tcY-NH2
Based on 1 publication(s) in Google Scholar
tcY-NH2 ((trans-Cinnamoyl)-YPGKF-NH2) is a potent selective PAR4 antagonist peptide. tcY-NH2 inhibits thrombin- and AY-NH2-induced platelet aggregation and endostatin release, and can be used in the research of inflammation, immunology.
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- Pureté : 99.93%
- CAS No.: 327177-34-4
- Formule: C40H49N7O7
- Masse moléculaire:739.86
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Stockage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) tcY-NH2
More
Activité biologique
Description
IC50 & Target
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PAR4 |
In Vitro
tcY-NH2 (0-500 μM) inhibits AYPGKF-NH2 (10 μM)-induced platelet (obtained from male albino Sprague–Dawley rats) aggregation, with an IC50 value of 95 μM[1].
tcY-NH2 potently activates aorta relaxation (RA) and gastric (LM) contraction, with IC50 values of 64 μM (RA) and 1 μM (LM)[1].
tcY-NH2 (Tc-YPGKF-NH2, 400 μM, 5 min) prevents endostatin release and platelet aggregation induced by thrombin or by AY-NH2[2].
tcY-NH2 (5 μM, 15 min) decreases infarct size (IS) by 51%, and increases recovery of ventricular function by 26% in an isolated heart model[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
tcY-NH2 (intraperitoneal injection, 0.6 mg/kg for a single dose) increases posttraumatic activation of CD4+ Tregs within the draining lymph nodes in burn injury mice model [4].
tcY-NH2 (intrapleural injection, 40 ng/kg for a single dose) inhibits neutrophil recruitment in experimental inflammation in mice[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Brain death (BD) rat model[3]
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Dosage:0.6 mg/kg for a single dose
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Administration:Tail vein injection for a single dose
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Result:Reduced 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).
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Animal Model:Burn injury model of C57BL/6 N mice[4]
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Dosage:0.6 mg/kg for a single dose
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Administration:Intraperitoneal injection
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Result:Increased expression and phosphorylation of PKC-θ in the presence of platelets, without affecting early posttraumatic hemostasis.
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Animal Model:BALB/c mice[6]
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Dosage:40 ng/kg for a single dose
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Administration:Intrapleural injection
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Result: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.
Chemical Information
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CAS No. 327177-34-4
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Appearance Solid
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Masse moléculaire 739.86
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Formule C40H49N7O7
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Color White to off-white
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Synonyms
(trans-Cinnamoyl)-YPGKF-NH2
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Sequence Shortening
{trans-Cinnamoyl}-YPGKF-NH2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Nutr Food Res
A Collagen-Derived Oligopeptide from Salmo salar Collagen Hydrolysates Restrains Atherogenesis in ApoE-/- Mice via Targeting P2 Y12 Receptor. [Abstract]2022 Jul;66(13):e2200166. PMID: 35490399
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (135.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
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 |
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| DMSO | 1 mM | 1.3516 mL | 6.7580 mL | 13.5161 mL | 33.7902 mL |
| 5 mM | 0.2703 mL | 1.3516 mL | 2.7032 mL | 6.7580 mL | |
| 10 mM | 0.1352 mL | 0.6758 mL | 1.3516 mL | 3.3790 mL | |
| 15 mM | 0.0901 mL | 0.4505 mL | 0.9011 mL | 2.2527 mL | |
| 20 mM | 0.0676 mL | 0.3379 mL | 0.6758 mL | 1.6895 mL | |
| 25 mM | 0.0541 mL | 0.2703 mL | 0.5406 mL | 1.3516 mL | |
| 30 mM | 0.0451 mL | 0.2253 mL | 0.4505 mL | 1.1263 mL | |
| 40 mM | 0.0338 mL | 0.1690 mL | 0.3379 mL | 0.8448 mL | |
| 50 mM | 0.0270 mL | 0.1352 mL | 0.2703 mL | 0.6758 mL | |
| 60 mM | 0.0225 mL | 0.1126 mL | 0.2253 mL | 0.5632 mL | |
| 80 mM | 0.0169 mL | 0.0845 mL | 0.1690 mL | 0.4224 mL | |
| 100 mM | 0.0135 mL | 0.0676 mL | 0.1352 mL | 0.3379 mL |
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