| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
P2Y1 Receptor 0.14 μM μM (IC50)
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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].
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| 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].
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| References |
[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.
[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. [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. |
| Molecular Formula |
C20H16N2O5S
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|---|---|
| Molecular Weight |
396.42
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| CAS # |
56583-49-4
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| SMILES |
[O-][N+]1C2C(=CC=CC=2)C(=O)C=1C1C=CC=CN=1.CC1C=CC(S(O)(=O)=O)=CC=1
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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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