GlpBio

8-Bromo-cGMP, sodium salt

目录号: GC10119纯度: >99.00%同义词: 8-溴代鸟苷-3',5'-环状单磷酸酯钠盐,??8-bromo-cGMP, 8-bromo Guanosine 3’,5’-cyclic monophosphate
8-Bromo-cGMP是一种可渗透细胞的cGMP类似物,可以诱导PKG激活。
8-Bromo-cGMP, sodium salt
Cas No.: 51116-01-9
规格价格库存数量操作
5mg¥630.00现货
1
10mg¥990.00现货
1
25mg¥1,980.00现货
1
50mg¥3,150.00现货
1
100mg¥5,220.00现货
1
10mM (in 1mL Water)¥693.00现货
1
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产品描述 Description

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.

8-Bromo-cGMP是一种可渗透细胞的cGMP类似物,可以诱导PKG激活。8-Bromo-cGMP抑制血管紧张素II或Ca2+积累,并且可以用于疼痛的缓解及抗高血压作用[1,2]。

8-Bromo-cGMP(1nM、100nM 和 10µM) 处理人前列腺癌细胞可以在缺氧条件下(0.2% O2)显著抑制HIF-1α 蛋白积累,而不能改变常氧(20% O2)条件下HIF-1α 蛋白积累。8-Bromo-cGMP可以缓解缺氧诱导的癌症恶性表型[3]。

8-Bromo-cGMP (72µg/kg/min)在自发性高血压大鼠(SHR)中,提高了大鼠的利尿钠反应,同时诱导总皮质匀浆 pSer552-NHE-3的表达,并降低了皮质匀浆中NHE-3和pSer23-NKA的表达。8-Bromo-cGM 激活cGMP信号途径,提高Src和VASP磷酸化的表达。8-Bromo-cGMP是具有抗高血压及尿钠排泄的功能,是高血压相关肾病的潜在治疗手段[4]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Human prostate carcinoma cell line DU145

Preparation Method

DU145 cells were maintained in RPMI 1640 medium. Cells were administered with 8-Bromo-cGMP (1nM, 100nM, and 10µM) for 4 hours in standard conditions (20% O2) or hypoxia conditions (0.2% O2).

Reaction Conditions

1nM, 100nM, and 10µM 8-Bromo-cGMP for 4 hours

Applications

In DU145 cells, 8-Bromo-cGMP inhibited the hypoxic accumulation of HIF-1α protein under hypoxia conditions (0.2% O2). HIF-1α protein levels in cells incubated in standard conditions (20% O2) were unaffected by exposure to 8-Bromo-cGMP.
Animal experiment [2]:

Animal models

4-week-old male and female spontaneously hypertensive rat (SHR)

Preparation Method

The left kidney of SHR received renal interstitial (RI) infusion of 8-Bromo-cGM (72µg/kg/min) for 30min. This procedure was performed 3 times.

Dosage form

72 µg/kg/min, renal interstitial (RI) infusion

Applications

8-Bromo-cGM increased total cortical homogenate pSer552-NHE-3 in SHR, while NHE-3 and pSer23-NKA were decreased by 8-Bromo-cGM. 8-Bromo-cGM induced the expression of cGMP downstream signaling molecules, such as p-Src.

References:

[1]. 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.
[2]. 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.

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号
51116-01-9
同义词
8-溴代鸟苷-3',5'-环状单磷酸酯钠盐,??8-bromo-cGMP, 8-bromo Guanosine 3’,5’-cyclic monophosphate
化学名
8-bromo-guanosine cyclic 3',5'-(hydrogen phosphate), monosodium salt
SMILES
BrC1=NC2=C(NC(N)=NC2=O)N1[C@@H]3O[C@@H]4[C@H]([C@H]3O)O[P@](OC4)([O-])=O.[Na+]
分子式
C10H10BrN5NaO7P
分子量
446.09 g/mol
溶解性
10mg in PBS(pH7.2)
保存条件
Desiccate at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol