| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
P2Y1 Receptor 0.14 μM μM (IC50)
P2Y1 receptor. PIT is a selective and noncompetitive antagonist of the P2Y1 receptor. It acts as a negative allosteric modulator (NAM), binding to an allosteric site on the receptor and inhibiting agonist-induced signaling. It displays irreversible antagonism at P2Y receptors in some smooth muscles and has an IC50 of 0.14 μM for the human P2Y1 receptor. |
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| ln Vitro |
PIT (0.1–10 μM) has an IC50 value of 0.14 μM and reduces human P2Y1 receptor signaling in a non-competitive and dose-dependent manner[1]. PIT (0.1–10 μM) totally inhibits 2-MeSADP's agonistic activity[1]. PIT (1 nM-10 μM) reduces the buildup of inositol phosphates caused by the agonist 2-MeSADP in a dose-dependent manner[1]. PIT (1 nM–10 μM) inhibits P2Y1 receptor signaling that is triggered by the endogenous agonist ADP in a dose-dependent manner [1]. Higher concentrations (3-100 μM) inhibit ATP-mediated inward current with an IC50 value of 13.2 μM, whereas PIT (0.1-3 μM) increases ATP-responses 2-5 fold[2]. PIT exhibits low affinity for several membrane receptors, such as muscarinic, central benzodiazepine, H1, μ-opioid, dihydropyridine, batrachotoxin, α1, α2-adrenoceptors, 5-HT1A, 5-HT1B, 5-HT2, 5-HT3, D1, D2, and D1[2]. PIT has a pKi value of 5.3 and exhibits affinity to an adenosine (A1) receptor[2]. Irreversibly, PIT (12.5-50 μM) opposes ATP relaxations in guinea pig isolated taenia caeca [2].
PIT selectively inhibits agonist-induced signaling for P2Y1 over P2Y2, P2Y4, and P2Y11 receptors in 1321N1 cells and the P2Y12 receptor in CHO cells at 10 µM. It inhibits ATP-induced relaxation of guinea pig taenia caeci preparations. PIT is also a spin trap that forms stable adducts with hydroxyl and superoxide radicals. |
| ln Vivo |
In rats with S-bromo-willardiine injection-induced tonic and tonicoclonic seizures, PIT (10 mg/kg; ip; for 5 days) dramatically protects the white matter and the cortical plate lesions against the insult[3].
In vivo, PIT has been shown to reduce periventricular white matter and cortical plate lesions induced by S-bromo-willardiine in mice. This demonstrates its ability to modulate P2Y1 receptor-mediated effects in the central nervous system. Its in vivo effects are mediated through its antagonism of the P2Y1 receptor and subsequent inhibition of downstream signaling pathways. |
| Enzyme Assay |
In vitro binding and functional assays are used to characterize PIT as a P2Y1 receptor antagonist. Radioligand binding assays can measure its ability to displace labeled P2Y1 ligands, while functional assays measuring downstream signaling, such as calcium mobilization, are used to determine its IC50 of 0.14 μM. Its selectivity is confirmed by testing against other P2Y receptor subtypes.
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| Cell Assay |
Cellular assays for PIT involve treating P2Y1-expressing cells with the compound and measuring inhibition of agonist-induced responses. Functional readouts include inhibition of intracellular calcium mobilization or other downstream signaling pathways. These assays confirm the compound's antagonistic activity and its selectivity for P2Y1 over other P2Y receptors.
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| Animal Protocol |
In vivo studies with PIT are performed in animal models to investigate P2Y1 receptor function. For example, PIT has been shown to reduce periventricular white matter and cortical plate lesions induced by S-bromo-willardiine in mice. The compound can be administered via injection, and its effects on disease progression and physiological responses are assessed.
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| ADME/Pharmacokinetics |
PIT (2,2'-Pyridylisatogen tosylate) has a molecular formula of C13H8N2O2 • C7H8O3S and is a solid compound with ≥98% purity. It is sparingly soluble in DMSO (1-10 mg/ml). As a small-molecule allosteric modulator, its pharmacokinetic properties would be characteristic of this class, with potential for oral bioavailability. The compound should be stored at -20°C.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for PIT. As a P2Y1 receptor antagonist, its safety profile would be an important consideration for potential therapeutic applications. Potential toxicities could be related to its effects on platelet aggregation and other P2Y1-mediated functions. Standard preclinical safety studies would be required to evaluate its safety.
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| References |
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| Additional Infomation |
It has an inhibitory effect on the action of ATP on smooth muscle; a P2Y1 purine receptor antagonist; structure
PIT (2,2'-Pyridylisatogen tosylate, CAS#: 56583-49-4) is a selective and noncompetitive antagonist of the P2Y1 receptor with an IC50 of 0.14 μM. It acts as a negative allosteric modulator and displays irreversible antagonism at P2Y receptors in some smooth muscles. It is also a spin trap that forms stable adducts with radicals. PIT is a research tool for studying P2Y1 receptor function. |
| Molecular Formula |
C20H16N2O5S
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|---|---|
| Molecular Weight |
396.42
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| Exact Mass |
396.078
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| CAS # |
56583-49-4
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| PubChem CID |
124333
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| Appearance |
Brown to reddish brown solid powder
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| LogP |
4.19
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
28
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| Complexity |
571
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=C(C=C1)S(=O)(=O)O.C1=CC=C2C(=C1)C(=O)C(=[N+]2[O-])C3=CC=CC=N3
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| InChi Key |
MMPTYEXNPWSTOR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H8N2O2.C7H8O3S/c16-13-9-5-1-2-7-11(9)15(17)12(13)10-6-3-4-8-14-10;1-6-2-4-7(5-3-6)11(8,9)10/h1-8H;2-5H,1H3,(H,8,9,10)
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| Chemical Name |
4-methylbenzenesulfonic acid;1-oxido-2-pyridin-2-ylindol-1-ium-3-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 83.33 mg/mL (210.21 mM )
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.25 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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