PIT|56583-49-4|(2,2'-Pyridylisatogen tosylate)-陌孚医药/Medlife

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PIT (Synonyms: 2,2'-Pyridylisatogen tosylate)

目录号: PC11170 纯度: ≥98%

CAS No. :56583-49-4

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中文名称	PIT
中文别名	2-(2-吡啶)-(3h)-吲哚-3-酮-1-氧化物 4-甲基苯磺酸盐
英文名称	PIT
英文别名	2-(2-PYRIDINYL)-(3H)-INDOL-3-ONE-1-OXIDE 4-METHYLBENZENESULFONATE;4-methylbenzenesulfonic acid;PIT;PIT,2-(2-Pyridinyl)-(3H)-indol-3-one-1-oxide4-methylbenzenesulfonate;1-oxido-2-pyridin-2-yl-indol-3-one;2,2'-pyridylisatogen tosylate
Cas No.	56583-49-4
分子式	C₁₃H₈N₂O₂^.C₇H₈O₃S
分子量	396.42
包装储存	-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.

性状

Solid

IC50 & Target[1][2]

P2Y1 Receptor

0.14 μM μM (IC₅₀)

体外研究(In Vitro)

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.

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

体内研究(In Vivo)

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.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Gao ZG, et al. 2,2-Pyridylisatogen tosylate antagonizes P2Y1 receptor signaling without affecting nucleotide binding. Biochem Pharmacol. 2004 Jul 15;68(2):231-7. [Information]

[2]. King BF, et al. Potentiation by 2,2-pyridylisatogen tosylate of ATP-responses at a recombinant P2Y1 purinoceptor. Br J Pharmacol. 1996 Mar;117(6):1111-8. [Information]

[3]. Menton K, et al. Role of spin trapping and P2Y receptor antagonism in the neuroprotective effects of 2,2-pyridylisatogen tosylate and related compounds. Eur J Pharmacol. 2002 May 24;444(1-2):53-60. [Information]

溶解度数据

体外研究:

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

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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