Vapreotide acetate (1:x) - CAS 849479-74-9
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C57H70N12O9S2.xC2H4O2
Molecular Weight:
1191.43 (x=1)
COA:
Inquire
Targets:
Others
Description:
Vapreotide is a synthetic somatostatin analog as a Somatotropin receptor antagonist. It can be used for the treatment of esophageal variceal bleeding in patients with cirrhotic liver disease and AIDS-related diarrhea.
Purity:
98%
Related CAS:
103222-11-3 (free base)
Appearance:
Powder
Synonyms:
BMY41606; RC160; BMY 41606; RC 160; BMY-41606; RC-160; Octastatin; (4R,7S,10S,13S,16S,19R)-13-((1H-indol-3-yl)methyl)-N-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-19-((R)-2-amino-3-phenylpropanamido)-10-(4-aminobutyl)-16-(4-hydroxybenzyl)-7-isopropyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carboxamide acetate
Solubility:
Soluble in DMSO
MSDS:
Inquire
Application:
esophageal variceal bleeding
Shelf Life:
2 month in rt, long time
InChIKey:
KBIZSMHYSQUHDH-UHFFFAOYSA-N
InChI:
InChI=1S/C57H70N12O9S2.C2H4O2/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;1-2(3)4/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);1H3,(H,3,4)
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.CC(=O)O
1.A new radiolabelled somatostatin analogue [111In-DTPA-D-Phe1]RC-160: preparation, biological activity, receptor scintigraphy in rats and comparison with [111In-DTPA-D-Phe1]octreotide.
Breeman WA;Hofland LJ;van der Pluijm M;van Koetsveld PM;de Jong M;Setyono-Han B;Bakker WH;Kwekkeboom DJ;Visser TJ;Lamberts SW Eur J Nucl Med. 1994 Apr;21(4):328-35.
We have evaluated the potential usefulness of indium-111 labelled [DTPA-D-Phe1]RC-160, derived from the octapeptide somatostatin analogue RC-160, as a radiopharmaceutical for the in vivo detection of somatostatin receptor-positive tumours. For this purpose 111In-and 115In-labelled [DTPA-D-Phe1]RC-160 was tested for its biological activity, and applied for somatostatin receptor scintigraphy in vivo to rats bearing the transplantable rat pancreatic tumour CA20948, which expresses somatostatin receptors. We previously described the development of the 111In-labelled somatostatin analogue [DTPA-D-Phe1]octreotide and its use in the in vivo visualization of somatostatin receptor-positive tumours in rats and in humans. Like [111In-DTPA-D-Phe1]octreotide, [111In-DTPA-D-Phe1]RC-160 showed uptake in and specific binding in vivo to somatostatin receptor-positive organs and tumours, and the tumours were clearly visualized by gamma camera scintigraphy. However, as compared to [111In-DTPA-D-Phe1]octreotide, blood radioactivity (background) was higher, resulting in a lower tumour to blood (background) ratio. Using this animal model we therefore conclude that [111In-DTPA-D-Phe1]RC-160 has no advantage over [111In-DTPA-D-Phe1]octreotide as a radiopharmaceutical in the visualization of somatostatin receptors which bind both analogues.
2.Inhibition of PC-3 human prostate cancers by analogs of growth hormone-releasing hormone (GH-RH) endowed with vasoactive intestinal peptide (VIP) antagonistic activity.
Plonowski A;Varga JL;Schally AV;Krupa M;Groot K;Halmos G Int J Cancer. 2002 Apr 1;98(4):624-9.
Vasoactive intestinal peptide (VIP) stimulates the proliferation and invasiveness of malignant prostatic cells. Receptors for VIP and the closely related growth hormone-releasing hormone (GH-RH) show considerable homology and are found in prostatic and other carcinomas. Among various analogs of GH-RH synthesized, JV-1-52 is a non-selective VIP/GH-RH antagonist, whereas JV-1-53 is a VIP antagonist devoid of GH-RH antagonistic effect. In our study, nude mice bearing PC-3 human androgen-independent prostate carcinomas were treated with JV-1-52 or JV-1-53 (20 microg/day, s.c.) for 28 days. Both antagonists produced a similar reduction in tumor volume (62-67%, p < 0.01) and tumor weight (59-62%; p < 0.05) vs. controls and extended tumor doubling-time from 9.1 to about 16 days (p < 0.05). To investigate the mechanisms involved, in another study we compared the effects of JV-1-53 with those of somatostatin analog RC-160. VIP antagonist JV-1-53 reduced tumor weight by 67% (p < 0.01) and suppressed the expression of mRNA for c-fos and c-jun oncogenes by about 34% (p < 0.05), without affecting serum levels of insulin-like growth factor-I (IGF-I). In contrast, RC-160 (50 microg/day) reduced serum IGF-I by 19% (p < 0.
3.Activation of human somatostatin receptor type 2 causes inhibition of cell growth in transfected HEK293 but not in transfected CHO cells.
Ren J;Bell G;Coy DH;Brunicardi FC J Surg Res. 1997 Jul 15;71(1):13-8.
Somatostatin (SS) is known to have an antiproliferative effect on cell growth via somatostatin receptors (SSTR). The purpose of this study was to transfect cell lines with human SSTR2 and determine the subsequent effect on cell growth in response to SSTR agonist. Heterologous Chinese hamster ovary (CHO-K1) and human embryonic kidney 293 (HEK) cells were transfected with SSTR2 cDNA using lipofectin. Stable transformants were selected by G418 and confirmed by 125I-SS binding and RT-PCR. Binding studies were performed in the presence of 10(-6) to 10(-12) M SS-14, SS-28, SS analogue RC-160, SSTR2 agonist NC-9-74, and SSTR5 agonist DC-37-39. Cell growth was determined by counting cell numbers after 48 hr incubation in the presence of 10(-6) to 10(-12) M SSTR2 agonist NC-9-74. Binding of 125I-SS-14 to transfected CHO and transfected HEK293 cells showed that the cells had high affinity for SS-14, SS-28, NC-9-74, and RC-160 but low affinity for DC-37-39. Incubation with 10(-6) to 10(-12) M NC-9-74, showed that 1 nM to 1 microM NC-9-74 significantly inhibited transfected HEK293 cell growth but did not affect growth on transfected CHO cells (n = 4 for each dose, P < 0.01). The two cell lines transfected with the human SSTR2 showed similar high affinity for SS-14, SS-28, RC-160, and SSTR2 agonist but not SSTR5 agonist.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Products


CAS 3688-85-5 Diapamide

Diapamide
(CAS: 3688-85-5)

Diapamide is a new diuretic and antihypertensive agent.

CAS 1077-28-7 DL-ThioCtic acid

DL-ThioCtic acid
(CAS: 1077-28-7)

DL-α-Lipoic acid is an non-specific free radical scavenger and has anti-oxidant properties. It could be used as a fat-metabolism stimulator.

RUSKI-201 dihydrochloride

RUSKI-201 dihydrochloride is a sonic hedgehog acyltransferase (HHAT) inhibitor (IC50 = 0.20 μM) devoid of off-target cytotoxicity, and quantitative whole-proteo...

AL-321
(CAS: 74772-68-2)

AL-321 is a bio-active chemical, but no detailed information has been published yet.

CAS 1187-84-4 S-Methyl-L-cysteine

S-Methyl-L-cysteine
(CAS: 1187-84-4)

S-Methyl-L-cysteine, a theurapeutic for neurodegenerative diseases, is a substrate in the catalytic antioxidant system mediated by methionine sulfoxide reductas...

CAS 356102-14-2 Ani 9

Ani 9
(CAS: 356102-14-2)

Ani 9 is a highly selective and potent anoctamin1 (ANO1)/transmembrane protein 16A (TMEM16A) inhibitor with IC50 value of 77 nM. It completely inhibits ANO1 chl...

CAS 51460-26-5 Carbazochrome sodium sulfonate (AC-17)

Carbazochrome sodium sulfonate (AC-17)
(CAS: 51460-26-5)

Carbazochrome sodium sulfonate (AC-17) is an antihemorrhagic for use in the treatment of hemorrhoids.

CAS 150113-99-8 Decanoyl-RVKR-CMK

Decanoyl-RVKR-CMK
(CAS: 150113-99-8)

Decanoyl-RVKR-CMK is a proprotein convertase inhibitor and has been found to restrain regulated secretion of the neuronal polypeptide VGF in PC12 cells.

Quick Inquiry

Verification code

Featured Items