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| Targets |
PAR-1
Protease-activated receptor-1 (PAR-1) [1] (DL-Isoser1)-TRAP-6 targets the protease-activated receptor 1 (PAR-1), functioning as a PAR-1 agonist that activates/agonizes platelets. It is used in biochemical research to study cellular signaling pathways, particularly those involving G-protein coupled receptors. |
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| ln Vitro |
In patients undergoing cardiac catheterization without acute coronary syndrome (ACS), (DL-Isoser1)-TRAP-6 (50 μM) stimulated significantly higher platelet surface expression of P-selectin and activated GPIIb/IIIa in women compared to men (P-selectin: 511 MFI [443-597] vs. 471 MFI [393-552], p=0.001; GPIIb/IIIa: 84 MFI [58-119] vs. 70 MFI [47-103], p=0.002). [1]
In patients with ACS, TRAP-stimulated P-selectin and activated GPIIb/IIIa were similar between sexes (P-selectin: 473 MFI [414-544] vs. 470 MFI [393-556], p=0.9; GPIIb/IIIa: 62 MFI [42-85] vs. 69 MFI [43-98], p=0.3). [1] In patients undergoing elective PCI (Group 2A), (DL-Isoser1)-TRAP-6 (25 μM for LTA, 32 μM for MEA) stimulated significantly higher platelet aggregation in women than in men (LTA: 66% [54-76] vs. 51% [41-65], p=0.007; MEA: 78 AU [66-107] vs. 62 AU [52-88], p=0.02). [1] In patients undergoing acute PCI (Group 2B), TRAP-stimulated platelet aggregation was similar between sexes (LTA: 74% [60-86] vs. 76% [59-94], p=0.6; MEA: 65 AU [48-83] vs. 67 AU [47-85], p=0.5). [1] In vitro, (DL-Isoser1)-TRAP-6 is a PAR-1 agonist that activates platelets. However, as a racemic isoserine analog of SFLLRN, it has only 15-20% of the platelet aggregating activity of the parent peptide SFLLRN. This reduced activity is compensated by significantly higher stability in plasma and serum. |
| ln Vivo |
In Group 1A, platelet activation in response to TRAP was significantly higher in women compared to men (P-selectin: 511 MFI [443-597 MFI] vs. 471 MFI [393-552 MFI]; GPIIb/IIIa: 84 MFI [58-119 MFI] vs. 70 MFI [47-103 MFI]; both p ≤ 0.002). In contrast, in Group 1B, TRAP-stimulated P-selectin and activated GPIIb/IIIa were similar in men and women (both p ≥ 0.3). Likewise, TRAP-stimulated platelet aggregation was significantly higher in female patients in Group 2A (LTA: 66% [54-76%] vs. 51% [41-65%]; MEA: 78 AU [66-107 AU] vs. 62 AU [52-88 AU]; both p ≤ 0.02), whereas men and women in Group 2 B had similar platelet aggregation (p = 0.5). The occurrence of ischemic endpoints did not differ significantly between men and women in Group 1A and Group 1B.Conclusions: Platelet PAR-1 signaling is more pronounced in women than in men without ACS. In ACS, however, PAR-1-mediated platelet activation is similar in male and female patients [1].
Specific in vivo activity data for (DL-Isoser1)-TRAP-6 is not detailed in the provided sources. As a PAR-1 agonist, it would be expected to have effects on platelet activation and thrombosis in vivo. Its increased stability in plasma suggests it may have a longer duration of action compared to the parent peptide. |
| Enzyme Assay |
In vitro receptor binding assays for (DL-Isoser1)-TRAP-6 typically involve measuring its affinity for the PAR-1 receptor. Functional assays, such as measuring platelet aggregation or calcium mobilization upon receptor activation, are used to confirm its agonistic activity.
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| Cell Assay |
For flow cytometry: Whole blood anticoagulated with 3.2% citrate was incubated for 5 min at 37°C, then incubated with 50 μM (DL-Isoser1)-TRAP-6 and PAC-1-FITC (monoclonal antibody specific for activated GPIIb/IIIa) for 5 min. Samples were fixed with 1% formaldehyde in HEPES buffer (10 mmol/L HEPES, 0.15 mol/L sodium chloride, pH 7.4). After 30 min fixation, samples were diluted and stained with CD61-PerCP (platelet identifier) and CD62P-PE (P-selectin). Analysis was performed on a FACSCalibur flow cytometer. Nonspecific binding of PAC-1-FITC was determined in the presence of eptifibatide (2 μg/mL), and nonspecific fluorescence in the PE channel was determined using PE-conjugated normal mouse IgG. Platelet surface P-selectin and activated GPIIb/IIIa were quantified by mean fluorescence intensity (MFI). [1]
For light transmission aggregometry (LTA): Citrate-anticoagulated whole blood was rested for 20 min at room temperature, then centrifuged at 150g for 10 min to obtain platelet-rich plasma (PRP). PRP was stimulated with 25 μM (DL-Isoser1)-TRAP-6. Platelet aggregation was recorded photoelectrically for 10 min to obtain maximal aggregation percentage, with platelet-poor plasma set as 100% aggregation. [1] For multiple electrode aggregometry (MEA): Hirudin-anticoagulated whole blood was diluted 1:2 with 0.9% NaCl and stirred for 3 min at 37°C, then 32 μM (DL-Isoser1)-TRAP-6 was added. Aggregation was continuously recorded for 6 min. The increase in impedance was detected and transformed to aggregation units (AU) at 6 min. [1] Cell culture protocols for (DL-Isoser1)-TRAP-6 involve treating cells expressing PAR-1, such as platelets or endothelial cells, with the peptide at varying concentrations. The effects on cell signaling, aggregation, and other functional responses are then assessed. The peptide is dissolved in a suitable solvent, such as DMSO, and added to the culture medium. |
| Animal Protocol |
Background and aims: Protease-activated receptor (PAR)-1-mediated platelet activation may vary according to sex and clinical situation. In order to investigate sex-specific platelet activation through PAR-1, we assessed platelet response to thrombin receptor-activating peptide (TRAP) in 562 patients undergoing cardiac catheterization without (Group 1A) and with (Group 1B) acute coronary syndrome (ACS). Subsequently, we sought to confirm our findings in 287 patients undergoing elective (Group 2A) or acute (Group 2B) percutaneous coronary intervention.Methods: TRAP-stimulated platelet surface expression of P-selectin and activated glycoprotein IIb/IIIa (GPIIb/IIIa) were measured by flow cytometry in Group 1. Light transmission aggregometry (LTA) and multiple electrode aggregometry (MEA) in response to TRAP were assessed in Group 2. [1]
In vivo animal study protocols for (DL-Isoser1)-TRAP-6 would depend on the specific research question. As a PAR-1 agonist, it could be used to study thrombosis, hemostasis, or inflammation in animal models. The peptide would be administered via intravenous injection, and its effects on platelet function and thrombus formation would be assessed. |
| ADME/Pharmacokinetics |
(DL-Isoser1)-TRAP-6 has a molecular weight of 748.88 g/mol, a formula of C34H56N10O9, and a CAS number of 150242-29-8. It is typically stored as a powder at -20°C. It is soluble in DMSO (~100 mg/mL) and is available with a purity of ≥98%.
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| Toxicity/Toxicokinetics |
Specific toxicological data for (DL-Isoser1)-TRAP-6 is not available. As a research peptide, standard laboratory safety precautions should be followed. No specific toxicity studies are mentioned in the provided sources. It is not intended for human therapeutic use.
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| References | |
| Additional Infomation |
(DL-Isoser1)-TRAP-6 (iso-TRAP) is a PAR-1 agonist used to study platelet activation. It is resistant to aminopeptidase M degradation due to isoserine substitution, making it more reproducible in whole blood assays compared to TRAP-6. The concentration of 50 μM iso-TRAP is approximately equivalent to 20 μM TRAP-6, as iso-TRAP is slightly less potent. [1]
(DL-Isoser1)-TRAP-6 has a CAS number of 150242-29-8. Its sequence is H-DL-Isoser-Phe-Leu-Leu-Arg-Asn-OH. It is a PAR-1 agonist and a synthetic peptide known for its role in biochemical research, particularly in the study of cellular signaling pathways. It is not approved for therapeutic use. |
| Molecular Formula |
C34H56N10O9
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| Molecular Weight |
748.87000
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| Exact Mass |
748.423
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| CAS # |
150242-29-8
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| PubChem CID |
102602236
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| Sequence |
{DL-Isoser}-Phe-Leu-Leu-Arg-Asn;
2-hydroxy-beta-alanyl-L-phenylalanyl-L-leucyl-L-leucyl-L-arginyl-L-asparagine;
H-bAla(2-OH)-Phe-Leu-Leu-Arg-Asn-OH
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| SequenceShortening |
{DL-Isoser}-FLLRN;
XFLLRN
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| Appearance |
White to off-white solid powder
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| LogP |
1.834
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| Hydrogen Bond Donor Count |
11
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
24
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| Heavy Atom Count |
53
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| Complexity |
1270
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CC(C)C[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(=O)N)C(=O)O)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)C(CN)O
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| InChi Key |
YYJYQAMJNGSSQH-BKJSQPKXSA-N
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| InChi Code |
InChI=1S/C34H56N10O9/c1-18(2)13-22(29(48)40-21(11-8-12-39-34(37)38)28(47)44-25(33(52)53)16-27(36)46)41-30(49)23(14-19(3)4)42-31(50)24(43-32(51)26(45)17-35)15-20-9-6-5-7-10-20/h5-7,9-10,18-19,21-26,45H,8,11-17,35H2,1-4H3,(H2,36,46)(H,40,48)(H,41,49)(H,42,50)(H,43,51)(H,44,47)(H,52,53)(H4,37,38,39)/t21-,22-,23-,24-,25-,26?/m0/s1
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| Chemical Name |
(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(3-amino-2-hydroxypropanoyl)amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-oxobutanoic acid
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| Synonyms |
150242-29-8; H-DL-Isoser-Phe-Leu-Leu-Arg-Asn-OH; iso-TRAP-6; (2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(3-amino-2-hydroxypropanoyl)amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-oxobutanoic acid; (DL-Isoser1)-TRAP-6; DL-Isoser-Phe-Leu-Leu-Arg-Asn; (DL-Isoser1)-TRAP-6 trifluoroacetate salt;
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| HS Tariff Code |
2934.99.9001
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| 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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~133.53 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3353 mL | 6.6767 mL | 13.3535 mL | |
| 5 mM | 0.2671 mL | 1.3353 mL | 2.6707 mL | |
| 10 mM | 0.1335 mL | 0.6677 mL | 1.3353 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.
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