8-Bromo-cGMP, sodium salt
(Synonyms: 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) 目录号 : GC101198-Bromo-cGMP是一种可渗透细胞的cGMP类似物,可以诱导PKG激活。
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.
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]。
| Cell experiment [1]: | |
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Cell lines |
Human prostate carcinoma cell line DU145 |
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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]: | |
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Animal models |
4-week-old male and female spontaneously hypertensive rat (SHR) |
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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. | |
| Cas No. | 51116-01-9 | SDF | |
| 别名 | 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 | ||
| Canonical 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 |
| 溶解度 | 10mg in PBS(pH7.2) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2417 mL | 11.2085 mL | 22.417 mL |
| 5 mM | 0.4483 mL | 2.2417 mL | 4.4834 mL |
| 10 mM | 0.2242 mL | 1.1209 mL | 2.2417 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet