CAY10512
Based on 1 Customer Validation
CAY10512 is a NF-κB inhibitor. CAY10512 can suppress the upregulation of NF-κB-sensitive proinflammatory miRNAs (miRNA-9, miRNA-125b, miRNA-146a, miRNA-155) in cerebrospinal fluid and extracellular fluid. CAY10512 significantly reduces the release of pro-inflammatory cytokines (such as TNF-α, MCP-1, IL-8, IL-6). CAY10512 can be used for researchs on neuroinflammation, islet transplantation and microRNA regulation.
For research use only. We do not sell to patients.
- Purity : 97.0%
- CAS No.: 139141-12-1
- Formula: C15H13FO
- Molecular Weight:228.26
-
Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
-
HY-78131B
(R)-(-)-IbuprofenNF-κB Inhibitor -
HY-10257
BAY 11-7085NF-κB Activation Inhibitor -
HY-18935A
CBL0137 hydrochlorideNF-κB Inhibitor -
HY-N0492
α-Lipoic AcidAntioxidant -
HY-32735
TriptolideImmunosuppressive Agent -
HY-N0191
AndrographolideNF-κB Inhibitor -
HY-N0141
ParthenolideNF-κB Inhibitor -
HY-N2065
Withaferin ANF-κB Inhibitor -
HY-124958
NDMC101Osteoclastogenesis Inhibitor -
HY-126307
Urolithin BNF-κB Inhibitor -
HY-13812
QNZTNF Receptor Inhibitor -
HY-78131BR
(R)-(-)-Ibuprofen (Standard)NF-κB Inhibitor
Biological Activity
Description
|
NF-κB |
IL-6 |
IL-8 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
0.15 μM
Compound: 6p
|
Inhibition of TNF-alpha-induced NF-kappaB activation in HEK293T cells
Inhibition of TNF-alpha-induced NF-kappaB activation in HEK293T cells
|
[PMID: 17125270] |
| HepG2 | EC50 |
5.4 μM
Compound: 1; LD55
|
Activation of Nrf2 (unknown origin) expressed in human HepG2 cells after 5 hrs by ARE-driven luciferase reporter gene assay
Activation of Nrf2 (unknown origin) expressed in human HepG2 cells after 5 hrs by ARE-driven luciferase reporter gene assay
|
[PMID: 28126440] |
In Vitro
CAY10512 (5 μM, 0-96 h) effectively inhibits miRNA-9, miRNA-125b, miRNA146a and miRNA-155 upregulation in HNG cells stimulated by AD-ECF[1].
CAY10512 (0.15 μM, 1-7 h) significantly protects pancreatic islet viability and effectively alleviates pancreatic islet cell damage by inhibiting the increase of pro-inflammatory factors and the expression of tissue factor TF in primary human islets[2].
CAY10512 (0.25 μM, 25 h) significantly inhibits the gene and protein expressions of pro-inflammatory factor IL-6 and inflammatory receptor TNFR2 induced by MR agonists (Aldosterone (HY-113313), 11-dehydrocorticosterone (HY-113447)) in BV-2 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Primary human islets
-
Concentration:0.15 μM
-
Incubation Time:Pre-treat for one hour, then mix with autologous blood and incubate for another 1, 3, 6 h
-
Result:Prevented the increase of TNF-α, MCP-1, IL-8 and IL-6.
-
Cell Line:BV-2 cells
-
Concentration:0.25 μM
-
Incubation Time:Pre-treatment for 1 hour, then add the stimulus and incubate for 24 hours
-
Result:Completely blocked the upregulation of IL-6 mRNA induced by Aldosterone and the upregulation of TNFR2 mRNA induced by 11-dehydrocorticosterone.
-
Cell Line:BV-2 cells
-
Concentration:0.25 μM
-
Incubation Time:Pre-treatment for 1 hour, then add the stimulus and incubate for 24 hours
-
Result:Completely blocked the phosphorylation of ILp65 induced by aldosterone and its translocation to the nucleus, as well as the upregulation of TNFR2 protein levels induced by 11-dehydrocorticosterone.
Chemical Information
-
CAS No. 139141-12-1
-
Appearance Solid
-
Molecular Weight 228.26
-
Formula C15H13FO
-
Color White to off-white
-
SMILES
COC(C=C1)=CC=C1/C=C/C2=C(C=CC=C2)F
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 33.33 mg/mL (146.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (10.95 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (276 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[1]. Alexandrov P N, et al. microRNA (miRNA) speciation in Alzheimer’s disease (AD) cerebrospinal fluid (CSF) and extracellular fluid (ECF)[J]. International journal of biochemistry and molecular biology, 2012, 3(4): 365. [Content Brief]
[2]. Kanak MA, et al. Alleviation of instant blood-mediated inflammatory reaction in autologous conditions through treatment of human islets with NF-κB inhibitors. Transplantation. 2014 Sep 15;98(5):578-84. [Content Brief]
[3]. Chantong B, et al. Mineralocorticoid and glucocorticoid receptors differentially regulate NF-kappaB activity and pro-inflammatory cytokine production in murine BV-2 microglial cells. J Neuroinflammation. 2012 Nov 28;9:260. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.3810 mL | 21.9048 mL | 43.8097 mL | 109.5242 mL |
| 5 mM | 0.8762 mL | 4.3810 mL | 8.7619 mL | 21.9048 mL | |
| 10 mM | 0.4381 mL | 2.1905 mL | 4.3810 mL | 10.9524 mL | |
| 15 mM | 0.2921 mL | 1.4603 mL | 2.9206 mL | 7.3016 mL | |
| 20 mM | 0.2190 mL | 1.0952 mL | 2.1905 mL | 5.4762 mL | |
| 25 mM | 0.1752 mL | 0.8762 mL | 1.7524 mL | 4.3810 mL | |
| 30 mM | 0.1460 mL | 0.7302 mL | 1.4603 mL | 3.6508 mL | |
| 40 mM | 0.1095 mL | 0.5476 mL | 1.0952 mL | 2.7381 mL | |
| 50 mM | 0.0876 mL | 0.4381 mL | 0.8762 mL | 2.1905 mL | |
| 60 mM | 0.0730 mL | 0.3651 mL | 0.7302 mL | 1.8254 mL | |
| 80 mM | 0.0548 mL | 0.2738 mL | 0.5476 mL | 1.3691 mL | |
| 100 mM | 0.0438 mL | 0.2190 mL | 0.4381 mL | 1.0952 mL |
CAY10512 Related Classifications
HY-120269 Related Classifications
Powered by Bioz