2. GPCR/G Protein
  3. P2Y Receptor
  4. PIT

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

Cat. No.: HY-108662 Purity: 98.57%
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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.

For research use only. We do not sell to patients.

PIT Chemical Structure

PIT Chemical Structure

CAS No. : 56583-49-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 77 In-stock
Solution
10 mM * 1 mL in DMSO USD 77 In-stock
Solid
5 mg USD 70 In-stock
10 mg USD 120 In-stock
25 mg USD 250 In-stock
50 mg USD 400 In-stock
100 mg USD 600 In-stock
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Based on 1 publication(s) in Google Scholar

PIT Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

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[1][2][3].

IC50 & Target

P2Y1 Receptor

0.14 μM μM (IC50)

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[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 IC50 value 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 pKi values of <5[2].
PIT shows affinity to an adenosine (A1) receptor with a pKi value of 5.3[2].
PIT (12.5-50 μM) irreversibly antagonizes relaxations of ATP in guinea-pig isolated taenia caeca[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PIT Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

396.42

Formula

C20H16N2O5S
CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

O=C1C(C2=NC=CC=C2)=[N+]([O-])C3=C1C=CC=C3.O=S(C4=CC=C(C)C=C4)(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (210.21 mM; ultrasonic and warming and heat to 70°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5226 mL 12.6129 mL 25.2258 mL 63.0644 mL
5 mM 0.5045 mL 2.5226 mL 5.0452 mL 12.6129 mL
10 mM 0.2523 mL 1.2613 mL 2.5226 mL 6.3064 mL
15 mM 0.1682 mL 0.8409 mL 1.6817 mL 4.2043 mL
20 mM 0.1261 mL 0.6306 mL 1.2613 mL 3.1532 mL
25 mM 0.1009 mL 0.5045 mL 1.0090 mL 2.5226 mL
30 mM 0.0841 mL 0.4204 mL 0.8409 mL 2.1021 mL
40 mM 0.0631 mL 0.3153 mL 0.6306 mL 1.5766 mL
50 mM 0.0505 mL 0.2523 mL 0.5045 mL 1.2613 mL
60 mM 0.0420 mL 0.2102 mL 0.4204 mL 1.0511 mL
80 mM 0.0315 mL 0.1577 mL 0.3153 mL 0.7883 mL
100 mM 0.0252 mL 0.1261 mL 0.2523 mL 0.6306 mL
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PIT Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PIT56583-49-42,2'-PyridylisatogenP2Y Receptor2-MeSADPATPchronic bronchitisasthmainositol phosphateADPmembrane receptorneuroprotectionInhibitorinhibitorinhibit

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