详情描述
AC 253 is an Amylin (AMY3) receptor antagonist, inhibiting andrenomedulin-stimulated cAMP production. AC 253 protects against oligomeric Aβ-induced increase in intracellular Ca2+, activation of PKA, MAPK, Akt and cFOS and cell death in neuronal cell culture. AC 253 blocks electrophysiological effects of Aβ.
Product information
CAS Number: 151804-79-4
Molecular Weight: 2847.11
Formula: C122H196N40O39
Chemical Name: (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-5-amino-5-oxopentanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S, 3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S, 3R)-1-[[(2S)-4-amino-1-[[(2S, 3R)-1-[[2-[[(2S)-1-[[(2S)-4-amino-1-[[(2S, 3R)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1, 4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1, 4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1, 5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid
Smiles: CC(=O)NC(CC(C)C)C(=O)NCC(=O)NC(CCCNC(N)=N)C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCC(N)=O)C(=O)NC(CCC(O)=O)C(=O)NC(CC(C)C)C(=O)NC(CC1=CNC=N1)C(=O)NC(CCCNC(N)=N)C(=O)NC(CC(C)C)C(=O)NC(CCC(N)=O)C(=O)NC(C(C)O)C(=O)NC(CC1C=CC(O)=CC=1)C(=O)N1CCCC1C(=O)NC(CCCNC(N)=N)C(=O)NC(C(C)O)C(=O)NC(CC(N)=O)C(=O)NC(C(C)O)C(=O)NCC(=O)NC(CO)C(=O)NC(CC(N)=O)C(=O)NC(C(C)O)C(=O)NC(CC1C=CC(O)=CC=1)C(N)=O
InChiKey: QOVDFCPGVUGNIP-UHFFFAOYSA-N
InChi: InChI=1S/C122H196N40O39/c1-55(2)40-76(141-63(13)169)99(181)138-50-91(176)142-69(18-14-36-135-120(128)129)100(182)150-79(43-58(7)8)108(190)157-85(53-164)113(195)147-72(30-33-87(123)172)102(184)145-74(32-35-93(178)179)103(185)152-78(42-57(5)6)107(189)153-80(46-66-49-134-54-140-66)109(191)144-70(19-15-37-136-121(130)131)101(183)151-77(41-56(3)4)106(188)146-73(31-34-88(124)173)105(187)160-97(62(12)168)118(200)156-83(45-65-24-28-68(171)29-25-65)119(201)162-39-17-21-86(162)114(196)148-71(20-16-38-137-122(132)133)104(186)159-96(61(11)167)117(199)155-82(48-90(126)175)111(193)158-94(59(9)165)115(197)139-51-92(177)143-84(52-163)112(194)154-81(47-89(125)174)110(192)161-95(60(10)166)116(198)149-75(98(127)180)44-64-22-26-67(170)27-23-64/h22-29,49,54-62,69-86,94-97,163-168,170-171H,14-21,30-48,50-53H2,1-13H3,(H2,123,172)(H2,124,173)(H2,125,174)(H2,126,175)(H2,127,180)(H,134,140)(H,138,181)(H,139,197)(H,141,169)(H,142,176)(H,143,177)(H,144,191)(H,145,184)(H,146,188)(H,147,195)(H,148,196)(H,149,198)(H,150,182)(H,151,183)(H,152,185)(H,153,189)(H,154,194)(H,155,199)(H,156,200)(H,157,190)(H,158,193)(H,159,186)(H,160,187)(H,161,192)(H,178,179)(H4,128,129,135)(H4,130,131,136)(H4,132,133,137)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: To be determined
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
References:
- H A Coppock, et al. Rat-2 fibroblasts express specific adrenomedullin receptors, but not calcitonin-gene-related-peptide receptors, which mediate increased intracellular cAMP and inhibit mitogen-activated protein kinase activity. Biochem J. 1999 Feb 15;338 ( Pt 1)(Pt 1):15-22.
- Wen Fu, ET AL. Amyloid β (Aβ) peptide directly activates amylin-3 receptor subtype by triggering multiple intracellular signaling pathways. J Biol Chem. 2012 May 25;287(22):18820-30.
- Jack H Jhamandas, et al. Actions of β-amyloid protein on human neurons are expressed through the amylin receptor. Am J Pathol. 2011 Jan;178(1):140-9.
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