PIT 2,2'-Pyridylisatogen tosylate|cas:56583-49-4|西域试剂

PIT 2,2'-Pyridylisatogen tosylate,98.57%

产品编号：Bellancom-108662| CAS NO：56583-49-4| 分子式：C₂₀H₁₆N₂O₅S| 分子量：396.42

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-108662	￥700.00	杭州北京（现货）
Bellancom-108662	￥1200.00	杭州北京（现货）
Bellancom-108662	￥2500.00	杭州北京（现货）
Bellancom-108662	￥4000.00	杭州北京（现货）
Bellancom-108662	￥6000.00	杭州北京（现货）

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PIT 2,2'-Pyridylisatogen tosylate

产品介绍

PIT (2,2'-Pyridylisatogen tosylate) 是 P2Y1 受体 的选择性和非竞争性拮抗剂，对人 P2Y1 受体的 IC₅₀ 值为 0.14 μM。PIT 在不影响核苷酸结合的情况下拮抗 P2Y1 受体信号。PIT 是一些平滑肌中代谢性嘌呤受体 (P2Y 家族) 对 ATP 反应的不可逆拮抗剂。PIT 可用于慢性支气管炎和哮喘的研究。

生物活性

PIT (2,2'-Pyridylisatogen tosylate) is a selective and non-competitive antagonist of P2Y1 receptor with an IC₅₀ value of 0.14 μM for human P2Y1 receptor. PIT antagonizes P2Y1 receptor signaling without affecting nucleotide binding. PIT is an irreversible antagonist of responses to ATP at metabotropic purinoceptors (of the P2Y family) in some smooth muscles. PIT can be used for the research of chronic bronchitis and asthma.

体外研究

PIT (0.1-10 μM) non-competitively and dose-dependently diminishs human P2Y1 receptor signaling with an IC₅₀ value of 0.14 μM.
PIT (0.1-10 μM) completely blocks the agonist activity of 2-MeSADP.
PIT (1 nM-10 μM) dose-dependently inhibits the accumulation of inositol phosphates induced by the agonist 2-MeSADP.
PIT (1 nM-10 μM) dose-dependently blocks the P2Y1 receptor signaling induced by the endogenous agonist ADP.
PIT (0.1-3 μM) increases ATP-responses 2-5 fold, while higher concentrations (3-100 μM) inhibits ATP-mediated inward current with an IC₅₀ value of 13.2 μM.
PIT shows a low affinity for a range of membrane receptors, including: α₁, α₂-adrenoceptors, 5-HT_1A, 5-HT_1B, 5-HT₂, 5-HT₃, D₁, D₂, muscarinic, central benzodiazepine, H₁, μ-opioid, dihydropyridine and batrachotoxin receptors with pK_i values of <5.
PIT shows affinity to an adenosine (A₁) receptor with a pK_i value of 5.3.
PIT (12.5-50 μM) irreversibly antagonizes relaxations of ATP in guinea-pig isolated taenia caeca.

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

体内研究

PIT (10 mg/kg; i.p.; for 5 days) significantly protects both the white matter and the cortical plate lesions against the insult in mice with S-bromo-willardiine injection induced tonic and tonicoclonic seizures.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 83.33 mg/mL (210.21 mM; ultrasonic and warming and heat to 70°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5226 mL	12.6129 mL	25.2258 mL
5 mM	0.5045 mL	2.5226 mL	5.0452 mL
10 mM	0.2523 mL	1.2613 mL	2.5226 mL

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 (sealed storage, away from moisture)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.25 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明