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500mg |
ln Vitro |
The human colorectal partner line (SW480) is treated with templovivint (Compound 175; 0.0003-10 μM) to decrease Wnt/p-catenin activity in a dose-regulated manner (EC50=152.9 nM) [1]. = 25 nM) as well as primary hMSCs (EC50=10.377 μM) from human mesenchymal stem cells [1]. With an EC50 ranging from 139 to 189 nM, teplinovivint (5.8, 10.8, 21.7, 41.7, 83.3, 166.6, 333.3, 750 nM) stimulates the expression of SCXA, tenacinC, and tenomoduLin in a dose-dependent manner [1].
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ln Vivo |
Teplinovivint (Compound 175; 10 mg/mL; given topically once daily for 21 days) reduces inflammation and tendon injury. Teplinovivint causes a decrease in the inflammatory arthritis biomarker KC/GRO in a collagenase-induced muscle damage injury model [1] Teplinovivint (1 mg/mL with 1% BA) had a Tmax of 1 hour in bundles [1].
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References |
[1]. Vishal DESHMUKH, et al. Methods of using indazole-3-carboxamides and their use as wnt/b-catenin signaling pathway inhibitors. WO2018075858A1.
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Molecular Formula |
C25H26N6O2
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Molecular Weight |
442.523
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Exact Mass |
442.2117
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CAS # |
1428064-91-8
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SMILES |
O=C(C1C2=C(C=CC(=C2)C2=CN=CC(=C2)CN2CCCCC2)NN=1)NC1C=NC(=CC=1)OC
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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 : ~83.33 mg/mL (~188.31 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.70 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 (4.70 mM) in 10% DMSO + 90% (20% SBE-β-CD in 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 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2598 mL | 11.2989 mL | 22.5978 mL | |
5 mM | 0.4520 mL | 2.2598 mL | 4.5196 mL | |
10 mM | 0.2260 mL | 1.1299 mL | 2.2598 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.