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KR-32568

Cat. No. M7878
KR-32568 Structure
Size Price Availability Quantity
5mg USD 190  USD190 In stock
10mg USD 300  USD300 In stock
25mg USD 600  USD600 In stock
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Biological Activity

KR-32568 is a sodium/hydrogen exchanger-1 (NHE-1) inhibitor with an IC50 value of 0.23 μM.

Chemical Information
Molecular Weight 261.25
Formula C13H12FN3O2
CAS Number 852146-73-7
Form Solid
Solubility (25°C) DMSO 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Weiguo Li, et al. Neurovascular protection in voltage-gated proton channel Hv1 knock-out rats after ischemic stroke: interaction with Na + /H + exchanger-1 antagonism

[2] Qiong Tang, et al. Persistent sodium current and Na+/H+ exchange contributes to the augmentation of the reverse Na+/Ca2+ exchange during hypoxia or acute ischemia in ventricular myocytes

[3] Li-Fang Hu, et al. Hydrogen sulfide regulates Na+/H+ exchanger activity via stimulation of phosphoinositide 3-kinase/Akt and protein kinase G pathways

[4] Hui-Yul Roh, et al. Cardioprotective effects of [5-(2-methyl-5-fluorophenyl)furan-2-ylcarbonyl]guanidine (KR-32568) in an anesthetized rat model of ischemia and reperfusion heart injury

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Zoniporide (CP-597396) hydrochloride hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride hydrate potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM).
Zoniporide hydrochloride

Zoniporide (CP-597396) hydrochloride is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM).
  Catalog
Abmole Inhibitor Catalog




Keywords: KR-32568 supplier, Na+/H+ Exchanger (NHE) , inhibitors, activators

 
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