COG133 (trifluoroacetate salt)

COG133 is a peptide fragment of ApoE that corresponds to residues 133-149 of the ApoE LDL receptor-binding domain and an antagonist of alpha7 nicotinic acetylcholine receptors (nAChRs, IC50 = 720 nM). It suppresses TNF-alpha and nitric oxide (NO) release in BV-2 microglia when used at concentrations ranging from 10 to 50 µM. In vivo, COG133 reduces LPS-induced increases in brain levels of TNF-alpha and IL-6 in mice. It decreases hippocampal neuronal degeneration and the latency to find the platform in the Morris water maze in a mouse model of closed head injury induced by surgical midline impact when administered at doses of 203 and 406 µg/kg. COG133 (1 mg/kg) also delays disease onset and reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).Formal Name: N-acetyl-L-leucyl-L-arginyl-L-valyl-L-arginyl-L-leucyl-L-alanyl-L-seryl-L-histidyl-L-leucyl-L-arginyl-L-lysyl-L-leucyl-L-arginyl-L-lysyl-L-arginyl-L-leucyl-L-leucinamide, trifuoroacetate salt. CAS Number: 514200-66-9. Synonyms: Ac-LRVRLASHLRKLRKRLL-NH2, ApoE (133-149). Molecular Formula: C97H181N37O19 . XCF3COOH. Formula Weight: 2169.7. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 1 mg/ml, PBS (pH 7.2): 1 mg/ml. SMILES: CC(C)C[C@@H](C(N)=O)NC([C@H](CC(C)C)NC([C@H](CCCNC(N)=N)NC([C@H](CCCCN)NC([C@H](CCCNC(N)=N)NC([C@H](CC(C)C)NC([C@H](CCCCN)NC([C@H](CCCNC(N)=N)NC([C@H](CC(C)C)NC([C@@H](NC([C@H](CO)NC([C@H](C)NC([C@H](CC(C)C)NC([C@H](CCCNC(N)=N)NC([C@H](C(C)C)NC([C@H](CCCNC(N)=N)NC([C@@H](NC(C)=O)CC(C)C)=O)=O)=O)=O)=O)=O)=O)CC1=CN=CN1)=O)=O)=O)=O)=O)=O)=O)=O)=O.FC(F)(C(O)=O)F. InChi Code: InChI=1S/C97H181N37O19.C2HF3O2/c1-50(2)40-67(76(100)137)127-89(150)72(45-55(11)12)130-82(143)64(30-23-37-114-95(105)106)122-78(139)60(26-17-19-33-98)120-79(140)62(28-21-35-112-93(101)102)123-87(148)70(43-53(7)8)129-81(142)61(27-18-20-34-99)121-80(141)63(29-22-36-113-94(103)104)124-88(149)71(44-54(9)10)131-90(151)73(46-59-47-111-49-117-59)132-91(152)74(48-135)133-77(138)57(15)118-85(146)69(42-52(5)6)128-83(144)65(31-24-38-115-96(107)108)126-92(153)75(56(13)14)134-84(145)66(32-25-39-116-97(109)110)125-86(147)68(41-51(3)4)119-58(16)136,3-2(4,5)1(6)7/h47,49-57,60-75,135H,17-46,48,98-99H2,1-16H3,(H2,100,137)(H,111,117)(H,118,146)(H,119,136)(H,120,140)(H,121,141)(H,122,139)(H,123,148)(H,124,149)(H,125,147)(H,126,153)(H,127,150)(H,128,144)(H,129,142)(H,130,143)(H,131,151)(H,132,152)(H,133,138)(H,134,145)(H4,101,102,112)(H4,103,104,113)(H4,105,106,114)(H4,107,108,115)(H4,109,110,116),(H,6,7)/t57-,60-,61-,62-,63-,64-,65-,66-,67-,68-,69-,70-,71-,72-,73-,74-,75-,/m0./s1. InChi Key: YRYTWYOGXATSSP-BGJGLIJFSA-N.