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Pasireotide

Catalog No.: 61115
Cas No.: 396091-73-9
Purity : 98% 
61115 - Pasireotide | CAS 396091-73-9

Catalog number : 61115

CAS number : 396091-73-9

分子式 : C58H66N10O9 

分子量 : 1047.21 

Iupac 化学名称 : Pasireotide 

Smile : c1ccc(cc1)C[C@H]2C(=O)N3C[C@@H](C[C@H]3C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N2)Cc4ccc(cc4)OCc5ccccc5)CCCCN)Cc6c[nH]c7c6cccc7)c8ccccc8)OC(=O)NCCN

InChiKey : VMZMNAABQBOLAK-DBILLSOUSA-N

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同义词SOM 230; SOM 320 
英文同义词SOM 230; SOM 320 
分子式C58H66N10O9 
分子量1047.21 
外观crystalline solid 
纯度98% 
可溶性Soluble in DMSO 
存储3 years -20ºCpowder 
运输条件Shipped under ambient temperature as non-hazardous chemical. 
Smilec1ccc(cc1)C[C@H]2C(=O)N3C[C@@H](C[C@H]3C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N2)Cc4ccc(cc4)OCc5ccccc5)CCCCN)Cc6c[nH]c7c6cccc7)c8ccccc8)OC(=O)NCCN
InChiKeyVMZMNAABQBOLAK-DBILLSOUSA-N
InChiInChI=1S/C58H66N10O9/c59-27-13-12-22-46-52(69)64-47(30-38-23-25-42(26-24-38)76-36-39-16-6-2-7-17-39)53(70)66-49(31-37-14-4-1-5-15-37)57(74)68-35-43(77-58(75)61-29-28-60)33-50(68)55(72)67-51(40-18-8-3-9-19-40)56(73)65-48(54(71)63-46)32-41-34-62-45-21-11-10-20-44(41)45/h1-11,14-21,23-26,34,43,46-51,62H,12-13,22,27-33,35-36,59-60H2,(H,61,75)(H,63,71)(H,64,69)(H,65,73)(H,66,70)(H,67,72)/t43-,46+,47+,48-,49+,50+,51+/m1/s1
MDLMFCD08067735
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Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively).

SOM230 showed a lower potency of GH release inhibition (IC(50), 0.5 nM), compared with OCT (IC(50), 0.02 nM) and SRIF-14 (IC(50), 0.02 nM). A positive correlation was found between sst(2) but not sst(5) mRNA levels in the adenoma cells and the inhibitory potency of OCT on GH release in vivo and in vitro, and the effects of SOM230 and SRIF-14 in vitro [2].  In cultures of human fetal pituitary cells, SOM230 inhibited GH secretion by 42 +/- 9% (P = 0.002) but had no effect on TSH release. SOM230 inhibited GH release from GH-secreting adenoma cultures by 34 +/- 8% (P = 0.002), PRL by 35 +/- 4% from PRL-secreting adenomas (P = 0.01), and alpha-subunit secretion from nonfunctioning pituitary adenomas by 46 +/- 18% (P = 0.34).

 

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