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Chemical Structure| 1052515-91-9 Chemical Structure| 1052515-91-9

Structure of VU0134992 HCl
CAS No.: 1052515-91-9

Chemical Structure| 1052515-91-9

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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.

Synonyms: VU0134992 hydrochloride

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Product Details of VU0134992 HCl

CAS No. :1052515-91-9
Formula : C20H32BrClN2O2
M.W : 447.84
SMILES Code : O=C(NC1CC(C)(C)NC(C)(C)C1)COC2=CC=C(C(C)C)C=C2Br.[H]Cl
Synonyms :
VU0134992 hydrochloride
MDL No. :MFCD05985784

Safety of VU0134992 HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Chinese hamster ovary (CHO) cells 30 µM and 300 µM 2 hours To test the effect of VU0134992 on ENaC-mediated Na+ transport. Results showed that higher concentrations of VU0134992 significantly reduced Na+ transport. Br J Pharmacol. 2022 Jun;179(12):2953-2968
Kir4.1/5.1 concatemeric channels 9.05 µM 20 minutes Evaluate the inhibitory effect of VU0134992 on Kir4.1/5.1 heterotetrameric channels, results show weaker inhibition on Kir4.1/5.1 Mol Pharmacol. 2018 Aug;94(2):926-937
HEK-293 cells 0.97 µM 20 minutes Evaluate the inhibitory effect of VU0134992 on Kir4.1, results show VU0134992 effectively inhibits Kir4.1 channels Mol Pharmacol. 2018 Aug;94(2):926-937
HK-2 cells 5 µM 24 hours To evaluate the protective effect of VU0134992 against polymyxin B-induced toxicity, results showed that VU0134992 significantly reduced polymyxin B-induced cell death Cell Mol Life Sci. 2022 May 15;79(6):296
Mouse cortical collecting duct (mCCD cl1) cells 30 µM 5 minutes To test the effect of VU0134992 on ENaC single-channel activity. Results showed that VU0134992 significantly reduced ENaC single-channel activity. Br J Pharmacol. 2022 Jun;179(12):2953-2968

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Mouse kidney explant culture model Added to culture medium 5 µM Single administration, lasting 20-24 hours To evaluate the protective effect of VU0134992 against polymyxin B-induced kidney toxicity, results showed that VU0134992 significantly reduced polymyxin B-induced apoptosis Cell Mol Life Sci. 2022 May 15;79(6):296
Sprague-Dawley rats Metabolic cage study Oral 50 and 100 mg/kg Single dose, duration of 4 hours Evaluate the effect of VU0134992 on renal function and electrolyte excretion, results show VU0134992 significantly increases urine volume, Na+ and K+ excretion Mol Pharmacol. 2018 Aug;94(2):926-937

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.16mL

2.23mL

1.12mL

22.33mL

4.47mL

2.23mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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