UFP101 (trifluoroacetate salt)

UFP101 is a synthetic peptide and an antagonist of the nociceptin receptor (Ki = 0.06 nM in CHO cells expressing the human receptor). It is selective for the nociceptin receptor over the kappa-opioid receptor (Ki = 204 nM in CHO cells expressing the rat receptor). UFP101 inhibits GTPgammaS release from the nociceptin receptor expressed in CHO cell membranes (EC50 = 1.86 nM). Intracerebroventricular administration of UFP101 (10 nmol/animal) increases the latency to tail withdrawal in the tail-flick test in mice. UFP101 (0.003, 0.03, and 0.3 mg/kg) increases survival in a mouse model of sepsis induced by cecal ligation and puncture.Formal Name: N-(phenylmethyl)glycylglycylglycyl-L-phenylalanyl-L-threonylglycyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-alanyl-L-arginyl-L-lysyl-L-arginyl-L-lysyl-L-asparaginyl-L-glutamamide, trifluoroacetate salt. Molecular Formula: C82H138N32O21 . XCF3COOH. Formula Weight: 1908.2. Purity: >95%. Formulation: (Request formulation change), A solid. Peptide Sequence: BnGGGFTGARKSARKRKNQ-NH2. Solubility: DMF: 5 mg/ml, DMSO: 10 mg/ml, PBS (pH 7.2): 10 mg/ml. SMILES: NC(CC[C@@H](C(N)=O)NC([C@H](CC(N)=O)NC([C@H](CCCCN)NC([C@H](CCCNC(N)=N)NC([C@H](CCCCN)NC([C@H](CCCNC(N)=N)NC([C@H](C)NC([C@H](CO)NC([C@H](CCCCN)NC([C@H](CCCNC(N)=N)NC([C@H](C)NC(CNC([C@H]([C@H](O)C)NC([C@@H](NC(CNC(CNC(CNCC1=CC=CC=C1)=O)=O)=O)CC2=CC=CC=C2)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O.OC(C(F)(F)F)=O. InChi Code: InChI=1S/C82H138N32O21.C2HF3O2/c1-45(102-64(121)43-101-79(135)66(47(3)116)114-77(133)57(37-48-19-6-4-7-20-48)104-65(122)42-100-63(120)41-99-62(119)40-95-39-49-21-8-5-9-22-49)68(124)106-54(26-16-34-96-80(89)90)71(127)110-53(25-12-15-33-85)75(131)113-59(44-115)78(134)103-46(2)69(125)107-55(27-17-35-97-81(91)92)72(128)108-51(23-10-13-31-83)70(126)111-56(28-18-36-98-82(93)94)73(129)109-52(24-11-14-32-84)74(130)112-58(38-61(87)118)76(132)105-50(67(88)123)29-30-60(86)117,3-2(4,5)1(6)7/h4-9,19-22,45-47,50-59,66,95,115-116H,10-18,23-44,83-85H2,1-3H3,(H2,86,117)(H2,87,118)(H2,88,123)(H,99,119)(H,100,120)(H,101,135)(H,102,121)(H,103,134)(H,104,122)(H,105,132)(H,106,124)(H,107,125)(H,108,128)(H,109,129)(H,110,127)(H,111,126)(H,112,130)(H,113,131)(H,114,133)(H4,89,90,96)(H4,91,92,97)(H4,93,94,98),(H,6,7)/t45-,46-,47+,50-,51-,52-,53-,54-,55-,56-,57-,58-,59-,66-,/m0./s1. InChi Key: JBYBTOHYBYFCOD-XLNLJAOCSA-N.