8-Bromo-cGMP, sodium salt (Synonyms: 8-bromo-cGMP, 8-bromo Guanosine 3’,5’-cyclic monophosphate) |
| カタログ番号GC10119 |
8-Bromo-cGMP、ナトリウム塩、cGMP の膜透過性類似体は、PKG (プロテインキナーゼ G) 活性化因子です。
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Cas No.: 51116-01-9
Sample solution is provided at 25 µL, 10mM.
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8-Bromo-cGMP is a cell-permeable cGMP analog that induces PKG activation. 8-Bromo-cGMP inhibits angiotensin II or Ca2+ accumulation and can be used for pain relief and antihypertensive effects [1,2].
8-Bromo-cGMP (1nM, 100nM, and 10µM) was used to treat human prostate cancer cells and can significantly inhibit HIF-1α protein accumulation under hypoxic conditions hypoxia conditions (0.2% O2) but has no effect on HIF-1α protein accumulation under standard conditions (20% O2). 8-Bromo-cGMP alleviates the malignant phenotype of cancer induced by hypoxia [3].
8-Bromo-cGMP (72µg/kg/min) increased the natriuretic response of rats in spontaneously hypertensive rats (SHR). The expression of total cortical homogenate pSer552-NHE-3 was enhanced by 8-Bromo-cGMP, while NHE-3 and pSer23-NKA were decreased. 8-Bromo-cGM treatment activates the cGMP signaling pathway by increasing the phosphorylation of Src and VASP. 8-Bromo-cGMP has anti-hypertensive and natriuretic functions [4].
References:
[1]. Rashatwar SS, Cornwell TL, Lincoln TM. Effects of 8-bromo-cGMP on Ca2+ levels in vascular smooth muscle cells: possible regulation of Ca2+-ATPase by cGMP-dependent protein kinase. Proc Natl Acad Sci U S A. 1987 Aug;84(16):5685-9. doi: 10.1073/pnas.84.16.5685. PMID: 3039502; PMCID: PMC298927.
[2]. Sandoval A, Duran P, Gandini MA, Andrade A, Almanza A, Kaja S, Felix R. Regulation of L-type CaV1.3 channel activity and insulin secretion by the cGMP-PKG signaling pathway. Cell Calcium. 2017 Sep;66:1-9. doi: 10.1016/j.ceca.2017.05.008. Epub 2017 May 15. PMID: 28807144; PMCID: PMC5776030.
[3]. Kim J, Barsoum IB, Loh H, ParÉ JF, Siemens DR, Graham CH. Inhibition of hypoxia-inducible factor 1α accumulation by glyceryl trinitrate and cyclic guanosine monophosphate. Biosci Rep. 2020 Jan 31;40(1):BSR20192345. doi: 10.1042/BSR20192345. PMID: 31912870.
[4]. Kemp BA, Howell NL, Gildea JJ, Keller SR, Carey RM. Identification of a Primary Renal AT2 Receptor Defect in Spontaneously Hypertensive Rats. Circ Res. 2020 Feb 28;126(5):644-659. doi: 10.1161/CIRCRESAHA.119.316193. Epub 2020 Jan 30. PMID: 31997705.
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