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Merck
CN
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主要文件

安全信息

SML3710

Sigma-Aldrich

Linaclotide

≥95% (HPLC)

别名:

CCEFCCNPACTGCF-OH cyclo(1-6),(2-10),(5-13)-tris(disulfide), Cys-Cys-Glu-Tyr-Cys-Cys-Asn-Pro-Ala-Cys-Thr-Gly-Cys-Tyr-OH cyclo(1-6),(2-10),(5-13)-tris(disulfide), L-Cysteinyl-L-cysteinyl-L-α-glutamyl-L-tyrosyl-L-cysteinyl-L-cysteinyl-L-asparaginyl-L-prolyl-L-alanyl-L-cysteinyl-L-threonylglycyl-L-cysteinyl-L-tyrosine-OH cyclo(1-6),(2-10),(5-13)-tris(disulfide)

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About This Item

经验公式（希尔记法）:
C59H79N15O21S6
CAS号:
851199-59-2
分子量:
1526.74
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

100

方案

≥95% (HPLC)

表单

(Powder or Lyophilized powder or film)

储存条件

desiccated

颜色

white to off-white

储存温度

-10 to -25°C

SMILES字符串

S1SC[C@@H]2NC(=O)[C@@H](NC(=O)[C@H]3N(CCC3)C(=O)[C@@H](NC(=O)[C@H]4NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CSSC4)N)C1)CCC(=O)O)Cc6ccc(cc6)O)CSSC[C@H](NC(=O)CNC(=O)C(NC2=O)[C@H](O)C)C(=O)N[C@@H](Cc5ccc(cc5)O)C(=O)O)CC(=O)N)C

InChI

1S/C59H79N15O21S6/c1-26-47(82)69-41-25-101-99-22-38-52(87)65-33(13-14-45(80)81)49(84)66-34(16-28-5-9-30(76)10-6-28)50(85)71-40(54(89)72-39(23-97-96-20-32(60)48(83)70-38)53(88)67-35(18-43(61)78)58(93)74-15-3-4-42(74)56(91)63-26)24-100-98-21-37(64-44(79)19-

InChI key

KXGCNMMJRFDFNR-IURAOCFRSA-N

生化/生理作用

Linaclotide is an orally active guanylate cyclase-C (GC-C) agonist that competes against bacterial STa enterotoxin binding to intestinal mucosal membranes from wild-type, but not GC-C null, mice (Ki = 16.4 nM). Linaclotide stimulates fluid secretion, upregulates cGMP accumulation in the intestinal lumen (5 μg/100 μL via injection into surgically ligated intestinal loops), and significantly increases the rate of gastrointestinal transit when administered orally in mice in vivo (100 μg/kg p.o.).

注意

Hygroscopic

象形图

Exclamation mark
GHS07

警示用语：

Warning

危险声明

H302

危险分类

Acute Tox. 4 Oral

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

常规特殊物品

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分析证书(COA)

Lot/Batch Number
0000378035
0000378035
0000239578
0000242552
0000242552

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Alexander P Bryant et al.
Life sciences, 86(19-20), 760-765 (2010-03-24)
Linaclotide is an orally administered 14-amino acid peptide being developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation. We determined the stability of linaclotide in the intestine, measured the oral bioavailability, and investigated whether the pharmacodynamic
John Cuppoletti et al.
BMC pharmacology, 12, 3-3 (2012-05-05)
Linaclotide has been proposed as a treatment for the same gastrointestinal indications for which lubiprostone has been approved, chronic idiopathic constipation and irritable bowel syndrome with constipation. Stressors damage the epithelial cell barrier and cellular homeostasis leading to loss of
Robert W Busby et al.
European journal of pharmacology, 649(1-3), 328-335 (2010-09-25)
Linaclotide is a first-in-class, orally administered 14-amino acid peptide that is in development for the treatment of irritable bowel syndrome with constipation and chronic constipation. We have characterized the solution structure of linaclotide, the in vitro binding and agonist activity

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