Bradykinin (1-5) TFA
Bradykinin (1-5) TFA is a metabolite of Bradykinin (HY-P0206) and a PAR inhibitor that inhibits thrombin-induced platelet aggregation by preventing protease-activated receptor (Protease Activated Receptor) cleavage and inhibiting Thrombin (MW 37kDa) (HY-114164). Bradykinin (1-5) TFA is used in research on thrombosis, carrageenan-induced pleurisy, nasal allergy, and hereditary angioedema.
For research use only. We do not sell to patients.
- Formula: C27H40N8O6.xHC2O2F3
- Molecular Weight:572.66 (free base)
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
Human α-Thrombin (HY-114164A)-induced platelet aggregation in human PRP, but the in vitro concentration required to inhibit Human γ-Thrombin (HY-114164B)-induced platelet aggregation reaches 7 mM, indicating a markedly lower ex vivo potency[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Healthy nonsmoking subjects (22 men and 14 women; 29 white, 7 black; mean age 29.8 years; mean BMI 26.0 kg/m2)[1]
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Dosage:47, 94, 188, and 377 pmol/min (first ten subjects); 377, 754, 3770, and 18,850 pmol/min (next 15 subjects); 37, 188, 377, and 754 pmol/min (dose-platelet inhibition-response experiments)
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Administration:intra-arterial; each dose infused for 5 min
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Result:Did not affect forearm blood flow at doses up to 18,850 pmol/min.
Had no effect on net t-PA release at doses up to 18,850 pmol/min.
Had no effect on net PAI-1 extraction at doses up to 18,850 pmol/min.
Increased venous concentration dose-dependently from 48.9 to 2099.5 fmol/mL (equimolar doses 47-377 pmol/min) and from 44.7 to 79,359 fmol/mL (up to 18,850 pmol/min).
Significantly attenuated α-thrombin-induced platelet aggregation (16% aggregation during infusion vs 88% at baseline).
Had no effect on TRAP 1-6-induced platelet aggregation (56.13% during infusion vs 52.2% at baseline).
Inhibited γ-thrombin (500 nM)-induced platelet aggregation with an ED50 of 183 pmol/min.
Chemical Information
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Molecular Weight 572.66 (free base)
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Formula C27H40N8O6.xHC2O2F3
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SMILES
N=C(NCCC[C@@H](C(N1[C@@H](CCC1)C(N2[C@@H](CCC2)C(NCC(N[C@H](C(O)=O)CC3=CC=CC=C3)=O)=O)=O)=O)N)N.OC(C(F)(F)F)=O.[x]
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Sequence
Arg-Pro-Pro-Gly-Phe
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Sequence Shortening
RPPGF
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)