PAR2 modulator-1 |
Catalog No.GC79232
One-Click Copy Product Info
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PAR2 modulator-1 is a biased protease-activated receptor 2 ( PAR2 ) inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2378159-28-3
Sample solution is provided at 25 µL, 10mM.
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In Vivo, PAR2 modulator-1 (C781) (1 μg; intraplantar injection; single dose) effectively blocks 2AT-induced persistent mechanical hyperalgesia without inducing pain on its own[1]. PAR2 modulator-1 (30 mg/kg; i.p.; single dose) effectively blocks 2AT-induced systemic mechanical hyperalgesia.
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].
References:
[1]. Scott A. BOITANO, et al. Small molecule modulators of par2 and uses thereof. WO2019199800A1. 2020-10-09
| Cas No. | 2378159-28-3 | SDF | |
| Formula | C27H41N5O5 | M.Wt | 515.64 |
| Solubility | DMSO: 100 mg/mL (193.93 mM; Need ultrasonic) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9393 mL | 9.6967 mL | 19.3934 mL |
| 5 mM | 387.9 μL | 1.9393 mL | 3.8787 mL |
| 10 mM | 193.9 μL | 969.7 μL | 1.9393 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)