PG 106Selective MC3 receptor antagonist CAS# 944111-22-2 |
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Quality Control & MSDS
3D structure
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| Cas No. | 944111-22-2 | SDF | Download SDF |
| PubChem ID | 134812822 | Appearance | Powder |
| Formula | C51H69N13O9 | M.Wt | 1008.19 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 1 mg/ml in 25% ethanol / water | ||
| Sequence | XDXXRWK (Modifications: X-1 = Ac-Nle, X-3 = beta-Ala, X-4 = D-2-Nal, Lys-7 = C-terminal amide, Asp-2, Lys-7, Cyclized) | ||
| Chemical Name | (3S)-16-(2-acetamidohexanoylamino)-6-[3-(diaminomethylideneamino)propyl]-3-(1H-indol-3-ylmethyl)-9-(naphthalen-2-ylmethyl)-2,5,8,11,15,18-hexaoxo-1,4,7,10,14,19-hexazacyclotetracosane-24-carboxamide | ||
| SMILES | CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)CCNC1=O)CC2=CC3=CC=CC=C3C=C2)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C | ||
| Standard InChIKey | ZFZDDBJAFMOQSH-RIXKQHLWSA-N | ||
| Standard InChI | InChI=1S/C51H69N13O9/c1-3-4-15-38(59-30(2)65)47(70)64-42-28-44(67)55-22-10-9-17-37(45(52)68)61-50(73)41(27-34-29-58-36-16-8-7-14-35(34)36)63-48(71)39(18-11-23-57-51(53)54)62-49(72)40(60-43(66)21-24-56-46(42)69)26-31-19-20-32-12-5-6-13-33(32)25-31/h5-8,12-14,16,19-20,25,29,37-42,58H,3-4,9-11,15,17-18,21-24,26-28H2,1-2H3,(H2,52,68)(H,55,67)(H,56,69)(H,59,65)(H,60,66)(H,61,73)(H,62,72)(H,63,71)(H,64,70)(H4,53,54,57)/t37?,38?,39?,40?,41-,42?/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 | Selective hMC3 receptor antagonist (IC50 = 210 nM). Exhibits no activity at hMC4 receptors and hMC5 receptors. |
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Further structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5.[Pubmed:17482720]
Peptides. 2007 Jun;28(6):1191-6.
Recently we have demonstrated that replacing His(6) by constrained amino acids(2) in the well-known antagonist SHU-9119 resulted in potent and selective antagonist ligands especially at the hMC3R and hMC5 receptors. With the aim to further explore position 6 in the sequence of SHU-9119 and MT-II, we have designed, synthesized, and pharmacologically characterized a series of peptide analogues of MT-II and SHU-9119 at the human melanocortin receptors subtypes MC3R, MC4R and MC5R. All these peptides were modified at position 6 with constrained amino acids which are commercially available. In this study, we have identified new selective ligands for the hMC4R, and an antagonist for the hMC3/hMC4 receptors. Additionally, we have discovered an interesting new selective antagonist at the hMC3R, Ac-Nle-c[Asp-betaAla-DNal(2')-Arg-Trp-Lys]-NH(2) (2, PG-106) which represents an important tool in further biological investigations of the hMC3R. PG-106 will be useful in further efforts to differentiate the substructural features responsible for selectivity at the hMC3R, hMC4R, and hMC5R.
PG 106,944111-22-2,Natural Products,Melanocortin (MC) Receptors, buy PG 106 , PG 106 supplier , purchase PG 106 , PG 106 cost , PG 106 manufacturer , order PG 106 , high purity PG 106
