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VU0134992 is an Kir4.1 blocker with an IC50 value of 0.97 μM

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $31 | In Stock | In Stock | |
| 10 mg | $54 | In Stock | In Stock | |
| 25 mg | $106 | In Stock | In Stock | |
| 50 mg | $179 | In Stock | In Stock | |
| 100 mg | $297 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $44 | In Stock | In Stock |
| Description | VU0134992 is an Kir4.1 blocker with an IC50 value of 0.97 μM |
| Targets&IC50 | KIR4.1:0.97 µM |
| In vitro | VU0134992 inhibits Kir4.1 with an IC50 value of 0.97 μM and is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50 = 9 μM) at -120 mV.?In thallium (Tl+) flux assays, VU0134992 is greater than 30-fold selective for Kir4.1 over Kir1.1, Kir2.1, and Kir2.2;?is weakly active toward Kir2.3, Kir6.2/SUR1, and Kir7.1;?and is equally active toward Kir3.1/3.2, Kir3.1/3.4, and Kir4.2. |
| In vivo | VU0134992 displayed a large free unbound fraction (fu) in rat plasma (fu = 0.213).?Consistent with the known role of Kir4.1 in renal function, oral dosing of VU0134992 led to a dose-dependent diuresis, natriuresis, and kaliuresis in rats. |
| Synonyms | VU 0134992 |
| Molecular Weight | 411.38 |
| Formula | C20H31BrN2O2 |
| Cas No. | 755002-90-5 |
| Smiles | N(C(COC1=C(Br)C=C(C(C)C)C=C1)=O)C2CC(C)(C)NC(C)(C)C2 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 60 mg/mL (145.85 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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