1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. α,β-Methylene-ATP trisodium

α,β-Methylene-ATP trisodium 

目录号: HY-108652 纯度: 99.75%
COA 产品使用指南 技术支持

α,β-Methylene-ATP trisodium 是 P2X1P2X3 受体的激动剂,能够透过血脑屏障。α,β-Methylene-ATP trisodium 可通过激活外周肌肉和中枢蓝斑核 (LC) 的 P2X 受体,引发反射性升压反应;该效应可被 P2X 拮抗剂 PPADS (HY-108960) 阻断。α,β-Methylene-ATP trisodium 还激活中枢蓝斑核的去甲肾上腺素能神经元,介导抗伤害作用;该效应可被蓝斑核损伤剂 DSP-4 (HY-103210/HY-121602) 削弱。α,β-Methylene-ATP trisodium 可用于研究神经性疼痛病理机制、心血管反射调节及中枢神经系统的抗伤害作用。

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α,β-Methylene-ATP trisodium

α,β-Methylene-ATP trisodium Chemical Structure

CAS No. : 1343364-54-4

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Other Forms of α,β-Methylene-ATP trisodium:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

α,β-Methylene-ATP trisodium is an agonist of P2X1 and P2X3 receptors and can cross the blood-brain barrier. α,β-Methylene-ATP trisodium can trigger a reflex pressor response by activating P2X receptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP trisodium also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP trisodium can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system[1][2][3].

IC50 & Target

p2x1 Receptor

 

P2X3 Receptor

 

P2X7 Receptor

 

体外研究
(In Vitro)

电生理活性:
α,β-Methylene-ATP trisodium (10 μM;3 秒) 在大鼠背根神经节 (DRG) 神经元中诱发快速内向电流,与 P2X3 受体激活有关。10 μM Diinosine pentaphosphate (Ip5I) 可显著抑制这种内向电[1]
α,β-Methylene-ATP trisodium (10 μM;瞬时) 在大鼠肾上腺髓质嗜铬细胞 (Chromaffin cells) 中增强 Acetylcholine (HY-B0282) 诱发的电流幅度,且对 α-conotoxin RgIA (HY-P5845) 敏感的电流比例增加[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

α,β-Methylene-ATP (5-50 μg/kg;左侧腘动脉注射;单剂量) trisodium 在去大脑猫模型中诱发反射性升压反应,该反应可被坐骨神经切断或 P2X 受体拮抗剂 PPADS (HY-108960) (10 mg/kg;左腘动脉注射) 阻断[2]
α,β-Methylene-ATP (10 nmol/rat;脑室内注射;单剂量) trisodium 在 Sprague-Dawley 大鼠中产生抗机械伤害作用,该作用可被 DSP-4 (HY-121602/HY-103210) (10 mg/kg DSP-4;腹腔注射) 预处理显著减弱[3]
α,β-Methylene-ATP (0.1-1 nmol/side;双侧蓝斑核微注射;单剂量) trisodium 在 Sprague-Dawley 大鼠中,以剂量依赖性升高大鼠的疼痛阈值,该效应可被 PPADS (HY-108960) (0.1-1 nmol/side) 共注射拮抗[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Decerebrate cats[2]
Dosage: 5, 20, 50 µg/kg α,β-Methylene-ATP
Administration: Left popliteal artery injection, single dose
Result: Significantly increased mean arterial pressure. The pressor response was attenuated by sciatic nerve section and completely blocked by prior popliteal artery injection of PPADS (10 mg/kg), indicating involvement of P2X receptors in muscle afferents.
Animal Model: Sprague-Dawley rats (male, 180-250 g, 6-8 weeks old)[3]
Dosage: 10 nmol/rat
Administration: Intracerebroventricular injection, single dose
Result: Elevated the mechanical nociceptive threshold by 63.6% at 5 min post-injection. Pretreatment with DSP-4 (50 mg/kg, i.p.), a noradrenergic neurotoxin, reduced the antinociceptive effect to baseline levels, suggesting involvement of locus coeruleus noradrenergic neurons.
Animal Model: Sprague-Dawley rats (male, 180-250 g, 6-8 weeks old)[3]
Dosage: 0.1-1 nmol/side
Administration: Bilateral locus coeruleus microinjection, single dose, no cycle
Result: Dose-dependently increased the nociceptive threshold (peak at 5 min, 117.9% above control at 1 nmol/side).
Co-injection of PPADS (1 nmol/side) completely antagonized the antinociceptive effect, confirming P2X receptor-mediated mechanism.
分子量

571.15

Formula

C11H15N5Na3O12P3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
细胞实验: 

H2O 中的溶解度 : 125 mg/mL (218.86 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7509 mL 8.7543 mL 17.5085 mL
5 mM 0.3502 mL 1.7509 mL 3.5017 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month (stored under nitrogen)。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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浓度
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体积
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

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体积 (start)

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浓度 (final)

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动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

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每只动物的给药体积

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工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.75%

参考文献

α,β-Methylene-ATP trisodium 相关分类

完整储备液配制表

* 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, 6 months; -20°C, 1 month (stored under nitrogen)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.7509 mL 8.7543 mL 17.5085 mL 43.7713 mL
5 mM 0.3502 mL 1.7509 mL 3.5017 mL 8.7543 mL
10 mM 0.1751 mL 0.8754 mL 1.7509 mL 4.3771 mL
15 mM 0.1167 mL 0.5836 mL 1.1672 mL 2.9181 mL
20 mM 0.0875 mL 0.4377 mL 0.8754 mL 2.1886 mL
25 mM 0.0700 mL 0.3502 mL 0.7003 mL 1.7509 mL
30 mM 0.0584 mL 0.2918 mL 0.5836 mL 1.4590 mL
40 mM 0.0438 mL 0.2189 mL 0.4377 mL 1.0943 mL
50 mM 0.0350 mL 0.1751 mL 0.3502 mL 0.8754 mL
60 mM 0.0292 mL 0.1459 mL 0.2918 mL 0.7295 mL
80 mM 0.0219 mL 0.1094 mL 0.2189 mL 0.5471 mL
100 mM 0.0175 mL 0.0875 mL 0.1751 mL 0.4377 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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