| Size | Price | Stock | Qty |
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| 1mg |
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| Targets |
WNK-IN-B targets the WNK (with-no-lysine kinase) signaling pathway, specifically inhibiting WNK4 (IC₅₀ = 16 μM) and WNK1 (IC₅₀ = 34.4 μM). It is a cell-permeable diaminoacridine derivative that binds reversibly to the CCT domain of SPAK and OSR1, downstream effectors of WNK signaling. This pathway regulates ion transport and blood pressure.
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| ln Vitro |
In mDCT cells, L-NAME's action on the phosphorylated sodium chloride cotransporter (NCC) is blocked by STOCK2S-26016 for 10 and 30 minutes [2]. The phosphorylation of STE20/SPS1-associated proline/alanine-rich protein kinase (SPAK) and NCC in mpkDCT cells is greatly reduced in a dose-dependent manner by STOCK2S-26016 (25-200 μM) [1]. In MOVAS cells, the phosphorylation of Na/K/Cl cotransporter 1 (NKCC1) and SPAK is dramatically and dose-dependently reduced by STOCK2S-26016 (50-200 μM) [1].
In vitro, WNK-IN-B inhibits WNK4 and WNK1 with IC₅₀ values of 16 μM and 34.4 μM, respectively. In mDCT cells, it blocks L-NAME's action on the phosphorylated sodium chloride cotransporter (NCC). In mpkDCT cells, it dose-dependently reduces phosphorylation of SPAK and NCC (25-200 μM). In MOVAS cells, it reduces phosphorylation of NKCC1 and SPAK (50-200 μM). |
| ln Vivo |
In vivo activity data for WNK-IN-B are limited. As an inhibitor of WNK signaling, it has potential applications in anti-hypertensive (blood pressure lowering) research. By inhibiting the WNK-SPAK/OSR1-NCC pathway, which regulates sodium reabsorption in the kidney, the compound may lower blood pressure. Further in vivo studies are needed to confirm its efficacy.
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| Enzyme Assay |
In vitro enzyme inhibition assays for WNK-IN-B are performed using purified WNK kinases or cell-based assays measuring downstream phosphorylation events. Kinase activity is assessed by measuring the phosphorylation of substrates such as SPAK, OSR1, NCC, or NKCC1 using phospho-specific antibodies. IC₅₀ values (16 μM for WNK4, 34.4 μM for WNK1) are calculated from concentration-response curves.
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| Cell Assay |
In vitro cellular assays for WNK-IN-B are performed using cell lines such as mDCT, mpkDCT, or MOVAS cells. Cells are treated with the compound at various concentrations (25-200 μM), and phosphorylation of downstream targets (SPAK, OSR1, NCC, NKCC1) is measured by Western blotting using phospho-specific antibodies. Dose-dependent inhibition of phosphorylation is quantified.
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| Animal Protocol |
In vivo animal experiments for WNK-IN-B are not extensively documented. As a potential anti-hypertensive agent, in vivo studies would typically involve administration to rodent models of hypertension. The compound would be administered via intraperitoneal or oral routes, and efficacy would be assessed by measuring blood pressure, electrolyte balance, and phosphorylation of NCC in kidney tissues.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of WNK-IN-B have been characterized in part. The compound has a molecular weight of 333.38 and molecular formula C₂₀H₁₉N₃O₂. It appears as a light yellow to yellow solid powder with a LogP of 3.8. It should be stored as a powder at -20°C for up to 3 years or at 4°C for up to 2 years.
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| Toxicity/Toxicokinetics |
Toxicological data for WNK-IN-B are not extensively reported. As a research-use compound, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
7-Ethoxy-N(3)-(2-furanmethyl)-3,9-acrididine diamine belongs to the aminoacrididine class of compounds. Its structure is acridine-9-amine, with [(furan-2-yl)methyl]amino and ethoxy groups substituted at positions 3 and 7, respectively. It is an inhibitor of the lysine-deficient protein kinase (WNK) signaling pathway (IC50 = 16 μM). It has the function of inhibiting the WNK signaling pathway. This compound belongs to the furans, aminoacrididines, aromatic ethers, and aromatic amines.
WNK-IN-B is also known as Compound B and STOCK2S-26016. Its chemical name is 7-ethoxy-N3-(furan-2-ylmethyl)acridine-3,9-diamine. It is a WNK signaling inhibitor with potential applications in anti-hypertensive research. This product is for research use only. |
| Molecular Formula |
C20H19N3O2
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|---|---|
| Molecular Weight |
333.384
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| Exact Mass |
333.147
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| CAS # |
332922-63-1
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| PubChem CID |
3135086
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
435
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(OC1=CC2C(=NC3=C(C=2N)C=CC(NCC2=CC=CO2)=C3)C=C1)C
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| InChi Key |
PGNWQNJXXLPZEL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H19N3O2/c1-2-24-14-6-8-18-17(11-14)20(21)16-7-5-13(10-19(16)23-18)22-12-15-4-3-9-25-15/h3-11,22H,2,12H2,1H3,(H2,21,23)
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| Chemical Name |
7-ethoxy-3-N-(furan-2-ylmethyl)acridine-3,9-diamine
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| Synonyms |
Compound B; WNK IN B; WNK-IN-B
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ≥ 50 mg/mL (~150.0 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (12.5 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: ≥ 1.25 mg/mL (3.75 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 DMSO stock solution (12.5 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9996 mL | 14.9979 mL | 29.9958 mL | |
| 5 mM | 0.5999 mL | 2.9996 mL | 5.9992 mL | |
| 10 mM | 0.3000 mL | 1.4998 mL | 2.9996 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.
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