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.
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
Bradykinin (1-5) (500 nM) significantly attenuates
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].
Bradykinin (1-5) (265.5-17700.0 pmol/L; 4-24 h) allows quantification of BK1-5 in human whole blood, with an LLOQ of 265.5 pmol/L and an LOD of 35.4 pmol/L[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
BK-(1-5) is the major and most stable kinin metabolite in carrageenan-induced pleurisy in rats, reaching a peak of 8800 pg/rat at 3 h and closely correlating with plasma exudation[3].
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)
Bradykinin (1-5) TFA Related Classifications
HY-P1488A Related Classifications
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