| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| Targets |
PAR4
|
|---|---|
| ln Vitro |
With an IC50 value of 95 μM, tcY-NH2 TFA (0-500 μM) inhibits the aggregation of platelets (obtained from male albino Sprague-Dawley rats) induced by AYPGKF-NH2 (10 μM). With IC50 values of 64 μM for aorta relaxation (RA) and 1 μM for gastric contraction (LM), tcY-NH2 TFA potently activates these processes[1]. tcY-NH2 TFA (Tc-YPGKF-NH2, 400 μM, 5 min) inhibits platelet aggregation and endostatin release that are brought on by thrombin or AY-NH2[2]. In an isolated heart model, tcY-NH2 TFA (5 μM, 15 min) increases recovery of ventricular function by 26% and decreases infarct size (IS) by 51%[5].
|
| ln Vivo |
In the Brain Death (BD) rat model, tcY-NH2 TFA (tail vein injection, 0.6 mg/kg for a single dosage) reduces liver injury as seen by improved histomorphology and decreased blood ALT/AST levels[3]. In the draining lymph nodes of burn damage mice model, tcY-NH2 TFA (intraperitoneal injection, 0.6 mg/kg for a single dosage) promotes posttraumatic activation of CD4+ Tregs[4]. In experimental inflammation in mice, tcY-NH2 TFA (intrapleural injection, 40 ng/kg for a single dose) suppresses neutrophil recruitment[6].
|
| Animal Protocol |
Animal/Disease Models: Brain death (BD) rat model[3]
Doses: 0.6 mg/kg for a single dose Route of Administration: Tail vein injection for a single dose Experimental Results: decreased blood platelet activation and hepatic platelet accumulation. Attenuated the inflammatory response and apoptosis in the livers. Inhibited the activation of NF-κB and MAPK pathways induced by Brain death (BD). Animal/Disease Models: Burn injury model of C57BL/6 N mice[4] Doses: 0.6 mg/kg for a single dose Route of Administration: intraperitoneal (ip) injection Experimental Results: Increased expression and phosphorylation of PKC-θ in the presence of platelets, without affecting early posttraumatic hemostasis. Animal/Disease Models: BALB/c mice[6] Doses: 40 ng/kg for a single dose Route of Administration: Intrapleural injection Experimental Results: Abolished the number of rolling and adhering neutrophils on the vessel wall. Inhibited CXCL8- and Cg-induced neutrophil migration into the pleural cavity of mice. |
| References |
[1]. Morley D Hollenberg, et al. Proteinase-activated receptor-4: evaluation of tethered ligand-derived peptides as probes for receptor function and as inflammatory agonists in vivo. Br J Pharmacol. 2004 Oct;143(4):443-54.
[2]. L Ma, et al. Thrombin-induced platelet endostatin release is blocked by a proteinase activated receptor-4 (PAR4) antagonist. Br J Pharmacol. 2001 Oct;134(4):701-4. [3]. Hongbo Fang, et al. Blocking protease-activated receptor 4 alleviates liver injury induced by brain death. Biochem Biophys Res Commun. 2022 Mar 5;595:47-53. [4]. Matthias Bock, et al. Platelets differentially modulate CD4 + Treg activation via GPIIa/IIIb-, fibrinogen-, and PAR4-dependent pathways. Immunol Res. 2022 Apr;70(2):185-196. [5]. Jennifer L Strande, et al. Inhibiting protease-activated receptor 4 limits myocardial ischemia/reperfusion injury in rat hearts by unmasking adenosine signaling. J Pharmacol Exp Ther. 2008 Mar;324(3):1045-54. [6]. Lindisley F Gomides, et al. Blockade of proteinase-activated receptor 4 inhibits neutrophil recruitment in experimental inflammation in mice. Inflamm Res. 2014 Nov;63(11):935-41. |
| Molecular Formula |
C42H50F3N7O9
|
|---|---|
| Molecular Weight |
853.88
|
| CAS # |
1262750-73-1
|
| Related CAS # |
tcY-NH2;327177-34-4
|
| SMILES |
C1CN(C([C@@H](NC(/C=C/C2C=CC=CC=2)=O)CC2C=CC(O)=CC=2)=O)[C@H](C(NCC(N[C@H](C(N[C@H](C(N)=O)CC2C=CC=CC=2)=O)CCCCN)=O)=O)C1.O=C(C(F)(F)F)O
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (117.11 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.44 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (2.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1711 mL | 5.8556 mL | 11.7112 mL | |
| 5 mM | 0.2342 mL | 1.1711 mL | 2.3422 mL | |
| 10 mM | 0.1171 mL | 0.5856 mL | 1.1711 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
