Catalog No. TP1065 Cas No. 1228078-65-6
Alias PAR-4-AP (TFA), AY-NH2 (TFA)
PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA)), is a selective activator of the proteinase-activated receptor-4 (PAR-4) that does not affect PAR-1 or PAR-2, and its activity can be inhibited by a PAR-4 antagonist.
Catalog No. TP1065 Alias PAR-4-AP (TFA), AY-NH2 (TFA) Cas No. 1228078-65-6
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Q What’s IC50?
A Half-maximal inhibitory concentration (IC50) refers to the concentration of the inhibitor which is required to inhibit a given biological or biochemical function by half.
Q What’s pIC50?
A pIC50 is the negative log of the IC50 value when converted to molar.That is, pIC50=-log(IC50).
Q What’s Ki?
A Inhibitory consent (Ki) reflects the strength of inhibitor binding to the target, corresponding to the concentration of free inhibitor when 50% of the target is bound by the inhibitor.
Q What’s Kd?
A Dissociation consent (Kd) reflects the affinity of a compound for its target. In some cases, it can be equivalent to Ki.
Q How to recommend specific or broad-spectrum inhibitors for a target? What is the difference between specificity and nonspecificity?
A Inhibitors can be classified into two types based on specificity: broad-spectrum (pan) and selective inhibitors. Pan inhibitors are inhibitors of a particular target that have inhibitory effects on all subtypes or members of the entire family. Selective inhibitors have particularly high inhibitory rates or specific inhibitory effects on a subtype of a protein kinase or a member of a family of proteins. The evaluation of the inhibitory efficiency of an inhibitor generally relies on the IC50 value, with lower IC50 values indicating higher inhibitory efficiency. We recommend considering the above characteristics comprehensively when selecting inhibitors, and you can also contact our technical team for recommendations on relevant inhibitors.
Purity: 99.72%
Appearance: Solid
Color: White
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Description PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA)), is a selective activator of the proteinase-activated receptor-4 (PAR-4) that does not affect PAR-1 or PAR-2, and its activity can be inhibited by a PAR-4 antagonist. In vivo SCID mice demonstrate a markedly enhanced abdominal response to colorectal distension (CRD), with distension levels ranging from 0.04 to 0.1 mL amplifying the intensity of the EMG response from 384% to 132%, respectively, as compared to BALB/cBy controls (P<0.01; P<0.01; P<0.01; P<0.001). Activation of PAR-4 significantly mitigates this hypersensitivity (P<0.01, P<0.05; P<0.05; P<0.05). Synonyms PAR-4-AP (TFA), AY-NH2 (TFA)
Molecular Weight 794.82
Formula C 36 H 49 F 3 N 8 O 9
Cas No. 1228078-65-6
Smiles OC(=O)C(F)(F)F.C[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
Relative Density no data available
Sequence Ala-Tyr-Pro-Gly-Lys-Phe-NH2
Sequence Short AYPGKF
Storage keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information H2O: 100 mg/mL (125.81 mM), Sonication is recommended. DMSO: 250 mg/mL (314.54 mM), Sonication is recommended. In Vivo Formulation 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (6.29 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
H2O/DMSO
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method: For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH 2 O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation: Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation: 1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear. 2) Add 50 μL Tween 80 and mix well until fully clarified. 3) Add 450 μL Saline, PBS or ddH 2 O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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