A bradykinin B1 receptor antagonist
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R 715 (trifluoroacetate salt)

Item No. 36890

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N2-acetyl-L-lysyl-L-arginyl-L-prolyl-L-prolylglycyl-L-phenylalanyl-L-seryl-3-(2-naphthalenyl)-D-alanyl-L-isoleucine, trifluoroacetate salt
Synonyms
  • Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH
  • [Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK
Molecular Formula
C57H81N13O12 • XCF3COOH
Formula Weight
1140.3
Purity
≥95%
Formulation (Request formulation change)
A solid
Peptide Sequence
Ac-KRPPGFSXI-OH (X = (2-naphthalenyl)-D-alanyl)
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 20 mg/mlPBS (pH 7.2): 5 mg/ml
SMILES
O=C(N1[C@@H](CCC1)C(NCC(N[C@H](C(N[C@@H](CO)C(N[C@@H](C(N[C@H](C(O)=O)[C@@H](C)CC)=O)CC2=CC3=C(C=CC=C3)C=C2)=O)=O)CC4=CC=CC=C4)=O)=O)[C@H]5N(CCC5)C([C@H](CCCNC(N)=N)NC([C@@H](NC(C)=O)CCCCN)=O)=O.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C57H81N13O12.C2HF3O2/c1-4-34(2)48(56(81)82)68-51(76)43(31-37-23-24-38-17-8-9-18-39(38)29-37)66-52(77)44(33-71)67-50(75)42(30-36-15-6-5-7-16-36)64-47(73)32-62-53(78)45-21-13-27-69(45)55(80)46-22-14-28-70(46)54(79)41(20-12-26-61-57(59)60)65-49(74)40(63-35(3)72)19-10-11-25-58;3-2(4,5)1(6)7/h5-9,15-18,23-24,29,34,40-46,48,71H,4,10-14,19-22,25-28,30-33,58H2,1-3H3,(H,62,78)(H,63,72)(H,64,73)(H,65,74)(H,66,77)(H,67,75)(H,68,76)(H,81,82)(H4,59,60,61);(H,6,7)/t34-,40-,41-,42-,43+,44-,45-,46-,48-;/m0./s1
InChi Key
ZFUJDXXJCMFOSK-WBUMRSSGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    R 715 is a bradykinin B1 receptor antagonist.1 It inhibits contractions induced by bradykinin (Item No. 37408) in isolated human umbilical cords, which express bradykinin B1 receptors (pA2 = 8.49). R 715 (200, 400, and 600 µg/kg) decreases the latency to tail withdrawal in the tail-flick test in a mouse model of diabetic neuropathy induced by streptozotocin (STZ; Item No. 13104).2 It reduces the incidence of hind limb weakness and paralysis, improves symmetrical gait, as well as decreases spinal inflammatory foci numbers, neuron demyelination, and lesion monocyte invasion, in a myelin oligodendrocyte glycoprotein (MOG) (35-55) (MOG35-55) antigen peptide-induced mouse model of experimental autoimmune encephalomyelitis (EAE) when administered at a dose of 1 mg/kg per day.3 R 715 (0.01 nmol/animal, i.c.v.) reduces mean arterial blood pressure and increases heart rate in spontaneously hypertensive rats.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gobeil, F., Neugebauer, W., Filteau, C., et al. Structure-activity studies of B1 receptor-related peptides. Antagonists. Hypertension 28(5), 833-839 (1996).

    2. Gabra, B.H., and Sirois, P. Role of bradykinin B1 receptors in diabetes-induced hyperalgesia in streptozotocin-treated mice. Eur. J. Pharmacol. 457(2-3), 115-124 (2002).

    3. Göbel, K., Pankratz, S., Schneider-Hohendorf, T., et al. Blockade of the kinin receptor B1 protects from autoimmune CNS disease by reducing leukocyte trafficking. J. Autoimmun. 36(2), 106-114 (2011).

    4. Emanueli, C., Chao, J., Regoli, D., et al. The bradykinin B1 receptor and the central regulation of blood pressure in spontaneously hypertensive rats. Br. J. Pharmacol. 126(8), 1769-1776 (1999).