Related Diseases
                                                                Schizophrenia
                             
                                                                                                                    
                                                                                                                    
                                                                        
                                                                        
                                                                Description
                                                                BMS-933043 is a Selective α7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia. BMS-933043 showed potent binding affinity to native rat (Ki = 3.3 nM) and recombinant human alpha7 nicotinic acetylcholine receptors (Ki = 8.1 nM) and agonist activity in a calcium fluorescence assay (EC50 = 23.4 nM) and whole cell voltage clamp electrophysiology (EC50 = 0.14 micromolar (rat) and 0.29 micromolar (human)). BMS-933043 showed no agonist or antagonist activity at other nicotinic acetylcholine receptor subtypes and was at least 300 fold weaker at binding to and antagonizing human 5-HT3A receptors (Ki = 2,451 nM; IC50 = 8,066 nM).
                             
                                                                        
                                                                        
                                                                Chemical Formula
                                                                C16H19N7O
                             
                                                                        
                                                                        
                                                                        
                                                                Elemental Analysis
                                                                C, 59.06; H, 5.89; N, 30.13; O, 4.92
                             
                                                                        
                                                                Synonym
                                                                BMS-933043; BMS 933043; BMS933043.
                             
                                                                        
                                                                IUPAC/Chemical Name
                                                                (2R)-N-(6-(1H-imidazol-1-yl)-4-pyrimidinyl)-4'H-spiro[4-azabicyclo[2.2.2]octane-2,5'-[1,3]oxazol]-2'-amine
                             
                                                                        
                                                                InChi Key
                                                                RLXBHTUZCPORKT-INIZCTEOSA-N
                             
                                                                        
                                                                InChi Code
                                                                InChI=1S/C16H19N7O/c1-4-22-5-2-12(1)16(9-22)8-18-15(24-16)21-13-7-14(20-10-19-13)23-6-3-17-11-23/h3,6-7,10-12H,1-2,4-5,8-9H2,(H,18,19,20,21)/t16-/m0/s1
                             
                                                                        
                                                                SMILES Code
                                                                C1(CC2)[C@@]3(OC(NC4=NC=NC(N5C=CN=C5)=C4)=NC3)CN2CC1
                             
                                                                        
                                                                        
                                                                Purity
                                                                >98% (or refer to the Certificate of Analysis)
                             
                                                                        
                                                                Shipping Condition
                                                                Shipped under ambient temperature as non-hazardous chemical.  This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
                             
                                                                        
                                                                Storage Condition
                                                                Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
                             
                                                                        
                                                                Solubility
                                                                Soluble in DMSO
                             
                                                                        
                                                                Shelf Life
                                                                >2 years if stored properly
                             
                                                                        
                                                                Drug Formulation
                                                                This drug may be formulated in DMSO
                             
                                                                        
                                                                Stock Solution Storage
                                                                0 - 4℃ for short term (days to weeks), or -20℃ for long term (months).
                             
                                                                        
                                                                HS Tariff Code
                                                                2934.99.9001