| Bioactivity | HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models[1][2][3]. | |||||||||
| Target | cyclic GMP-dependent protein kinase, cyclic AMP-dependent protein | |||||||||
| In Vivo | HA-1004 (40 nmol/day；由微型泵注入，流速=1 μL/h) 与吗啡同时作用，在大鼠中拮抗吗啡戒断时 ERK1/2 和 TH 的磷酸化，抑制 NA 转换的增加[1]。 | |||||||||
| Name | HA-1004 | |||||||||
| CAS | 91742-10-8 | |||||||||
| Formula | C12H15N5O2S | |||||||||
| Molar Mass | 293.34 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
|
|||||||||
| Reference | [1]. Almela P, et al. Crosstalk between G protein-coupled receptors (GPCRs) and tyrosine kinase receptor (TXR) in the heart after morphine withdrawal. Front Pharmacol. 2013 Dec 27;4:164. [2]. Goodman HM, et al. The isoquinoline sulfonamide inhibitors of protein phosphorylation, H-7, H-8, and HA-1004, also inhibit RNA synthesis: studies on responses of adipose tissue to growth hormone. Endocrinology. 1990 Jan;126(1):441-50. [3]. Ishikawa T, et al. Relaxation of vascular smooth muscle by HA-1004, an inhibitor of cyclic nucleotide-dependent protein kinase. J Pharmacol Exp Ther. 1985 Nov;235(2):495-9. |