Procion Blue HB (Reactive Blue 2)
(Synonyms: 蓝色染料; Reactive Blue 2) 目录号 : GC33665
Procion Blue HB (Reactive Blue 2) (Reactive Blue 2) 是一种嘌呤能拮抗剂。
Cas No.:12236-82-7
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Procion Blue HB (Reactive Blue 2) is a purinergic antagonist.
Reactive Blue 2 is used as an ATP receptor antagonist and induces Ca2+ oscillations in HeLa cells. Reactive Blue 2 enhances a Ca2+ response to histamine that is linked to the PLC cascade. Reactive Blue 2 may activate the PLC cascade in an extracellular Ca2+-dependent manner and induce Ca2+ oscillations[1]. The application of Reactive Blue 2 increases K+ secretion in a dose-dependent manner, and this increase is characterized as a peak followed by a partial relaxation to a steady-state. Reactive Blue 2 has antagonistic activities at P2Y4, and the antagonist potency at P2Y4 paralleled the potency of K+ secretion[2].The anthraquinone dye reactive blue 2 is found to be a potent inhibitor of a protein kinase isolated and purified from thylakoids. The mode of inhibition is noncompetitive, with a Ki of 8 μM for the membrane-bound kinase, and 6 microM for the purified kinase. The inhibitor does not modify the substrate preference of the endogenous kinase and could be removed from the membrane by washing[3]. Reactive blue 2 selectively inhibits responses mediated via the P2ypurinoceptor, at least within a limited concentration range. In preparations where the tone has been raised with noradrenaline, ATP and 2-methylthio ATP, but not α,β-methylene ATP, produce relaxations of the vessel. These relaxations are inhibited in the presence of reactive blue 2[4]. Reactive blue 2, at concentrations of 0.3-10 μM blocks the ATP-induced oscillation in a concentration-dependent manner[5].
[1]. Okuda A, et al. Reactive blue 2 induces calcium oscillations in HeLa cells. Jpn J Physiol. 2001 Jun;51(3):389-93. [2]. Lee JH, et al. Reactive blue 2, an antagonist of rat P2Y4, increases K+ secretion in rat cochlea strial marginal cells. Hear Res. 2006 Sep;219(1-2):66-73. [3]. Coughlan SJ, et al. Reactive blue 2 is a potent inhibitor of a thylakoid protein kinase. Eur J Biochem. 1991 Apr 23;197(2):467-71. [4]. Burnstock G, et al. P2-purinoceptors of two subtypes in the rabbit mesenteric artery: reactive blue 2 selectively inhibits responses mediated via the P2y-but not the P2x-purinoceptor. Br J Pharmacol. 1987 Feb;90(2):383-91. [5]. Uneyama H, et al. Suramin and reactive blue 2 are antagonists for a newly identified purinoceptor on rat megakaryocyte. Br J Pharmacol. 1994 Jan;111(1):245-9.
| Cas No. | 12236-82-7 | SDF | |
| 别名 | 蓝色染料; Reactive Blue 2 | ||
| Canonical SMILES | O=S(C(C(N)=C1C2=O)=CC(NC3=CC=C(NC4=NC(Cl)=NC(NC5=CC=CC(S(=O)(O)=O)=C5)=N4)C(S(=O)(O)=O)=C3)=C1C(C6=C2C=CC=C6)=O)(O)=O.O=S(C(C(N)=C7C8=O)=CC(NC9=CC=C(NC%10=NC(Cl)=NC(NC%11=CC=C(S(=O)(O)=O)C=C%11)=N%10)C(S(=O)(O)=O)=C9)=C7C(C%12=C8C=CC=C%12)=O)(O)=O | ||
| 分子式 | C29H20ClN7O11S3 | 分子量 | 774.16 |
| 溶解度 | DMSO : ≥ 110 mg/mL (142.09 mM);Water : 10 mg/mL (12.92 mM);Ethanol : < 1 mg/mL (insoluble) | 储存条件 | 4°C, protect from light |
| 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。 |
||
| 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 | 1.2917 mL | 6.4586 mL | 12.9172 mL |
| 5 mM | 0.2583 mL | 1.2917 mL | 2.5834 mL |
| 10 mM | 0.1292 mL | 0.6459 mL | 1.2917 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Evaluation of Reactive Blue 2 derivatives as selective antagonists for P2Y receptors
Vascul Pharmacol 2002 Dec;39(6):309-15.PMID:14567069DOI:10.1016/s1537-1891(03)00030-2.
P2Y receptor pharmacology is hampered by a lack of subtype selective antagonists. However, a recent study evaluated series of compounds, structurally related to the dye Reactive Blue 2, for their antagonist selectivity at P2X vs. P2Y receptors. Acid blue 129, acid blue 80, acid blue 25 and acid violet 34 were found to be the most potent of the antagonists studied, at P2Y receptors [Naunyn Schmiedeberg's Arch. Pharmacol. 357 (1998) 111]. In this study, we have determined the ability of these four agents to selectively antagonize inositol phosphate turnover mediated by P2Y1 and P2Y2 receptors that are natively expressed in bovine aortic endothelial (BAE) cells. Acid blue 129, acid blue 80, and acid violet 34 shifted the dose-response curve of the P2Y1 agonist 2-methylthio adenosine trisphosphate (2MeSATP) to the right. Acid blue 129 and acid blue 80 were also very weak antagonists of the P2Y2 agonist uridine 5'-triphosphate (UTP). At 30 and 100 microM, acid violet 34 failed to have any significant effect on the dose-response to UTP. However, at 10 microM, acid violet 34 enhanced the UTP responses. Acid blue 80, acid blue 129 and acid violet 34 are P2Y vs. P2X selective, but show poor selectivity between P2Y1 and P2Y2 receptors and are therefore of limited use in the field of P2Y receptor pharmacology. Furthermore, contrary to previous reports, acid blue 25 is not a P2Y-selective antagonist.
Antagonism by Reactive Blue 2 but not by brilliant blue G of extracellular ATP-evoked responses in PC12 phaeochromocytoma cells
Br J Pharmacol 1991 Apr;102(4):851-4.PMID:1855114DOI:10.1111/j.1476-5381.1991.tb12265.x.
1. The effects of Reactive Blue 2 and brilliant blue G, which have been shown to block extracellular ATP-evoked responses, were investigated to discover whether these compounds act as P2-purinoceptor antagonists in PC12 phaeochromocytoma cells. 2. Reactive Blue 2 (10 to 100 microM) suppressed the ATP-stimulated dopamine secretion from PC12 cells in a dose-dependent manner. The concentration-response curve for ATP was shifted to the right and the maximal response was decreased by reactive blue (30 and 100 microM). Brilliant blue G (up to 100 microM) did not significantly affect the secretion. 3. Reactive Blue 2 (10 to 100 microM) suppressed the ATP-activated inward current recorded from the voltage-clamped cells in a concentration-dependent manner. Brilliant blue G (up to 100 microM) did not affect the current. 4. The results suggest that Reactive Blue 2 but not brilliant blue G is a P2-purinoceptor antagonist in PC12 cells. The purinoceptors in these cells may be the same type as those involved in ATP-evoked smooth muscle relaxation, judging from the antagonism by Reactive Blue 2.
Coomassie Brilliant Blue G is a more potent antagonist of P2 purinergic responses than Reactive Blue 2 (Cibacron Blue 3GA) in rat parotid acinar cells
Biochem Biophys Res Commun 1989 Dec 29;165(3):1279-85.PMID:2610693DOI:10.1016/0006-291x(89)92741-1.
The ability of Brilliant Blue G (Coomassie Brilliant Blue G) and Reactive Blue 2 (Cibacron Blue 3GA) to block the effects of extracellular ATP on rat parotid acinar cells was examined by evaluating their effects on ATP-stimulated 45Ca2+ entry and the elevation of [Ca2+]i (Fura 2 fluorescence). ATP (300 microM) increased the rate of Ca2+ entry to more than 25-times the basal rate and elevated [Ca2+]i to levels more than three times the basal value. Brilliant Blue G and Reactive Blue 2 greatly reduced the entry of 45Ca2+ into parotid cells, but the potency of Brilliant Blue G (IC50 approximately 0.4 microM) was about 100-times that of Reactive Blue 2. Fura 2 studies demonstrated that inhibitory concentrations of these compounds did not block the cholinergic response of these cells, thus demonstrating the selectivity of the dye compounds for purinergic receptors. Unlike Reactive Blue 2, effective concentrations of Brilliant Blue G did not substantially quench Fura 2 fluorescence. The greater potency of Brilliant Blue G suggests that it may be very useful in identifying P2-type purinergic receptors, especially in studies which utilize fluorescent probes.
Interaction of 4-carboxy-2-hydroxymuconate-6-semialdehyde dehydrogenase with Reactive Blue 2 and related dyes
J Biochem 1988 Apr;103(4):714-21.PMID:3170510DOI:10.1093/oxfordjournals.jbchem.a122334.
Steady-state kinetic analyses suggest that Pseudomonas ochraceae 4-carboxy-2-hydroxymuconate-6-semialdehyde dehydrogenase (4-carboxy-2-hydroxy-cis,cis-muconate-6-semialdehyde: NADP+ oxidoreductase [EC 1.2.1.45]) functions through an ordered BiBi mechanism. The enzyme binds one NADP+ molecule per subunit with a Kd of 4.8 +/- 0.8 microM. The enzyme is adsorbed to a Blue Sepharose CL-6B column and can be eluted therefrom with reagents having high affinity for the enzyme such as NADP+, NAD+, ATP, and Reactive Blue 2. Equilibrium dialysis and difference spectral titration show the binding of four molecules of Reactive Blue 2 per enzyme subunit. Two of these dye molecules show high-affinity binding with a Kd of 0.03 +/- 0.02 microM. The resulting 1: 2 enzyme-dye complex can be isolated by gel filtration on Bio-Gel P-6. The kinetic, spectroscopic, and chromatographic properties of the complex indicate that the dye-binding sites are different from the coenzyme binding site. The other two dye molecules, in contrast, bind loosely with a Kd of 0.8 +/- 0.5 microM to a site overlapping the coenzyme binding site. This is confirmed by the following findings: NADP+ effectively abolishes the difference spectrum associated with the enzyme-dye binding, and the slope of the double reciprocal plot showing the competitive inhibition of the dye (Ki = 0.20 +/- 0.02 microM) with respect to NADP+ linearly depends on the square of the dye concentration. Essentially similar results are also obtained with methoxy Reactive Blue 2 and Reactive Blue 4.(ABSTRACT TRUNCATED AT 250 WORDS)
Reactive Blue 2, an antagonist of rat P2Y4, increases K+ secretion in rat cochlea strial marginal cells
Hear Res 2006 Sep;219(1-2):66-73.PMID:16839719DOI:10.1016/j.heares.2006.05.011.
Extracellular ATP decreases K+ secretion in strial marginal cells via apical P2Y4 receptors. We investigated the effect of Reactive Blue 2 (RB-2), an antagonist of rat P2Y4, on rat strial marginal cells using a voltage-sensitive vibrating probe. The application of RB-2 increased K+ secretion in a dose-dependent manner, and this increase was characterized as a peak followed by a partial relaxation to a steady-state. Moreover, this response was similar to that caused by 4,4'-diisothiocyanatostilbene-2,2'-disulfonic acid (DIDS). Suramin had no similar effect, except at high concentration. Thus, we tested the effects of these chemicals on P2Y4 receptors in strial marginal cells. Both RB-2 and DIDS had antagonistic activities at P2Y4, and the antagonist potency at P2Y4 paralleled the potency of K+ secretion. Interestingly, 2'- and 3'-O-(4-benzoyl-benzoyl)adenosine 5'-triphosphate (BzATP) exhibited an agonistic effect at P2Y4 receptor, which was blocked by RB-2, but not by pyridoxalphosphate-6-azophenyl-2',4'-disulfonic acid (PPADS). Based on these results, we speculate that direct and/or indirect inhibitory mechanisms between P2Y4 and KENQ1/KCNE1 K+ channels exist in strial marginal cell.