M 1145Potent and selective GAL2 agonist CAS# 1172089-00-7 |
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Quality Control & MSDS
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| Cas No. | 1172089-00-7 | SDF | Download SDF |
| PubChem ID | 71744999 | Appearance | Powder |
| Formula | C128H205N37O32 | M.Wt | 2774.26 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 5 mg/ml in water | ||
| Sequence | RGRGNWTLNSAGYLLGPVLPPPALALA (Modifications: Ala-27 = C-terminal amide) | ||
| SMILES | CC(C)CC(C(=O)NC(C)C(=O)NC(CC(C)C)C(=O)NC(C)C(=O)N)NC(=O)C(C)NC(=O)C1CCCN1C(=O)C2CCCN2C(=O)C3CCCN3C(=O)C(CC(C)C)NC(=O)C(C(C)C)NC(=O)C4CCCN4C(=O)CNC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC5=CC=C(C=C5)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(CC6=CNC7=CC=CC=C76)NC(=O)C(CC(=O)N)NC(=O)CNC(=O)C(CCCNC(=N)N)NC(=O)CNC(=O)C(CCCNC(=N)N)N | ||
| Standard InChIKey | XIHYPTIVAPJZFP-HEPWHOECSA-N | ||
| Standard 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)/t69-,70-,71-,72-,73+,78-,80-,81-,82-,83-,84-,85-,86-,87-,88-,89-,90-,91-,92-,93-,94-,95-,102-,103-/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. |
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| 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. |
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| 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. | ||
| Description | Potent and selective galanin receptor 2 (GAL2) agonist (EC50 = 38 nM, Ki values are 6.55, 497 and 587 nM at GAL2, GAL3 and GAL1 respectively). Has an additive effect on the signal transduction of galanin. |
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Extended release versus immediate release tacrolimus in kidney transplant recipients: a systematic review and meta-analysis.[Pubmed:29961086]
Eur J Clin Pharmacol. 2018 Oct;74(10):1249-1260.
PURPOSE: To compare the estimated glomerular filtration rate (eGFR) at 12 months together with other outcomes among adult kidney transplant recipients (KTRs) who received extended release, once daily tacrolimus (ER-Tac) compared to those who received the immediate release, twice daily tacrolimus (IR-Tac) administration. METHODS: In accordance with the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) Statement, we systematically reviewed all randomized controlled trials (RCTs) that compared clinical outcomes between ER-Tac versus IR-Tac in KTRs. The systematic searches were conducted on PubMed, EMBASE, Cochrane Register of Controlled Trials, Scopus, Web of Science, and CINAHL without language restriction. The trials registered and reference lists were also searched and reviewed. Data were extracted for eGFR, serum creatinine (Scr), creatinine clearance (CrCl), biopsy-proven acute rejection rate (BPAR), graft survival, and overall patient survival at different times over 24 months after kidney transplant (KT). A meta-analysis was performed to integrate the results from eligible studies. RESULTS: FroM 1145 articles screened, 11 RCTs were included. The pooled results of included RCTs showed no significant difference of eGFR at 12 months between ER-Tac and IR-Tac groups (four trials, n = 1738; mean difference - 0.77 mL/min/1.73 m(2), 95% CI: - 2.41 to 0.87; p = 0.56; I(2) = 0%). Comparing between the two tacrolimus formulations, there were no significant differences of eGFR, CrCl, Scr, BPAR, graft survival, and patient survival at different times over 4 years after transplantation. CONCLUSIONS: Based upon currently available evidences in KTRs, the impact on kidney allograft function appears to be comparable between ER-Tac and IR-Tac.
A novel GalR2-specific peptide agonist.[Pubmed:19467704]
Neuropeptides. 2009 Jun;43(3):187-92.
The galanin peptide family and its three receptors have with compelling evidence been implicated in several high-order physiological disorders. The co-localization with other neuromodulators and the distinct up-regulation during and after pathological disturbances has drawn attention to this neuropeptide family. In the current study we present data on receptor binding and functional response for a novel galanin receptor type 2 (GalR2) selective chimeric peptide, M1145 [(RG)(2)-N-galanin(2-13)-VL-(P)(3)-(AL)(2)-A-amide]. The M1145 peptide shows more than 90-fold higher affinity for GalR2 over GalR1 and a 76-fold higher affinity over GalR3. Furthermore, the peptide yields an agonistic effect in vitro, seen as an increase in inositol phosphate (IP) accumulation, both in the absence or the presence of galanin. The peptide design with a N-terminal extension of galanin(2-13), prevails new insights in the assembly of novel subtype specific ligands for the galanin receptor family and opens new possibilities to apply the galanin system as a putative drug target.
