VU0134992 hydrochloride NEW
| Price | $34 | $55 | $98 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: VU0134992 hydrochloride | CAS No.: 1052515-91-9 |
| Purity: 100% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | VU0134992 hydrochloride |
| Description | VU0134992 hydrochloride is the first subtype-preferring, orally active and selective blocker of the Kir4.1 potassium channel pore (IC50: 0.97 μM). |
| Animal Research | VU0134992 hydrochloride (250-300 g Male Sprague-Dawley rats;50 and 100 mg/kg) Oral gavage |
| In vitro | In whole-cell patch-clamp electrophysiology experiments, VU0134992 inhibits Kir4.1 with an IC50 value of 0.97 M and is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50 = 9 M) 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. This potency and selectivity profile is superior to Kir4.1 inhibitors amitriptyline, nortriptyline, and fluoxetine. Medicinal chemistry identified components of VU0134992 that are critical for inhibiting Kir4.1. Patch-clamp electrophysiology, molecular modeling, and site-directed mutagenesis identified pore-lining glutamate 158 and isoleucine 159 as critical residues for block of the channel. |
| 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.Thus, VU0134992 represents the first in vivo active tool compound for probing the therapeutic potential of Kir4.1 as a novel diuretic target for the treatment of hypertension. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 230 mg/mL (513.58 mM), Sonication is recommended. |
| Keywords | VU0134992 | oral | hypertension | patch-clamp | electrophysiology | Kir4.1 | VU 0134992 | Inhibitor | natriuresis | inhibit | VU-0134992 hydrochloride | whole-cell | VU-0134992 Hydrochloride | VU0134992 Hydrochloride | selective | kaliuresis | VU0134992 hydrochloride | VU 0134992 Hydrochloride | Potassium Channel | KcsA | VU-0134992 | diuresis |
| Inhibitors Related | Minoxidil sulfate | Quinine | (±)-Naringenin | Tolbutamide | Tetraethylammonium bromide | Halothane | Butamben | Tetraethylammonium chloride | Cloperastine hydrochloride | 2,2,2-Trichloroethanol | Chlorzoxazone | Indapamide |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | NO PAINS Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Potassium Channel Targeted Library | Ion Channel Targeted Library | Anti-Cancer Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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