R 715 (trifluoroacetate salt)

R 715 is a bradykinin B1 receptor antagonist. It inhibits contractions induced by bradykinin (Cay-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, Cay-13104). 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. R 715 (0.01 nmol/animal, i.c.v.) reduces mean arterial blood pressure and increases heart rate in spontaneously hypertensive rats.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-betaNal7,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: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 20 mg/ml, PBS (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.