1052515-91-9
1052515-91-9 structure
- Name: VU0134992 hydrochloride
- Chemical Name: VU0134992 hydrochloride
- CAS Number: 1052515-91-9
- Molecular Formula: C20H32BrClN2O2
- Molecular Weight: 447.84
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel Potassium Channel
- Create Date: 2020-04-07 10:36:30
- Modify Date: 2024-01-14 11:09:27
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VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV[1].
| Name | VU0134992 hydrochloride |
|---|
| Description | VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV[1]. |
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| Related Catalog | |
| In Vitro | VU0134992 hydrochloride 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[1].The selectivity of VU0134992 hydrochloride for Kir4.1 versus nine other members of the Kir channel family was evaluated at concentrations ranging from 0.3 nM to 30 µM in 11-point CRC experiments, using established Tl+ flux assays. VU0134992 hydrochloride inhibits Kir3.1/Kir3.2 (92% inhibition at 30 µM, IC50=2.5 µM), Kir3.1/Kir3.4 (92% inhibition at 30 µM, IC50=3.1 µM), and Kir4.2 (100% inhibition at 30 µM, IC50=8.1 µM) with approximately the same efficacy and potency that VU0134992 inhibits Kir4.1 (100% at 30 µM, IC50=5.2 µM)[1]. |
| In Vivo | VU0134992 hydrochloride (50-100 mg/kg; oral gavage) statistically significantly increased urinary Na+ as well as K+ excretion[1]. Animal Model: Male Sprague-Dawley rats (250-300 g)[1] Dosage: Oral gavage Administration: 50 and 100 mg/kg Result: Statistically significantly increased urinary Na+ as well as K+ excretion. |
| References |
| Molecular Formula | C20H32BrClN2O2 |
|---|---|
| Molecular Weight | 447.84 |