M617

Selective GAL1 agonist CAS# 860790-38-1

M617

Catalog No. BCC5929----Order now to get a substantial discount!

Product Name & Size Price Stock
M617: 5mg $1794 In Stock
M617: 10mg Please Inquire In Stock
M617: 20mg Please Inquire Please Inquire
M617: 50mg Please Inquire Please Inquire
M617: 100mg Please Inquire Please Inquire
M617: 200mg Please Inquire Please Inquire
M617: 500mg Please Inquire Please Inquire
M617: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of M617

Number of papers citing our products

Chemical structure

M617

3D structure

Chemical Properties of M617

Cas No. 860790-38-1 SDF Download SDF
PubChem ID 16158157 Appearance Powder
Formula C112H161N29O28 M.Wt 2361.68
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Galanin(1-13)-Gln<sup>14</sup>-bradykinin(2-9)amide
Solubility Soluble to 1 mg/ml in water
Sequence GWTLNSAGYLLGPQPPGFSPFR

(Modifications: Arg-22 = C-terminal amide)

Chemical Name (2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-5-amino-1-[(2S)-2-[(2S)-2-[[2-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1,5-dioxopentan-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]butanediamide
SMILES CC(C)CC(C(=O)NC(CC(C)C)C(=O)NCC(=O)N1CCCC1C(=O)NC(CCC(=O)N)C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NCC(=O)NC(CC4=CC=CC=C4)C(=O)NC(CO)C(=O)N5CCCC5C(=O)NC(CC6=CC=CC=C6)C(=O)NC(CCCNC(=N)N)C(=O)N)NC(=O)C(CC7=CC=C(C=C7)O)NC(=O)CNC(=O)C(C)NC(=O)C(CO)NC(=O)C(CC(=O)N)NC(=O)C(CC(C)C)NC(=O)C(C(C)O)NC(=O)C(CC8=CNC9=CC=CC=C98)NC(=O)CN
Standard InChIKey PAYBRARNTYCYOT-OTTBQUPZSA-N
Standard InChI InChI=1S/C112H161N29O28/c1-59(2)44-73(130-97(155)74(45-60(3)4)131-99(157)77(49-66-33-35-68(145)36-34-66)127-90(149)54-121-95(153)62(7)124-104(162)81(57-142)135-102(160)80(51-88(115)147)132-98(156)75(46-61(5)6)134-108(166)93(63(8)144)137-103(161)79(125-89(148)52-113)50-67-53-120-70-27-16-15-26-69(67)70)96(154)123-56-92(151)138-40-18-30-84(138)106(164)129-72(37-38-87(114)146)109(167)141-43-21-32-86(141)111(169)140-42-19-29-83(140)105(163)122-55-91(150)126-76(47-64-22-11-9-12-23-64)100(158)136-82(58-143)110(168)139-41-20-31-85(139)107(165)133-78(48-65-24-13-10-14-25-65)101(159)128-71(94(116)152)28-17-39-119-112(117)118/h9-16,22-27,33-36,53,59-63,71-86,93,120,142-145H,17-21,28-32,37-52,54-58,113H2,1-8H3,(H2,114,146)(H2,115,147)(H2,116,152)(H,121,153)(H,122,163)(H,123,154)(H,124,162)(H,125,148)(H,126,150)(H,127,149)(H,128,159)(H,129,164)(H,130,155)(H,131,157)(H,132,156)(H,133,165)(H,134,166)(H,135,160)(H,136,158)(H,137,161)(H4,117,118,119)/t62-,63+,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,84-,85-,86-,93-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of M617

DescriptionSelective galanin GAL1 receptor agonist (Ki values are 0.23 and 5.71 nM for GAL1 and GAL2 receptors respectively). Enhances food consumption in rats following i.c.v. administration and reduces CAP-induced inflammatory pain.

M617 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

M617 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University
Featured Products
New Products
 

References on M617

Antinociceptive effects induced by intra-periaqueductal grey injection of the galanin receptor 1 agonist M617 in rats with morphine tolerance.[Pubmed:23831348]

Neurosci Lett. 2013 Aug 29;550:125-8.

The present study was performed to investigate the antinociceptive effects of M617, a selective galanin receptor 1 agonist, and M1145, a selective galanin receptor 2 agonist, in the periaqueductal grey (PAG) in rats with morphine tolerance. Intra-PAG injection of 0.1 nmol, 0.5 nmol and 1 nmol of M617 induced dose-dependent increases in hindpaw withdrawal latencies (HWLs) to noxious thermal and mechanical stimulations in rats with morphine tolerance. Nevertheless, intra-PAG injection of 5 nmol of the selective galanin receptor 2 agonist M1145 showed no significant influences on HWLs to noxious thermal and mechanical stimulations in rats with morphine tolerance. The results demonstrated that it is the selective galanin receptor 1 agonist M617, not the selective galanin receptor 2 agonist M1145, induced significant antinociceptive effects in morphine-tolerant rats, indicating that galanin receptor 1 is involved in nociceptive modulation in the PAG of morphine-tolerant rats.

Antinociceptive effects induced by intra-lateral habenula complex injection of the galanin receptor 1 agonist M617 in rats.[Pubmed:26525710]

Exp Brain Res. 2016 Feb;234(2):493-7.

The present study was performed to explore the antinociceptive effects of the galanin receptor 1 agonist M617 in lateral habenula complex in rats. Intra-lateral habenula injection of 0.1, 0.5, 1 or 2 nmol of galanin induced dose-dependent increases in hindpaw withdrawal latencies (HWLs) to noxious thermal and mechanical stimulations in rats. Furthermore, intra-lateral habenula injection of 0.1, 0.5, 1 or 2 nmol of the galanin receptor 1 agonist M617 also induced dose-dependent increases in HWLs to noxious thermal and mechanical stimulations in rats. Interestingly, there were no significant differences between the antinociceptive effects induced by intra-lateral habenula injection of 2 nmol of M617 and 2 nmol of galanin. The results indicate that galanin receptor 1 may be involved in the galanin-induced antinociceptive effects in the lateral habenula.

Central injection of GALR1 agonist M617 attenuates diabetic rat skeletal muscle insulin resistance through the Akt/AS160/GLUT4 pathway.[Pubmed:27041232]

Mech Ageing Dev. 2017 Mar;162:122-128.

Insulin resistance of skeletal muscle plays an important role in the pathogenesis of type 2 diabetes. Galanin, a 29/30-amino-acid neuropeptide, plays multiple biological actions, including anti-diabetic effects. Although recent results of our study showed that administration of galanin could mitigate insulin resistance by promoting glucose transporter 4 (GLUT4) expression and translocation in skeletal muscle of rats, there is no literature available regarding to the effect of type 1 of galanin receptors (GALR1) on insulin resistance in skeletal muscle of type 2 diabetic rats. Herein, we intended to survey the central effect of GALR1 agonist M617 on insulin resistance in skeletal muscle and its underlying mechanisms. We found that the intracerebroventricular injection of M617 increased glucose infusion rates in hyperinsulinemic euglycemic clamp tests, but attenuated the plasma insulin and glucose concentrations of diabetic rats. Furthermore, administration of M617 markedly increased GLUT4 mRNA expression and GLUT4 translocation in skeletal muscle of diabetic rats. Last, perfusion of M617 increased phosphorylated Akt and phosphorylated AS160 levels in the skeletal muscle of diabetic rats. In conclusion, central injection of M617 mitigated insulin resistance of skeletal muscle by enhancing GLUT4 translocation from intracellular pools to plasma membranes via the activation of the Akt/AS160/GLUT4 signaling pathway.

Central injection of GalR1 agonist M617 facilitates GLUT4 expression in cardiac muscle of type 2 diabetic rats.[Pubmed:25449850]

Exp Gerontol. 2015 May;65:85-9.

Although galanin has been shown to increase GLUT4 expression in the cardiac muscle of rats, there is no literature available about the effect of GalR1 on GLUT4 expression in the cardiac muscle of type 2 diabetic rats. The aim of this study was to determine whether intracerebroventricular injection of GalR1 agonist M617 would elevate GLUT4 expression in the cardiac muscle of type 2 diabetic rats. The rats tested were divided into four groups: rats from healthy and type 2 diabetic drug groups were injected with 10nM/kg/d M617 in 5mul artificial cerebrospinal fluid for 21days, while control received 5mul vehicle injections. The blood samples were analyzed for glucose and insulin concentration. Cardiac muscle was collected and processed for determination of GLUT4 mRNA expression and GLUT4 protein levels. The present findings showed that fasting blood glucose levels in both M617 treatment groups were lower compared with each control. The insulin levels in both M617 treatment groups were decreased compared with each control. Moreover, the GLUT4 content in the cardiac muscle in both drug groups was higher compared with each control. M617 treatment increased GLUT4 mRNA expression and GLUT4 protein levels compared with each control group. These observations suggest that GalR1 agonist M617, acting through its central GalR1, can promote GLUT4 expression and enhance GLUT4 content in the cardiac muscle of type 2 diabetic rats. Central GalR1 may play a significant role in regulation of glucose metabolic homeostasis in the cardiac muscle of type 2 diabetic rats.

Activation of peripheral galanin receptors: differential effects on nociception.[Pubmed:16996122]

Pharmacol Biochem Behav. 2006 Sep;85(1):273-80.

Numerous reports suggest a significant role of peripheral galanin (GAL) in pain transmission; however, due to the lack of selective galanin receptor agonists and antagonists, the role of GAL receptors (GalR1-3) in pain transmission remains unclear. In this study, a new agonist, M617, that preferentially binds to GalR1, a GalR2 agonist (AR-M1896), and a GalR2 antagonist (M871) were tested in the periphery to elucidate the role of peripheral GalR1 and GalR2 in nociception. Ipsilateral, but not contralateral, hindpaw injection of M617 reduced capsaicin (CAP)-induced flinching by approximately 50%, suggesting that GalR1 activation produces anti-nociception. This anti-nociceptive effect was blocked by intraplantar injection of the non-selective GalR antagonist M35. In contrast ipsilateral, but not contralateral, intraplantar injection of GalR2 agonist AR-M1896 enhanced the CAP-induced nociception (1.7-fold). The GalR2 antagonist M871 blocked the pro-nociceptive effect of AR-M1896 in a dose-dependent manner. This antagonist had no effect on nociceptive behaviors induced by CAP alone. The data demonstrate that activation of peripheral GalR1 results in anti-nociception but activation of peripheral GalR2 produces pro-nociception. Thus, the use of these pharmacological tools may help to elucidate the contribution of GalR subtypes in nociceptive processing, identifying potential drug targets for the treatment of peripheral pain.

Regulation of kindling epileptogenesis by hippocampal galanin type 1 and type 2 receptors: The effects of subtype-selective agonists and the role of G-protein-mediated signaling.[Pubmed:16699066]

J Pharmacol Exp Ther. 2006 Aug;318(2):700-8.

The search for antiepileptic drugs that are capable of blocking the progression of epilepsy (epileptogenesis) is an important problem of translational epilepsy research. The neuropeptide galanin effectively suppresses acute seizures. We examined the ability of hippocampal galanin receptor type 1 (GalR1) and type 2 (GalR2) to inhibit kindling epileptogenesis and studied signaling cascades that mediate their effects. Wistar rats received 24-h-long intrahippocampal infusion of a GalR1/2 agonist galanin(1-29), GalR1 agonist M617 [galanin(1-13)-Gln14-bradykinin(2-9)-amide], or GalR2 agonist galanin(2-11). The peptides were administered alone or combined with an inhibitor of Gi protein pertussis toxin (PTX), Gi-protein activated K+ channels (GIRK) inhibitor tertiapin Q (TPQ), G(q/11) protein inhibitor [D-Arg1,D-Trp(5,7,9),Leu11]-substance P (dSP), or an inhibitor of intracellular Ca2+ release dantrolene. Sixteen hours into drug delivery, the animals were subjected to rapid kindling-60 electrical trains administered to ventral hippocampus every 5 min. M617 delayed epileptogenesis, whereas galanin(1-29) and galanin(2-11) completely prevented the occurrence of full kindled seizures. TPQ abolished anticonvulsant effect of M617 but not of galanin(2-11). PTX blocked anticonvulsant effects of M617 and inversed the action of galanin(1-29) and galanin(2-11) to proconvulsant. dSP and dantrolene did not modify seizure suppression through GalR1 and GalR2, but eliminated the proconvulsant effect of PTX + galanin(1-29) and PTX + galanin(2-11) combinations. We conclude that hippocampal GalR1 exert their disease-modifying effect through the Gi-GIRK pathway. GalR2 is antiepileptogenic through the Gi mechanism independent of GIRK. A secondary proconvulsant pathway coupled to GalR2 involves G(q/11) and intracellular Ca2+. The data are important for understanding endogenous mechanisms regulating epileptogenesis and for the development of novel antiepileptogenic drugs.

Keywords:

M617,860790-38-1,Galanin(1-13)-Gln<sup>14</sup>-bradykinin(2-9)amide,Natural Products,Galanin Receptors, buy M617 , M617 supplier , purchase M617 , M617 cost , M617 manufacturer , order M617 , high purity M617

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: