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PIT
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PIT图片
CAS NO:56583-49-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
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 ofP2Y1 receptorwith anIC50value of 0.14 μM for humanP2Y1 receptor. PIT antagonizesP2Y1 receptorsignaling 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[1][2][3].

IC50& Target

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 IC50value of 0.14 μM[1].
PIT (0.1-10 μM) completely blocks the agonist activity of 2-MeSADP[1].
PIT (1 nM-10 μM) dose-dependently inhibits the accumulation of inositol phosphates induced by the agonist 2-MeSADP[1].
PIT (1 nM-10 μM) dose-dependently blocks the P2Y1 receptor signaling induced by the endogenous agonist ADP[1].
PIT (0.1-3 μM) increases ATP-responses 2-5 fold, while higher concentrations (3-100 μM) inhibits ATP-mediated inward current with an IC50value of 13.2 μM[2].
PIT shows a low affinity for a range of membrane receptors, including: α1, α2-adrenoceptors, 5-HT1A, 5-HT1B, 5-HT2, 5-HT3, D1, D2, muscarinic, central benzodiazepine, H1, μ-opioid, dihydropyridine and batrachotoxin receptors with pKivalues of<5[2].
PIT shows affinity to an adenosine (A1) receptor with a pKivalue of 5.3[2].
PIT (12.5-50 μM) irreversibly antagonizes relaxations of ATP in guinea-pig isolated taenia caeca[2].

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[3].

Clinical Trial
分子量

396.42

Formula

C20H16N2O5S

CAS 号

56583-49-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
In Vitro: 

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

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5226 mL12.6129 mL25.2258 mL
5 mM0.5045 mL2.5226 mL5.0452 mL
10 mM0.2523 mL1.2613 mL2.5226 mL
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-CDin 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 μL20% 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
*以上所有助溶剂都可在本网站选购。