| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
TC ASK 10 (ASK1 Inhibitor 10) is a novel and potent apoptosis signal-regulating kinase 1 (ASK1) inhibitor ( IC50 = 14 nM).
| ln Vitro |
In INS-1 pancreatic β-cells, treatment with TC ASK 10 (Compound 10; 0–10 μM; 1 hour; INS-1 cells) at 0.3 μM suppresses the JNK that is produced by streptozotocin (STZ). Additionally, p38 phosphorylation is suppressed in a dose-dependent manner [1].
|
|---|---|
| ln Vivo |
Rats were used in the pharmacokinetic profile testing. Oral bioavailability of TC ASK 10 (Compound 10·HCl; rat box at 0.1 mg/kg intravenously and 1 mg/kg orally) is good. For TC ASK 10, 0–8 hours, the Cmax, Tmax, and AUCpo are, respectively, 285.1 ng/mL, 1.67 h, and 275.4 ng.h/mL [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: INS-1 Cell Tested Concentrations: 0 μM, 0.3 μM, 1 μM, 3 μM, 10 μM Incubation Duration: 1 hour Experimental Results: Streptozotocin (STZ) found to inhibit streptozotocin (STZ) in INS- Induced JNK 1 pancreatic beta cells at a concentration of 0.3 μM. Phosphorylation of p38 was also inhibited in a dose-dependent manner. |
| References |
| Molecular Formula |
C21H23CL2N5O
|
|---|---|
| Molecular Weight |
432.346222162247
|
| Exact Mass |
431.127
|
| CAS # |
1005775-56-3
|
| PubChem CID |
68661090
|
| Appearance |
White to pink solid powder
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
29
|
| Complexity |
525
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
IKKLFEDUYFZNBO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H21N5O.2ClH/c1-21(2,3)16-6-4-15(5-7-16)20(27)24-18-13-26-12-17(8-9-19(26)23-18)25-11-10-22-14-25;;/h4-14H,1-3H3,(H,24,27);2*1H
|
| Chemical Name |
4-tert-butyl-N-(6-imidazol-1-ylimidazo[1,2-a]pyridin-2-yl)benzamide;dihydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~231.29 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.78 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 (5.78 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 (5.78 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 | 2.3129 mL | 11.5647 mL | 23.1294 mL | |
| 5 mM | 0.4626 mL | 2.3129 mL | 4.6259 mL | |
| 10 mM | 0.2313 mL | 1.1565 mL | 2.3129 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
