Size | Price | Stock | Qty |
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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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ln Vitro |
VU0134992 hydrochloride has a selectivity for Kir4.1 that is more than thirty times more than that of Kir1.1, Kir2.1, and Kir2.2. Its activity is the same toward Kir3.1/3.2, Kir3.1/3.4, and Kir4.2, but it is weak against Kir2.3, Kir6.2/SUR1, and Kir7.1[1]. Using a well-established Tl+ flux assay, an 11-point CRC experiment was conducted to assess the selectivity of VU0134992 hydrochloride for Kir4.1 against nine other members of the Kir channel family spanning a dose range of 0.3 nM to 30 µM. The study reports that VU0134992 Hydrochloride exhibits the same level of efficacy and potency as VU0134992 when it comes to inhibiting 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).
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ln Vivo |
The oral gavage of VU0134992 hydrochloride (50-100 mg/kg) considerably increases the excretion of K+ and Na+ in the urine [1].
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Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (250-300 g) [1]
Doses: po (oral gavage): 50 and 100 mg/kg Experimental Results: Urinary Na+ and K+ excretion increased Dramatically. |
References |
[1]. Kharade SV, et al. Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992. Mol Pharmacol. 2018 Aug;94(2):926-937.
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Molecular Formula |
C₂₀H₃₂BRCLN₂O₂
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Molecular Weight |
447.84
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CAS # |
1052515-91-9
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Related CAS # |
VU0134992;755002-90-5
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
BrC1C=C(C=CC=1OCC(NC1CC(C)(C)NC(C)(C)C1)=O)C(C)C.Cl
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Synonyms |
VU-0134992 HCl; VU 0134992 HCl
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~250 mg/mL (~558.24 mM)
H2O : ~2.27 mg/mL (~5.07 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.64 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2329 mL | 11.1647 mL | 22.3294 mL | |
5 mM | 0.4466 mL | 2.2329 mL | 4.4659 mL | |
10 mM | 0.2233 mL | 1.1165 mL | 2.2329 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.