| Size | Price | Stock | Qty |
|---|---|---|---|
| 2mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
Purity: ≥98%
CY 09 is a novel, potent, selective and direct NLRP3 inhibitor that blocks NLRP3 inflammasome assembly and activation, and exhibits therapeutic effects on mouse models of cryopyrin-associated autoinflammatory syndrome (CAPS) and type 2 diabetes. It binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation.
| ln Vitro |
CY-09 demonstrates responsiveness to monosodium urate (MSU), MSU, ATP-induced caspase-1 activation, and IL-1β walking in LPS-challenged bone marrow-derived macrophages (BMDM) at concentrations of 1 to 10 μM. Death-dependent inhibition. Cytosolic LPS-induced non-canonical NLRP3 activation in BMDM can also be swollen by CY-09 administration. CY-09 buffer activates the NLRP3 inflammasome and has no effect on the LPS-induced priming effect. CY-09 treated major inhibitory factors and found that CY-09 treated the interaction of Flag-NLRP3 and mCherry-NLRP3 in HEK-293T cells, indicating that CY-09 prevented NLRP3 oligomerization [1].
|
|---|---|
| ln Vivo |
The monosodium urate (MSU) injection-induced IL-1β generation and neutrophil influx were significantly suppressed in chambers treated with CY-09, suggesting that CY-09 can prevent MSU-induced NLRP3 inflammasome activation within the chamber. Even when therapy was terminated on day 25, CY-09 treatment raised the even rate of NLRP3 mutations to 30 to 48 days. CY-09 also inhibits the even processing of caspase-1 (caspase-1) channels, which is shown in adipose tissue on a high-fat diet (HFD) [1].
|
| References |
[1]. Jiang H, et al. Identification of a selective and direct NLRP3 inhibitor to treat inflammatory disorders. J Exp Med. 2017 Nov 6;214(11):3219-3238
|
| Molecular Formula |
C19H12F3NO3S2
|
|---|---|
| Molecular Weight |
423.4287
|
| CAS # |
1073612-91-5
|
| SMILES |
O=C(O)C1=CC=C(/C=C(SC(N2CC3=CC=CC(C(F)(F)F)=C3)=S)\C2=O)C=C1
|
| Chemical Name |
4-[[4-Oxo-2-thioxo-3-[[3-(trifluoromethyl)phenyl]methyl]-5-thiazolidinylidene]methyl]benzoic acid
|
| Synonyms |
CY 09 CY-09 CY09
|
| 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 : ≥ 150 mg/mL (~354.25 mM)
H2O : ~1.1 mg/mL (~2.60 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.90 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 (5.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 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 | 2.3617 mL | 11.8083 mL | 23.6167 mL | |
| 5 mM | 0.4723 mL | 2.3617 mL | 4.7233 mL | |
| 10 mM | 0.2362 mL | 1.1808 mL | 2.3617 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
COA