A bradykinin B1 receptor antagonist
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Lys-(Des-Arg9, Leu8)-Bradykinin (trifluoroacetate salt)

Item No. 35462

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
9-L-leucine-1-9-kallidin, trifluoroacetate salt
Synonyms
  • [Des-Arg10,Leu9]-Kallidin
  • [Des-Arg10,Leu9]-KD
  • Lys[Leu8]Des-Arg9-BK
  • Lys[Leu8]Des-Arg9-Bradykinin
Molecular Formula
C47H75N13O11 • XCF3COOH
Formula Weight
998.2
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 3 mg/mlPBS (pH 7.2): 10 mg/ml
SMILES
N[C@@H](CCCCN)C(N[C@@H](CCCNC(N)=N)C(N1[C@H](C(N2[C@H](C(NCC(N[C@H](C(N[C@@H](CO)C(N3[C@H](C(N[C@@H](CC(C)C)C(O)=O)=O)CCC3)=O)=O)CC4=CC=CC=C4)=O)=O)CCC2)=O)CCC1)=O)=O.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C47H75N13O11.C2HF3O2/c1-28(2)24-33(46(70)71)56-42(66)36-17-10-21-58(36)44(68)34(27-61)57-40(64)32(25-29-12-4-3-5-13-29)54-38(62)26-53-41(65)35-16-9-22-59(35)45(69)37-18-11-23-60(37)43(67)31(15-8-20-52-47(50)51)55-39(63)30(49)14-6-7-19-48;3-2(4,5)1(6)7/h3-5,12-13,28,30-37,61H,6-11,14-27,48-49H2,1-2H3,(H,53,65)(H,54,62)(H,55,63)(H,56,66)(H,57,64)(H,70,71)(H4,50,51,52);(H,6,7)/t30-,31-,32-,33-,34-,35-,36-,37-;/m0./s1
InChi Key
XZONNUSAEDEAIA-YHHCAOACSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $82

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    10 mg

    $146

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    25 mg

    $343

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    50 mg

    $643

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    Product Description

    Lys-(Des-Arg9, Leu8)-Bradykinin is a bradykinin B1 receptor antagonist (Ki = 0.43 nM for the rabbit aorta receptor).1 It is selective for the bradykinin B1 over the B2 receptor (Ki = >10 µM for the rabbit ileum receptor).2 Lys-(Des-Arg9, Leu8)-Bradykinin inhibits contractions induced by the bradykinin B1 receptor agonist Des-Arg9-bradykinin (Item No. 31136) in isolated rabbit aortic rings (pA2 = 8.54).3 Intraperitoneal administration of Lys-(Des-Arg9, Leu8)-bradykinin (5 mg/kg per day for three days) reduces increases in paw edema in a rat model of arthritis induced by peptidoglycan-polysaccharide (PGPS).4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. MacNeil, T., Bierilo, K.K., Menke, J.G., et al. Cloning and pharmacological characterization of a rabbit bradykinin B1 receptor. Biochim. Biophys. Acta 1264(2), 223-228 (1995).

    2. Meini, S., Cucchi, P., Catalani, C., et al. Radioligand binding characterization of the bradykinin B2 receptor in the rabbit and pig ileal smooth muscle. Eur. J. Pharmacol. 635(1-3), 34-39 (2010).

    3. Drapeau, G., Audet, R., Levesque, L., et al. Development and in vivo evaluation of metabolically resistant antagonists of B1 receptors for kinins. J. Pharmacol. Exp. Ther. 266(1), 192-199 (1993).

    4. Blais, C., Jr., Couture, R., Drapeau, G., et al. Involvement of endogenous kinins in the pathogenesis of peptidoglycan-induced arthritis in the Lewis rat. Arthritis Rheum. 40(7), 1327-1333 (1997).