M1145

M1145, a chimeric peptide, is a selective galanin receptor type 2 (GAL2) agonist, with a Ki of 6.55 nM. M1145 shows more than 90-fold higher affinity for GAL2 over GAL1 (Ki=587 nM) and a 76-fold higher affinity over GalR3 (Ki=497 nM). M1145 has an additive effect on the signal transduction of galanin.

Product information

CAS Number: 1172089-00-7

Molecular Weight: 2774.23

Formula: C128H205N37O32

Chemical Name: N-[1-[[1-[[1-[[4-amino-1-[[1-[[1-[[2-[[1-[[1-[[1-[[2-[2-[[1-[[1-[2-[2-[2-[[1-[[1-[[1-[[1-[(1-amino-1-oxopropan-2-yl)amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1, 4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[2-[[2-[[2-[(2-amino-5-carbamimidamidopentanoyl)amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]butanediamide

Smiles: CC(O)C(NC(=O)C(CC1=CNC2=CC=CC=C12)NC(=O)C(CC(N)=O)NC(=O)CNC(=O)C(CCCNC(N)=N)NC(=O)CNC(=O)C(N)CCCNC(N)=N)C(=O)NC(CC(C)C)C(=O)NC(CC(N)=O)C(=O)NC(CO)C(=O)NC(C)C(=O)NCC(=O)NC(CC1=CC=C(O)C=C1)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NCC(=O)N1CCCC1C(=O)NC(C(C)C)C(=O)NC(CC(C)C)C(=O)N1CCCC1C(=O)N1CCCC1C(=O)N1CCCC1C(=O)NC(C)C(=O)NC(CC(C)C)C(=O)NC(C)C(=O)NC(CC(C)C)C(=O)NC(C)C(N)=O

InChiKey: XIHYPTIVAPJZFP-UHFFFAOYSA-N

InChi: InChI=1S/C128H205N37O32/c1-62(2)46-81(110(181)143-60-101(174)162-42-24-32-92(162)121(192)160-102(68(13)14)122(193)158-90(51-67(11)12)124(195)164-44-26-34-94(164)126(197)165-45-27-35-95(165)125(196)163-43-25-33-93(163)120(191)147-72(18)107(178)152-83(48-64(5)6)112(183)146-71(17)106(177)151-82(47-63(3)4)111(182)144-69(15)104(132)175)153-113(184)84(49-65(7)8)154-115(186)86(52-74-36-38-76(168)39-37-74)149-99(172)57-140-105(176)70(16)145-119(190)91(61-166)159-117(188)89(55-97(131)170)156-114(185)85(50-66(9)10)157-123(194)103(73(19)167)161-118(189)87(53-75-56-139-79-30-21-20-28-77(75)79)155-116(187)88(54-96(130)169)150-100(173)59-142-109(180)80(31-23-41-138-128(135)136)148-98(171)58-141-108(179)78(129)29-22-40-137-127(133)134/h20-21,28,30,36-39,56,62-73,78,80-95,102-103,139,166-168H,22-27,29,31-35,40-55,57-61,129H2,1-19H3,(H2,130,169)(H2,131,170)(H2,132,175)(H,140,176)(H,141,179)(H,142,180)(H,143,181)(H,144,182)(H,145,190)(H,146,183)(H,147,191)(H,148,171)(H,149,172)(H,150,173)(H,151,177)(H,152,178)(H,153,184)(H,154,186)(H,155,187)(H,156,185)(H,157,194)(H,158,193)(H,159,188)(H,160,192)(H,161,189)(H4,133,134,137)(H4,135,136,138)

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

How to use

In Vitro:

M1145 has an additive effect on the signal transduction of galanin, are concentrations of M1145 of 0.1 μM and higher all give a maximum transduction. Signal transduction was examined by assessing the ability to stimulate inositol phosphates (IP) production in CHO cells expressing GalR2. Treatment with M1145, which stimulates IP production with an EC50 of 38 nM.

References:

1. Runesson J, Saar I, Lundström L, Järv J, Langel U. A novel GalR2-specific peptide agonist. Neuropeptides. 2009;43(3):187-192.

Products are for research use only. Not for human use.