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Potent, non-competitive antagonis of NMDA receptort (IC50 = 93 nM) that inhibits inward currents evoked by NMDA in central nervous system neurons (IC50 = 350 nM). Exhibits broad anticonvulsant and antiparkinsonian activity in vivo at doses devoid of behavioral toxicity.
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M.F/Formula | C127H201N35O49S3 |
M.W/Mr. | 3098.4 |
Sequence | H-Gly-Glu-Gla-Gla-Val-Ala-Lys-Met-Ala-Ala-Gla-Leu-Ala-Arg-Gla-Asn-Ile-Ala-Lys-Gly-Cys(1)-Lys-Val-Asn-Cys(1)-Tyr-Pro-OH |
Labeling Target | NMDA Receptor |
Appearance | White lyophilised solid |
Purity | >98% |
Activity | Antagonist |
Long-term Storage Conditions | Soluble in DMSO |
InChI | InChI=1S/C127H201N35O49S3/c1-15-57(8)93(116(192)142-62(13)96(172)145-69(24-16-19-36-128)99(175)137-51-89(167)144-83-52-213-214-53-84(113(189)157-82(43-63-29-31-64(163)32-30-63)117(193)162-40-23-28-85(162)126(210)211)158-109(185)80(48-86(132)164)156-115(191)92(56(6)7)159-104(180)71(148-112(83)188)26-18-21-38-130)161-111(187)81(49-87(133)165)155-108(184)78(46-67(122(202)203)123(204)205)152-102(178)72(27-22-39-136-127(134)135)147-95(171)60(11)140-105(181)75(42-54(2)3)151-106(182)76(44-65(118(194)195)119(196)197)150-98(174)59(10)138-94(170)58(9)139-100(176)74(35-41-212-14)149-101(177)70(25-17-20-37-129)146-97(173)61(12)141-114(190)91(55(4)5)160-110(186)79(47-68(124(206)207)125(208)209)154-107(183)77(45-66(120(198)199)121(200)201)153-103(179)73(33-34-90(168)169)143-88(166)50-131/h29-32,54-62,65-85,91-93,163H,15-28,33-53,128-131H2,1-14H3,(H2,132,164)(H2,133,165)(H,137,175)(H,138,170)(H,139,176)(H,140,181)(H,141,190)(H,142,192)(H,143,166)(H,144,167)(H,145,172)(H,146,173)(H,147,171)(H,148,188)(H,149,177)(H,150,174)(H,151,182)(H,152,178)(H,153,179)(H,154,183)(H,155,184)(H,156,191)(H,157,189)(H,158,185)(H,159,180)(H,160,186)(H,161,187)(H,168,169)(H,194,195)(H,196,197)(H,198,199)(H,200,201)(H,202,203)(H,204,205)(H,206,207)(H,208,209)(H,210,211)(H4,134,135,136)/t57-,58-,59-,60-,61-,62-,69-,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,84-,85-,91-,92-,93-/m0/s1 |
InChI Key | MJQQZSPLVNQFRB-HHXUSTKESA-N |
Isomeric SMILES | CC[C@H](C)[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)C(C)C)CC(=O)N)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N3CCC[C@H]3C(=O)O)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CC(C(=O)O)C(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C(=O)O)C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C(=O)O)C(=O)O)NC(=O)[C@H](CC(C(=O)O)C(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CN |
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