Size | Price | |
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100mg | ||
250mg | ||
500mg |
Targets |
p38 MAP kinase
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ln Vitro |
The piperidine analogs MKK7-COV-10 and MKK7-COV-11, as well as the carboxylic acid MKK7-COV-8, demonstrate poor permeability and inactivity in ICW in 3T3 cells. As an amide counterpart, MKK7-COV-9, in contrast, keeps its activity (EC50=4.06 μM) and additionally offers a new vector for further derivatization[1].
MKK7-COV-9 (10 μM; 48 hours) only exhibits a minimally cytotoxic effect at the highest tested concentration. For these two substances, only one cell line, HCT116, showed a half-maximal lethal dose (LD50)<10 μM[1]. Except for the negative control MKK7-NEG-1, MKK7-COV-9 (10 μM; 2 hr pre-incubation) is able to inhibit 60% of the CD86+ response to LPS stimulation in primary mouse B cells. In response to lipopolysaccharide , JNK is known to mediate B cell activation via the TLR4 signaling pathway. Through the TLR4 signaling pathway, MKK7-COV-9 (0–10 M; 2 hr pre-incubation) is able to mediate the activation of B cells in response to LPS; it displays dose-response curves for inhibiting LPS-induced activation and exhibits an EC50 value of μM.(EC50=4.98 μM for MKK7-COV-12; EC50>10 μM for MKK7-COV-7; EC50=2.23 μM for JNK-IN-8)[1]. |
References |
Molecular Formula |
C18H16N4O2
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Molecular Weight |
320.35
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Exact Mass |
320.12732577
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CAS # |
2283355-59-7
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Related CAS # |
2283355-59-7
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Appearance |
Solid
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SMILES |
CNC(=O)C1=CC(=CC(=C1)C2=NNC3=CC=CC=C32)NC(=O)C=C
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InChi Key |
OIVBYXJDKPKZFE-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C18H16N4O2/c1-3-16(23)20-13-9-11(8-12(10-13)18(24)19-2)17-14-6-4-5-7-15(14)21-22-17/h3-10H,1H2,2H3,(H,19,24)(H,20,23)(H,21,22)
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Chemical Name |
3-(1H-indazol-3-yl)-N-methyl-5-(prop-2-enoylamino)benzamide
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Synonyms |
MKK7-COV-9
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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: ~50 mg/mL (~156.1 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.80 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 (7.80 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 (7.80 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 | 3.1216 mL | 15.6079 mL | 31.2159 mL | |
5 mM | 0.6243 mL | 3.1216 mL | 6.2432 mL | |
10 mM | 0.3122 mL | 1.5608 mL | 3.1216 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.