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HA-1004 dihydrochloride

HA-1004 dihydrochloride
HA-1004 dihydrochloride is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel protein
Catalog No. T8681Cas No. 92564-34-6
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HA-1004 dihydrochloride

Catalog No. T8681Cas No. 92564-34-6

HA-1004 dihydrochloride is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel protein
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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1 mg$3706-8 weeks
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Product Introduction

Bioactivity
Description
HA-1004 dihydrochloride is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel protein
In vivo
HA-1004, was shown to be a potent inhibitor of two cyclic nucleotide-dependent protein kinases, cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein kinase and the Ki values were 1.4 and 2.3 microM, respectively.?HA-1004 relaxed rabbit aortic strips contracted by various agonists and with similar ED50 values.?Phenotolamine, propranolol and atropine did not affect this HA-1004-induced relaxation, thereby suggesting that this compound does not act through these membrane receptor associated mechanisms.?HA-1004 shifted the dose-response curve for CaCl2 to the right in a competitive manner in depolarized rabbit renal arterial strips.?This compound also relaxed the A-23187 and phenylephrine-induced contractions elicited in Ca++-free solution.?HA-1004 exerts its action at the intracellular or submembranal level.?This vasodilator has little effect on actomyosin adenosine triphosphatase and Ca++-calmodulin-dependent myosin light chain kinase.?Studies using its derivatives with various lengths of alkyl chain (C0-C6) indicated that the potencies of these compounds, as vasorelaxants, correlated well with their potential to inhibit cyclic nucleotide-dependent protein kinase.?HA-1004 should be a useful tool for investigating in smooth muscle, regulatory mechanism(s) by second messengers, cyclic AMP and cyclic GMP[1].
Chemical Properties
Molecular Weight329.81
FormulaC12H16ClN5O2S
Cas No.92564-34-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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