RC 160 - CAS 103222-11-3
Category: Inhibitor
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Molecular Formula:
C57H70N12O9S2
Molecular Weight:
1131.37
COA:
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Targets:
Neurokinin Receptor | Somatostatin Receptor
Description:
RC 160 is a cyclic octapeptide somatostatin analog (Ki= 0.7, 5.4, 30.9, 45 and > 1000 nM for sst5, sst2, sst3, sst4 and sst1 receptors respectively). RC 160 is a peptide neurokinin-1 receptor (NK1) antagonist and inhibits increases in vascular permeability stimulated by substance P in a concentration-dependent manner in isolated guinea pig trachea and main bronchi. It is used in the treatment of esophageal variceal bleeding in patients with cirrhotic liver disease and AIDS-related diarrhea.
Sequence:
FCYWKVCW
(Modifications: Phe-1 = D-Phe, Trp-4 = D-Trp, Trp-8 = C-terminal amide, Disulfide bridge between 2-7)
Related CAS:
849479-74-9 (acetate)
Synonyms:
D-phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-valyl-L-cysteinyl-L-tryptophanamide, cyclic (2→7)-disulfide; BMY-41606; BMY 41606; BMY41606; RC160; RC 160; RC-160; DP-05-094; Octastatin; Vapreotide acetate
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
Inquire
InChIKey:
SWXOGPJRIDTIRL-DOUNNPEJSA-N
InChI:
InChI=1S/C57H70N12O9S2/c1-32(2)49-57(78)68-48(55(76)64-44(50(60)71)26-35-28-61-41-16-8-6-14-38(35)41)31-80-79-30-47(67-51(72)40(59)24-33-12-4-3-5-13-33)56(77)65-45(25-34-19-21-37(70)22-20-34)53(74)66-46(27-36-29-62-42-17-9-7-15-39(36)42)54(75)63-43(52(73)69-49)18-10-11-23-58/h3-9,12-17,19-22,28-29,32,40,43-49,61-62,70H,10-11,18,23-27,30-31,58-59H2,1-2H3,(H2,60,71)(H,63,75)(H,64,76)(H,65,77)(H,66,74)(H,67,72)(H,68,78)(H,69,73)/t40-,43+,44+,45+,46-,47+,48+,49+/m1/s1
Canonical SMILES:
CC(C)C1C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=C(C=C4)O)NC(=O)C(CC5=CC=CC=C5)N)C(=O)NC(CC6=CNC7=CC=CC=C76)C(=O)N
1.Meta-analysis: vasoactive medications for the management of acute variceal bleeds.
Wells M1, Chande N, Adams P, Beaton M, Levstik M, Boyce E, Mrkobrada M. Aliment Pharmacol Ther. 2012 Jun;35(11):1267-78. doi: 10.1111/j.1365-2036.2012.05088.x. Epub 2012 Apr 8.
BACKGROUND: Vasoactive medications such as vasopressin, somatostatin and their analogues (terlipressin, vapreotide and octreotide) are commonly used for the treatment of acute variceal bleeding. However, the risks and benefits of these interventions are not well understood.
2.Multifunctional targeting vinorelbine plus tetrandrine liposomes for treating brain glioma along with eliminating glioma stem cells.
Li XT1, Tang W2, Jiang Y1, Wang XM1, Wang YH1, Cheng L1, Meng XS1. Oncotarget. 2016 Mar 25. doi: 10.18632/oncotarget.8360. [Epub ahead of print]
Malignant brain glioma is the most lethal and aggressive type of cancer. Surgery and radiotherapy cannot eliminate all glioma stem cells (GSCs) and blood-brain barrier (BBB) restricts the movement of antitumor drugs from blood to brain, thus leading to the poor prognosis with high recurrence rate. In the present study, the targeting conjugates of cholesterol polyethylene glycol polyethylenimine (CHOL-PEG2000-PEI) and D-a-tocopheryl polyethylene glycol 1000 succinate vapreotide (TPGS1000-VAP) were newly synthesized for transporting drugs across the BBB and targeting glioma cells and GSCs. The multifunctional targeting vinorelbine plus tetrandrine liposomes were constructed by modifying the targeting conjugates. The studies were undertaken on BBB model, glioma cells, GSCs, and glioma-bearing mice. In vitro results showed that multifunctional targeting drugs-loaded liposomes with suitable physicochemical property could enhance the transport drugs across the BBB, increase the intracellular uptake, inhibit glioma cells and GSCs, penetrate and destruct the GSCs spheroids, and induce apoptosis via activating related apoptotic proteins.
3.
4.111In-Labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-conjugated monomeric [Tyr3]octreotide.
AuthorsShan L.
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CAS 103222-11-3 RC 160

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