| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
TWIK-related arachidonic acid-stimulated K+ channel (TRAAK).
|
|---|---|
| ln Vitro |
RU-TRAAK-2 shows no activity against non-K2P channels, including Kv1.2, GIRK2, and Slo1, indicating high selectivity for TRAAK. The exact IC50 value for TRAAK inhibition has not been publicly disclosed.
|
| ln Vivo |
RU-TRAAK-2 is widely used in neuroscience research to explore mechanogated ion channel physiology, pain pathways, and neuronal signaling under stress conditions.
|
| Enzyme Assay |
For binding studies, TRAAK channels are expressed in heterologous systems like Xenopus oocytes or HEK293 cells. Whole-cell patch-clamp electrophysiology is performed to measure potassium currents. RU-TRAAK-2 is applied at varying concentrations, and the inhibition of K+ current is measured. Its fully reversible nature is confirmed by washout.
|
| Cell Assay |
The selectivity of RU-TRAAK-2 can be confirmed using cell lines expressing non-K2P channels (e.g., Kv1.2, GIRK2, Slo1). Whole-cell patch-clamp recordings are performed, and the compound shows no significant inhibition of these channels at concentrations active on TRAAK.
|
| Animal Protocol |
A typical in vivo protocol involves administering RU-TRAAK-2 (formulated in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline) via intraperitoneal injection to mice at a dose of 1-10 mg/kg. Its effects on pain behavior are then assessed using models like the formalin test or CFA-induced hyperalgesia.
|
| ADME/Pharmacokinetics |
No specific pharmacokinetic data is publicly available. As a small molecule (MW 335.42) with an alkyne group, it is likely soluble in DMSO, and its LogP is estimated to be around 2-3.
|
| Toxicity/Toxicokinetics |
The acute toxicity of RU-TRAAK-2 has not been formally studied. However, as a TRAAK inhibitor, it may affect neuronal excitability, and high doses could lead to neurotoxicity. For research use, standard laboratory safety precautions should be followed.
|
| References | |
| Additional Infomation |
RU-TRAAK-2 contains an alkyne group and can be used as a click chemistry reagent for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing azide groups.
|
| Molecular Formula |
C19H17N3OS
|
|---|---|
| Molecular Weight |
335.422782659531
|
| Exact Mass |
335.109
|
| CAS # |
1210538-56-9
|
| PubChem CID |
45876004
|
| Appearance |
White to yellow solid powder
|
| LogP |
3.4
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
24
|
| Complexity |
491
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
S1C2C=CC=CC=2N=C1CN(C(NCC#CC1C=CC=CC=1)=O)C
|
| InChi Key |
YIQVUMDINCCARL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H17N3OS/c1-22(14-18-21-16-11-5-6-12-17(16)24-18)19(23)20-13-7-10-15-8-3-2-4-9-15/h2-6,8-9,11-12H,13-14H2,1H3,(H,20,23)
|
| Chemical Name |
1-(1,3-benzothiazol-2-ylmethyl)-1-methyl-3-(3-phenylprop-2-ynyl)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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 50 mg/mL (149.07 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9813 mL | 14.9067 mL | 29.8134 mL | |
| 5 mM | 0.5963 mL | 2.9813 mL | 5.9627 mL | |
| 10 mM | 0.2981 mL | 1.4907 mL | 2.9813 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.