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PAR3 (1-6) (human)

* Please kindly note that our products are not to be used for therapeutic purposes and cannot be sold to patients.

PAR3 (1-6) is a synthetic hexapeptide agonist of proteinase-activated receptor 1 (PAR1). PAR1 is a high-affinity thrombin receptor expressed in epithelium, neurons, astrocytes, immune cells, and cancer-associated fibroblasts.

Category

Peptide Inhibitors

Catalog number

BAT-015084

CAS number

320347-28-2

Molecular Formula

C29H45N9O8

Molecular Weight

647.72

Specification
Reference Reading

IUPAC Name

(2S)-1-[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]propanoyl]pyrrolidine-2-carboxylic acid

Synonyms

Thrombin Receptor-Like 2 (1-6) (human); L-threonyl-L-phenylalanyl-L-arginyl-glycyl-L-alanyl-L-proline; H-TFRGAP-OH; L-Proline, L-threonyl-L-phenylalanyl-N5-(diaminomethylene)-L-ornithylglycyl-L-alanyl-; L-Threonyl-L-phenylalanyl-N5-(diaminomethylene)-L-ornithylglycyl-L-alanyl-L-proline

Appearance

Crystalline Solid

Purity

≥98%

Density

1.46±0.1 g/cm3

Sequence

H-Thr-Phe-Arg-Gly-Ala-Pro-OH

Storage

Store at -20°C

Solubility

Soluble in DMF, DMSO, Ethanol, PBS (pH 7.2)

InChI

InChI=1S/C29H45N9O8/c1-16(27(44)38-13-7-11-21(38)28(45)46)35-22(40)15-34-24(41)19(10-6-12-33-29(31)32)36-25(42)20(14-18-8-4-3-5-9-18)37-26(43)23(30)17(2)39/h3-5,8-9,16-17,19-21,23,39H,6-7,10-15,30H2,1-2H3,(H,34,41)(H,35,40)(H,36,42)(H,37,43)(H,45,46)(H4,31,32,33)/t16-,17+,19-,20-,21-,23-/m0/s1

InChI Key

LGNVPMUJJJLQHG-WZZXNIEWSA-N

Canonical SMILES

CC(C(C(=O)NC(CC1=CC=CC=C1)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)NC(C)C(=O)N2CCCC2C(=O)O)N)O

1. PAR-3 is a low-affinity substrate, high affinity effector of thrombin

Whyte G Owen Biochem Biophys Res Commun . 2003 May 23;305(1):166-8. doi: 10.1016/s0006-291x(03)00732-0.

A polypeptide corresponding to the extracellular domain of protease-activated receptor 3 (PAR-3) is hydrolyzed by thrombin slowly because of high K(M) (>100 microM). However, thrombin is found to bind two PAR-3, one without catalyzing hydrolysis or blocking the active site, while the other is hydrolyzed. In a solvent lacking Na(+), hydrolysis of a nitroanilide substrate is enhanced 1.6-fold by addition of PAR-3 polypeptide, with half-saturation at 2.5 microM. In contrast, the fibrinogen clotting activity of thrombin is inhibited completely by PAR-3, with a K(I) of 3 microM. None of the activities of thrombin are affected by addition of 50 microM PAR-4 polypeptide. Thus, PAR-3 in low concentrations binds thrombin in a configuration that blocks the anion-binding exosite but not the catalytic site, while hydrolysis of PAR-3, PAR-4, and other substrates that do not interact with exosite I persists. The allosteric effect of PAR-3 is characteristic of that of Na(+).