PeptideDB

PAR 4 (1-6) (human) 225779-44-2

PAR 4 (1-6) (human) 225779-44-2

CAS No.: 225779-44-2

PAR 4 (1-6) TFA (GYPGQV TFA) is a hexapeptide that is a fragment of the protease-activated receptor 4 (PAR4) and acts as
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PAR 4 (1-6) TFA (GYPGQV TFA) is a hexapeptide that is a fragment of the protease-activated receptor 4 (PAR4) and acts as a PAR4-specific agonist.

Physicochemical Properties


Molecular Formula C28H41N7O9
Molecular Weight 619.67
Exact Mass 619.297
CAS # 225779-44-2
PubChem CID 10240159
Appearance Typically exists as solid at room temperature
LogP 0.363
Hydrogen Bond Donor Count 8
Hydrogen Bond Acceptor Count 10
Rotatable Bond Count 16
Heavy Atom Count 44
Complexity 1060
Defined Atom Stereocenter Count 4
SMILES

CC([C@H](NC([C@@H](NC(CNC([C@@H]1CCCN1C([C@@H](NC(CN)=O)CC2=CC=C(O)C=C2)=O)=O)=O)CCC(N)=O)=O)C(O)=O)C

InChi Key VTCFYKYDKDAJKZ-XHOYROJHSA-N
InChi Code

InChI=1S/C28H41N7O9/c1-15(2)24(28(43)44)34-25(40)18(9-10-21(30)37)32-23(39)14-31-26(41)20-4-3-11-35(20)27(42)19(33-22(38)13-29)12-16-5-7-17(36)8-6-16/h5-8,15,18-20,24,36H,3-4,9-14,29H2,1-2H3,(H2,30,37)(H,31,41)(H,32,39)(H,33,38)(H,34,40)(H,43,44)/t18-,19-,20-,24-/m0/s1
Chemical Name

(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-1-[(2S)-2-[(2-aminoacetyl)amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-5-oxopentanoyl]amino]-3-methylbutanoic acid
Synonyms

QUR
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


ln Vitro PAR 4 (1-6) (GYPGQV) promotes [3H]-thymidine incorporation in smooth muscle cells (SMCs). At 500 μM, the peptide increased DNA synthesis 2.5-fold compared to the control. This was comparable to the proliferative effects obtained when SMCs were stimulated with 10 nM thrombin or 100 μM SFLLRN, respectively.
References

[1]. Protease-activated receptor 1 is the primary mediator of thrombin-stimulated platelet procoagulant activity. Proc Natl Acad Sci U S A. 1999 Sep 28;96(20):11189-93.

[2]. Evidence for functionally active protease-activated receptor-4 (PAR-4) in human vascular smooth muscle cells. Br J Pharmacol. 2001 Apr;132(7):1441-6.


Solubility Data


Solubility (In Vitro) May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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).
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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.6138 mL 8.0688 mL 16.1376 mL
5 mM 0.3228 mL 1.6138 mL 3.2275 mL
10 mM 0.1614 mL 0.8069 mL 1.6138 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.