| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
| ln Vitro |
The Huh-7.5 cells treated with oltipraz (OPZ) or NK-252 exhibited dose-dependent activation of NAD (P) H quinone oxidoreductase 1 (NQO1)-ARE as evidenced by luciferase activity. Based on the fact that NK-252 exhibits a higher potency for this effect than OPZ, NK-252's EC2 value (concentration induced by two times above background) is 1.36 μM, while OPZ's is 20.8 μM, determined by linearly extrapolating values above and below the induction threshold. NK-252 may function in hepatocytes as a Nrf2 activator. It has been documented that prototypic Nrf2 activators, such as OPZ, shield microglia from the cytotoxicity caused by H2O2. Huh-7 cells were used to assess the antioxidant qualities of OPZ and NK-252 in relation to their ability to protect against H2O2-induced cytotoxicity. When OPZ or NK-252 are applied to cells, they enhance their resistance against H2O2-induced cytotoxicity in comparison to control cells [1].
|
|---|---|
| ln Vivo |
When compared to CDAA control rats, animals on a choline-deficient L-amino acid-defining (CDAA) diet administered OPZ or NK-252 had lower fibrosis scores, with a median score of 3, indicating bridging fibrosis. When compared to rats fed a normal control diet (naïve), the liver fibrosis area in CDAA control rats was nearly 20 times larger (14.7 vs. 0.72%, respectively). by giving either NK-252 or OPZ (5.80% of NK-252_high, 6.20% of NK-252_low, and 4.97% of OPZ). Dose-dependent effects of NK-252 are observed on fibrosis area and score [1]. P388/S and P388/VCR mice showed no anticancer effect from NK-252 alone. When NK-252 was given orally in addition to Etoposide, the mice that were intraperitoneally injected with P388/S lived much longer when compared to when Etoposide was used alone. When compared to the comparable survival time of Etoposide alone, the combined treatment of NK-252 and Etoposide considerably increased the lifespan of mice intraperitoneally vaccinated with P388/VCR [2].
|
| References |
|
| Additional Infomation |
See also: NK 252 (Note moved to).
|
| Molecular Formula |
C13H11N5O3
|
|---|---|
| Molecular Weight |
285.2581
|
| Exact Mass |
285.086
|
| CAS # |
1414963-82-8
|
| PubChem CID |
71618700
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.51
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
21
|
| Complexity |
357
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
FNSCFQXZZNCDAI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H11N5O3/c19-12(15-8-9-4-1-2-6-14-9)16-13-18-17-11(21-13)10-5-3-7-20-10/h1-7H,8H2,(H2,15,16,18,19)
|
| Chemical Name |
1-[5-(furan-2-yl)-1,3,4-oxadiazol-2-yl]-3-(pyridin-2-ylmethyl)urea
|
| 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 : ≥ 29 mg/mL (~101.66 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.29 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 (7.29 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 (7.29 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 | 3.5056 mL | 17.5279 mL | 35.0557 mL | |
| 5 mM | 0.7011 mL | 3.5056 mL | 7.0111 mL | |
| 10 mM | 0.3506 mL | 1.7528 mL | 3.5056 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
