ChemicalBook > CAS DataBase List > Linaclotide

Linaclotide

Product Name
Linaclotide
CAS No.
851199-59-2
Chemical Name
Linaclotide
Synonyms
Linacllotide;Rinalodipine Acetate;CY-14;Argpessin;Liclotide;inaclotide;Linaclotide;Linaelotide;Linaelotide Acetate;Linaclotide USP/EP/BP
CBNumber
CB82498818
Molecular Formula
C59H79N15O21S6
Formula Weight
1526.74
MOL File
851199-59-2.mol
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Linaclotide Property

Melting point:
231-235°C (dec.)
Boiling point:
2045.0±65.0 °C(Predicted)
Density 
1.60
storage temp. 
Hygroscopic, Refrigerator, under inert atmosphere
solubility 
DMSO (Slightly, Heated), Methanol ((Slightly, Heated)), Water (Slightly, Heated)
pka
3.05±0.10(Predicted)
form 
Solid
color 
White
Stability:
Hygroscopic
InChI
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)19-62-57(92)46(27(2)75)73-55(41)90)51(86)68-36(59(94)95)17-29-7-11-31(77)12-8-29/h5-12,26-27,32-42,46,75-77H,3-4,13-25,60H2,1-2H3,(H2,61,78)(H,62,92)(H,63,91)(H,64,79)(H,65,87)(H,66,84)(H,67,88)(H,68,86)(H,69,82)(H,70,83)(H,71,85)(H,72,89)(H,73,90)(H,80,81)(H,94,95)/t26-,27+,32-,33+,34-,35-,36-,37-,38-,39-,40-,41-,42-,46?/m0/s1
InChIKey
KXGCNMMJRFDFNR-VRMHCMCOSA-N
SMILES
[C@@]12(NC([C@]3([H])CSSC[C@@H](C(=O)N[C@@H](CC4C=CC(O)=CC=4)C(=O)O)NC(=O)CNC(=O)C([C@H](O)C)NC(=O)[C@]([H])(CSSC[C@@]([H])(C(=O)N[C@H](CCC(=O)O)C(N[C@@H](CC4C=CC(O)=CC=4)C(=O)N3)=O)NC(=O)[C@@H](N)CSSC1)NC(=O)[C@H](C)NC(=O)[C@]1([H])CCCN1C(=O)[C@H](CC(=O)N)NC2=O)=O)[H]
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Safety

Hazardous Substances Data
851199-59-2(Hazardous Substances Data)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
24085
Product name
Linaclotide
Purity
≥95%
Packaging
500μg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
24085
Product name
Linaclotide
Purity
≥95%
Packaging
1mg
Price
$57
Updated
2024/03/01
Cayman Chemical
Product number
24085
Product name
Linaclotide
Purity
≥95%
Packaging
5mg
Price
$184
Updated
2024/03/01
Cayman Chemical
Product number
24085
Product name
Linaclotide
Purity
≥95%
Packaging
10mg
Price
$330
Updated
2024/03/01
TRC
Product number
L465880
Product name
Linaclotide
Packaging
100mg
Price
$1540
Updated
2021/12/16
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Linaclotide Chemical Properties,Usage,Production

Description

In August 2012, the US FDA approved linaclotide (also referred to as MD-1100), a first-in-class, orally administered 14-amino acid peptide as a therapy for patients suffering from chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation (IBS-C). Linaclotide and its active metabolite MM-419447, which results from the cleavage of the C-terminal tyrosine residue by carboxypeptidase A, mimic the actions of the endogenous intestinal peptides guanylin (15 amino acids) and uroguanylin (16 amino acids) by activating guanylyl cyclase C (GC-C) on the intestinal epithelium. Activation of GC-C leads to increased intra- and extracellular levels of cGMP and activation of the CFTR ion channel, resulting in increased levels of HCO3-, Cl-, and water in the intestinal lumen and accelerated gastrointestinal transit. Based on an in vitro assaymeasuring the accumulation of cGMP in T84 cell exposed to an agonist, the EC50 of linaclotide at pH 7.0 was 99±17.5 nM. In preclinical studies in mice using the transit of activated charcoal as ameasure of efficacy, linaclotide at 100 μg/kg significantly accelerated transit compared to wild-type mice treated with charcoal only or GC-Cnullmice treatedwith and without linaclotide.118 Efficacy was also seen in rats treatedwith linaclotide atdoses of 5, 10, and 20 μg/kg. Linaclotide has been synthesized using conventional solid-phase peptide technology.

Originator

Ironwood Pharmaceuticals and Forest Pharmaceuticals (United States)

Uses

Linaclotide is a guanylate cyclase-C agonist currently being studied in Phase 3 trials for the treatment of irritable bowel syndrome with constipation.

Definition

ChEBI: Linaclotide is a fourteen-membered heterodetic cyclic peptide consisting of Cys, Cys, Glu, Tyr, Cys, Cys, Asn, Pro, Ala, Cys, Thr, Gly, Cys and Tyr residues joined in sequence and cyclised by three disulfide bonds: between Cys(1) and Cys(6), between Cys(2) and Cys(10), and between Cys(5) and Cys(13). Used for treatment of irritable bowel syndrome accompanied by constipation. It has a role as a guanylate cyclase 2C agonist.

brand name

Linzess

Biological Functions

Linaclotide works by increasing fluid in your intestines and helping speed up movement of food through the gut. Linaclotide may improve stool texture and lessen symptoms such as bloating, abdominal pain/discomfort, straining, and feelings of incomplete bowel movements.

Side effects

Side effects include:Diarrhea, abdominal pain, flatulence, abdominal distension, viral gastroenteritis, headache, upper respiratory tract infection, sinusitis

Linaclotide Preparation Products And Raw materials

Raw materials

Preparation Products

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Linaclotide Suppliers

Canada 1 China 249 India 9 Israel 1 Sweden 2 Switzerland 1 United States 12 Global 275
Chinese Peptide Company
Tel
0571-86737118-8680 15988144796
Email
sales@chinesepeptide.com
Country
China
ProdList
12
Advantage
58
GL Biochem (Shanghai) Ltd
Tel
21-61263452 13641803416
Fax
86-21-61263399
Email
ymbetter@glbiochem.com
Country
China
ProdList
9981
Advantage
64
Shenzhen JYMed Technology Co., Ltd.
Tel
755-755-26612112 15013529272;
Fax
+86 (755) 8635-0488
Email
jymed@jymedtech.com
Country
China
ProdList
81
Advantage
58
Hangzhou Peptide Biochem Co.,Ltd
Tel
0571-89197072; 18668118770
Fax
0571-89197072
Email
linda@peptide-china.com
Country
China
ProdList
248
Advantage
56
Hangzhou Xinhai Pharmaceutical Technology Co., Ltd.
Tel
0571-86758863 13867485072
Fax
0571-86758863
Email
lulu@thinheal.com
Country
China
ProdList
300
Advantage
58
Hangzhou Peptidego Biotech Co.,Ltd.
Tel
0571-87213919
Fax
0571-87213919
Email
eric@peptidego.com
Country
China
ProdList
6347
Advantage
58
Changzhou jinhan pharmaceutical technology co., LTD
Tel
13917833665
Email
lyg@world-goldpharma.com
Country
China
ProdList
144
Advantage
58
Apextide Co Ltd
Tel
15700198315
Email
shubin.zhao@apextide.com
Country
China
ProdList
73
Advantage
58
Beijing Zhongshuo Pharmaceutical Technology Development Co., Ltd
Tel
010-53679529 13801208576
Fax
010-64215766
Email
sales.2@chinazhongshuo.com
Country
China
ProdList
97
Advantage
65
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
94838
Advantage
76
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View Lastest Price from Linaclotide manufacturers

Sinoway Industrial co., ltd.
Product
Linaclotide 851199-59-2
Price
US $0.00/Kg/Bag
Min. Order
2Kg/Bag
Purity
98% up
Supply Ability
20 tons
Release date
2022-08-24
ANHUI SHENGZHIKAI BIOTECHNOLOGY CO.,LTD
Product
Linaelotide Acetate 851199-59-2
Price
US $1.00-1.00/mg
Min. Order
1mg
Purity
99%
Supply Ability
20g/week
Release date
2023-11-20
Zibo Hangyu Biotechnology Development Co., Ltd
Product
Linaclotide 851199-59-2
Price
US $55.00-550.00/kg
Min. Order
10kg
Purity
0.99
Supply Ability
20tons
Release date
2023-11-27

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  • Linacllotide
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  • Rinalodipine Acetate
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  • Linaclotide/Linaelotide Acetate
  • 851199-59-2
  • C59H79N15O21S6
  • C59H78N16O22S6
  • Inhibitors
  • 851199-59-2