 nM Incubation Duration: 4, 8, 16, 24, 48 hrs (hours) Experimental Results: Inhibited HBV antigens through inhibition of HBV RNAs. |
References |
[1]. Hu Y, et al. Discovery and preclinical evaluations of GST-HG131, a novel HBV antigen inhibitor for the treatment of chronic hepatitis B infection. Bioorg Med Chem Lett. 2022 Nov 1;75:128977.
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Molecular Formula |
C23H29NO7
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Molecular Weight |
431.48
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CAS # |
2270215-69-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O1C2=CC(OCCCOC)=C(OC)C=C2C2=CC(=O)C(C(O)=O)=CN2[C@H](C(C)(C)C)C1
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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 : 100 mg/mL (231.76 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.79 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 (5.79 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 (5.79 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 | 2.3176 mL | 11.5880 mL | 23.1760 mL | |
5 mM | 0.4635 mL | 2.3176 mL | 4.6352 mL | |
10 mM | 0.2318 mL | 1.1588 mL | 2.3176 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.