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VU0134992 is an Kir4.1 blocker with an IC50 value of 0.97 μM
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $68 | In Stock | |
5 mg | $141 | In Stock | |
10 mg | $212 | In Stock | |
25 mg | $358 | In Stock | |
50 mg | $509 | In Stock | |
100 mg | $702 | In Stock | |
200 mg | $947 | In Stock | |
1 mL x 10 mM (in DMSO) | $167 | 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. |
Alias | 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 60 mg/ml (145.85 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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