Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
Purity: ≥98%
RIPA-56 is a novel, highly potent, selective, and metabolically stable inhibitor of receptor-interacting protein 1 (RIP1) with an IC50 of 13 nM. Tumor necrosis factor alpha (TNFα)-induced mortality and multiorgan damage were successfully decreased by RIPA-56. RIPA-56 is more effective in animal model studies, much more stable in vivo, and potent in both human and murine cells compared to other known RIP1 inhibitors.
Targets |
RIP1 (IC50 = 13 nM)
|
---|---|
ln Vitro |
RIPA-56 shows efficient inhibition of RIP1 kinase activity, with an IC50 of 13 nM.At a 10 µM concentration, it showed no evidence of inhibiting RIP3 kinase activity. Based on the 13 nM RIP1 ADP-Glo activity, RIPA-56 does not inhibit IDO activity at a concentration of 200 µM, which is thought to have a 10,000-fold selectivity window[1].
|
ln Vivo |
RIPA-56 has an impressive in vivo PK profile in mice, with a 3.1 h half-life, 22% oral bioavailability (PO), and 100% bioavailability from intraperitoneal injection (IP). RIPA-56 is very good at crossing the blood–brain barrier. RIPA-56 effectively decreased mortality and multi-organ damage brought on by tumor necrosis factor alpha (TNFα) in the SIRS mouse disease model[1].
|
Cell Assay |
Cell necrosis assay is performed in 96-well cell culture plate. Each well receives 3,000 cells, which are then cultured at 37°C over night. For 24 hours, HT-29 cells are treated with 20 ng/mL TNF, 100 nM Smac Mimetics, 20 μM z-VAD-FMK, and RIPA-56. 20 ng/mL TNFα/20 μM z-VAD-FMK, and RIPA-56 are applied to L929 cells and left on the cells for 6 hours. The Cell Titer-Glo Luminescent Cell Viability Assay kit[1] is used to calculate the cell survival ratio.
|
References |
Molecular Formula |
C13H19NO2
|
---|---|
Molecular Weight |
221.29546380043
|
Exact Mass |
221.14
|
Elemental Analysis |
C, 70.56; H, 8.65; N, 6.33; O, 14.46
|
CAS # |
1956370-21-0
|
Appearance |
Solid powder
|
SMILES |
CCC(C)(C)C(=O)N(CC1=CC=CC=C1)O
|
InChi Key |
AVYVHIKSFXVDBG-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C13H19NO2/c1-4-13(2,3)12(15)14(16)10-11-8-6-5-7-9-11/h5-9,16H,4,10H2,1-3H3
|
Chemical Name |
N-benzyl-N-hydroxy-2,2-dimethylbutanamide
|
Synonyms |
RIPA-56; RIPA-56; RIPA-56
|
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: ~44 mg/mL (~198.8 mM)
Ethanol: ~ 44 mg/mL (~198.8 mM) |
---|
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.5188 mL | 22.5938 mL | 45.1875 mL | |
5 mM | 0.9038 mL | 4.5188 mL | 9.0375 mL | |
10 mM | 0.4519 mL | 2.2594 mL | 4.5188 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.