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100mg | ||
250mg | ||
500mg |
ln Vitro |
Nuclear HIF-1 stabilizes in response to TRC160334 (100~400 μM; 4 hours; Hep3B cells) in a dose-dependent manner [1]. Hep3B cells treated with TRC160334 (75~300 μM; 4 hours) exhibit dose-dependent transcriptional activation of HIF-1. HIF target genes, including adrenomedullin and EPO, express themselves in TRC160334 in a dose-dependent manner [1].
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ln Vivo |
TRC160334 (0.1 and 0.3 mg/kg; i.p.) significantly lowers serum creatinine and blood urea nitrogen [1]. TRC160334 (0.3 and 0.6 mg/kg; i.p.) demonstrated a trend toward decreasing acute tubular necrosis [1]. TRC160334 considerably lowers the dose-dependent increase in electrolyte excretion. Pre-ischemia treatment with TRC160334 resulted in considerable induction of HSP70 in the kidney for 6 hours, whereas post-ischemia therapy with TRC160334 resulted in significant induction of HSP70 in the kidney for 12 hours compared to the matching vehicle control [1].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: Hep3B cells Tested Concentrations: 100~400 μM Incubation Duration: 4 hrs (hours) Experimental Results: Result in dose-dependent stabilization of nuclear HIF-1. |
Animal Protocol |
Animal/Disease Models: SD (SD (Sprague-Dawley)) male rats (250–300 g) [1]
Doses: 0.1 and 0.3 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Serum creatinine and blood urea nitrogen were Dramatically diminished. Animal/Disease Models: SD (SD (Sprague-Dawley)) male rats (250–300 g) [1] Doses: 0.3 and 0.6 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: demonstrated a trend towards diminished acute tubular necrosis. |
References |
[1]. Jamadarkhana P, et al. Treatment with a novel hypoxia-inducible factor hydroxylase inhibitor (TRC160334) ameliorates ischemic acute kidney injury. Am J Nephrol. 2012;36(3):208-218.
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Molecular Formula |
C14H15N3O5S
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Molecular Weight |
337.35
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CAS # |
1293289-69-6
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Related CAS # |
1293290-41-1 (sodium);1293290-44-4 (potassium);1293289-69-6 (free acid);1293290-45-5 (calcium);
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SMILES |
S1C2=NC(=C(C(NCC(=O)O)=O)C(N2C2=C1CCCCC2)=O)O
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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 : ~25 mg/mL (~74.11 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.17 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 20.8 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: ≥ 2.08 mg/mL (6.17 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 20.8 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: ≥ 2.08 mg/mL (6.17 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 | 2.9643 mL | 14.8214 mL | 29.6428 mL | |
5 mM | 0.5929 mL | 2.9643 mL | 5.9286 mL | |
10 mM | 0.2964 mL | 1.4821 mL | 2.9643 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.