PAR2 modulator-1
Based on 1 Customer Validation
PAR2 modulator-1 is a biased protease-activated receptor 2 (PAR2) inhibitor. PAR2 modulator-1 blocks the PAR2-dependent MAPK signaling pathway with an IC50 value of 8.5 μM, without altering the PAR2-dependent Ca2+ signaling pathway. PAR2 modulator-1 blocks pain responses induced by PAR2 agonists. PAR2 modulator-1 can be used in the research of chronic pain.
For research use only. We do not sell to patients.
- CAS No.: 2378159-28-3
- Formula: C27H41N5O5
- Molecular Weight:515.64
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PAR2 8.5 μM (IC50) |
In Vitro
PAR2 modulator-1 (C781) (30-300 nM) inhibits 2AT-induced PAR2 responses in a dose-dependent manner, with almost complete inhibition observed at 300 nM[1].
PAR2 modulator-1 (100 nM-100 μM) significantly reduces MAPK phosphorylation in cells expressing PAR2, with an IC50 of 8.5 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PAR2 modulator-1 (30 mg/kg; i.p.; single dose) effectively blocks 2AT-induced systemic mechanical hyperalgesia.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[1]
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Dosage:1 μg
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Administration:intraplantar injection; single dose
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Result:Effectively blocked 2AT-induced persistent mechanical hypersensitivity and did not itself cause pain.
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Animal Model:Mice[1]
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Dosage:30 mg/kg
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Administration:i.p.; single dose
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Result:Effectively blocked 2AT-induced systemic mechanical hypersensitivity.
Chemical Information
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CAS No. 2378159-28-3
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Molecular Weight 515.64
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Formula C27H41N5O5
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SMILES
O=C(C1=CC=CO1)N2C3N(C([C@H](C2)NC(CC(C)C)=O)=O)[C@H](C(N(C3)CC4CCNCC4)=O)CC(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (193.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9393 mL | 9.6967 mL | 19.3934 mL | 48.4834 mL |
| 5 mM | 0.3879 mL | 1.9393 mL | 3.8787 mL | 9.6967 mL | |
| 10 mM | 0.1939 mL | 0.9697 mL | 1.9393 mL | 4.8483 mL | |
| 15 mM | 0.1293 mL | 0.6464 mL | 1.2929 mL | 3.2322 mL | |
| 20 mM | 0.0970 mL | 0.4848 mL | 0.9697 mL | 2.4242 mL | |
| 25 mM | 0.0776 mL | 0.3879 mL | 0.7757 mL | 1.9393 mL | |
| 30 mM | 0.0646 mL | 0.3232 mL | 0.6464 mL | 1.6161 mL | |
| 40 mM | 0.0485 mL | 0.2424 mL | 0.4848 mL | 1.2121 mL | |
| 50 mM | 0.0388 mL | 0.1939 mL | 0.3879 mL | 0.9697 mL | |
| 60 mM | 0.0323 mL | 0.1616 mL | 0.3232 mL | 0.8081 mL | |
| 80 mM | 0.0242 mL | 0.1212 mL | 0.2424 mL | 0.6060 mL | |
| 100 mM | 0.0194 mL | 0.0970 mL | 0.1939 mL | 0.4848 mL |
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