| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
| ln Vitro |
In a dose-dependent manner, SOD1-Derlin-1 inhibitor-2 (compound 56-59; 0.1-100 μM) suppresses the SOD1-Derlin-1 response [1].
|
|---|---|
| ln Vivo |
SOD1-Derlin-1 inhibitor-2 (compound 56-59; icv; 3 mM, flow rate 0.15 μL/h) improves ALS pathology in ALS model mice [1].
|
| Animal Protocol |
Animal/Disease Models: ALS model C57BL/6 mice[1]: 3 mM, flow rate 0.15 μL/h
Route of Administration: intracerebroventricular injection Experimental Results: Dramatically delayed onset, with a median time of 4.5 weeks (14.5% improvement), and prolonged survival period, with a median time of 5 weeks (14.2% improvement). |
| References |
[1]. Tsuburaya N, et al. A small-molecule inhibitor of SOD1-Derlin-1 interaction ameliorates pathology in an ALS mouse model. Nat Commun. 2018 Jul 10;9(1):2668.
|
| Molecular Formula |
C22H18N4OS
|
|---|---|
| Molecular Weight |
386.469522953033
|
| Exact Mass |
386.12
|
| Elemental Analysis |
C, 68.37; H, 4.69; N, 14.50; O, 4.14; S, 8.30
|
| CAS # |
2170170-27-9
|
| PubChem CID |
132251324
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
4.7
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
28
|
| Complexity |
553
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
NQWFEZIEBLGBMV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H18N4OS/c1-2-13-26(16-8-4-3-5-9-16)22(27)20-19(23)17-10-11-18(25-21(17)28-20)15-7-6-12-24-14-15/h2-12,14H,1,13,23H2
|
| Chemical Name |
3-amino-N-phenyl-N-prop-2-enyl-6-pyridin-3-ylthieno[2,3-b]pyridine-2-carboxamide
|
| Synonyms |
SOD1-Derlin-1 inhibitor 56-59; SOD1-Derlin-1 inhibitor-2; 2170170-27-9; SCHEMBL19737511; EX-A7213;
|
| 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 |
| 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 : ~50 mg/mL (~129.38 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.47 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 (6.47 mM) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5875 mL | 12.9376 mL | 25.8752 mL | |
| 5 mM | 0.5175 mL | 2.5875 mL | 5.1750 mL | |
| 10 mM | 0.2588 mL | 1.2938 mL | 2.5875 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
