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Linaclotide - CAS 851199-59-2

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Category
Inhibitor
Product Name
Linaclotide
Catalog Number
851199-59-2
Synonyms
Linzess; Constella; 11: PN: WO2008151257 SEQID: 55 claimed protein; 13: PN: WO2008151257 SEQID: 57 claimed protein; 18: PN: WO2015054500 SEQID: 72 claimed protein; 1: PN: WO2014131024 SEQID: 55 claimed protein; 1: PN: WO2015054500 SEQID: 55 claimed protein; 2074: PN: US20090062207 SEQID: 3 claimed protein; 3: PN: WO2015054500 SEQID: 57 claimed protein; 40: PN: WO2010065751 SEQID: 55 claimed protein; 42: PN: WO2010065751 SEQID: 57 claimed protein; 55: PN: US20100152118 SEQID: 55 claimed protein; 55: PN: WO2011069038 SEQID: 55 claimed sequence; 55: PN: WO2012037380 SEQID: 55 unclaimed protein; 55: PN: WO2015054649 SEQID: 55 claimed protein; 57: PN: WO2011069038 SEQID: 57 claimed sequence; 57: PN: WO2012037380 SEQID: 57 claimed protein; 7: PN: WO2015054500 SEQID: 61 claimed protein
CAS Number
851199-59-2
Description
Linaclotide is a peptide agonist of guanylate cyclase 2C that is undergoing clinical trials for use in treating abdominal pain in patients with irritable bowel syndrome (IBS) accompanied by constipation. The drug also has promising outlooks for the treatment of gastroparesis, ulcerative colitis, chronic intestinal pseudo-obstruction (CIPO), and inertia coli as well.
Molecular Weight
1526.74
Molecular Formula
C59H79N15O21S6
Quantity
Grams-Kilos
Quality Standard
In-house Standard
COA
Certificate of Analysis-Linaclotide 851199-59-2 B15LNCT0907  
MSDS
Inquire
Canonical SMILES
O=C(O)[C@@H](NC(=O)[C@H]4NC(=O)CNC(=O)[C@@H](NC(=O)[C@H]2NC(=O)[C@@H](NC(=O)[C@H]5N(C(=O)[C@@H](NC(=O)[C@H]1NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)CSSC1)CSSC2)CCC(=O)O)Cc3ccc(O)cc3)CSSC4)CC(=O)N)CCC5)C)[C@H](O)C)Cc6ccc(O)cc6
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-WDRJZQOASA-N
Targets
Guanylate Cyclase
Size Price Stock Quantity
50 mg $698 In stock
100 mg $998 In stock

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Structure
CAS 851199-59-2 Linaclotide
Specification
Purity
≥ 98.0%
Boiling Point
2045.0±65.0 °C | Condition: Press: 760 Torr
Melting Point
231-235°C
Density
1.60 g/cm3
Appearance
White Solid
Application
For research used only
Storage
Refrigerator
Solubility
DMSO (Slightly, Heated), Methanol ((Slightly, Heated)), Water (Slightly, Heated)
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Reference Reading
1.Cost-effectiveness of linaclotide compared to antidepressants in the treatment of irritable bowel syndrome with constipation in Scotland
Mark Fisher • Andrew Walker • Meritxell Falques. Eur J Health Econ
Linaclotide is indicated as a continuous treatment provided the patient does not discontinue due to lack of efficacy or adverse events. Clinical efficacy data were available up to 26 weeks based upon the phase III clinical trials and therefore required extrapolation for the purposes of the cost-effectiveness model. In order to capture the important differences in costs and outcomes for IBS-C treatment, with moderate data extrapolation, a 5-year time horizon was chosen. The impact of alternative time horizons was tested in sensitivity analyses, which considered shorter (1-year, and within trial) and longer (10-year) time horizons. A 4-week cycle length was chosen for consistency with monitoring requirements in the product label. Costs and health benefits were discounted at an annual rate of 3.5 % and a halfcycle correction was implemented within the model. The model structure and assumptions were validated with Scottish experts.
2.Recent Advances in the Management of Difficult Constipation
Brian E. Lacy & John Levenick & Michael Crowell. Curr Gastroenterol Rep (2012) 14:306–312
Linaclotide is a 14-amino acid peptide that stimulates intestinal guanylate cyclase type-C (GC-C) receptors (see Fig. 1;). Linaclotide is acid stable and protease resistant with low bioavailability; it is undetectable in the systemic circulation at therapeutic doses. Activation of GC-C stimulates the production of cyclic guanosine monophosphate (cGMP) from guanosine triphosphate (GTP), which then increases the flow of electrolytes (HCO3- and Cl-) and water into the lumen of the GI tract (see Fig. 1). This is associated with faster GI transit. Stimulation of the GC-C receptor on intestinal epithelial cells and release of cGMP into the serosa leads to a reduction in visceral hyperalgesia.
3.New Options in Constipation Management
Mellar Davis & Pamela Gamier. Curr Oncol Rep (2015) 17: 55
Linaclotide is a first-in-class minimally adsorbed 14-aminoacid peptide agonist of guanylate cyclase C drug that acts on the intestinal enterocyte. The result is stimulation of chloride channels (CIC-2) and increase secretion of fluid into the gut lumen (Fig. 1). It is presently licensed for CIC and IBS-C in the USA. Oral bioavailability is 0.1 %, and less than 1 % is excreted in the stool in the first 24 h. Linaclotide undergoes proteolysis within the GI tract. However, it is resistant to pepsin, trypsin, aminopeptidases, and chymotrypsin proteolysis and thus is able to bind to duodenal and jejunal chloride channels. Linaclotide is converted to an active metabolite (MM-419447) which has the same pharmacodynamics and pharmacokinetics as the parent drug. Besides increasing luminal fluid, linaclotide also increases GI transit and reduces visceral hypersensitivity.
4.Linaclotide, Novel Therapy for the Treatment of Chronic Idiopathic Constipation and Constipation-Predominant Irritable Bowel Syndrome
Maria I. Vazquez-Roque · Ernest P. Bouras. Adv Ther (2013) 30(3):203–11.
A randomized, double-blind, placebocontrolled efficacy trial of linaclotide was conducted to evaluate its safety in 42 patients with CC. Patients were randomized to receive 100, 300, or 1,000 μg of linaclotide or placebo once daily for 14 days. Rebound constipation was assessed in an 8-day posttreatment period. Efficacy parameters were daily bowel movements using weekly rates of spontaneous bowel movements (SBM), complete SBM (CSBM), stool consistency, straining, and complete evacuation. At all doses studied, linaclotide produced an increase in SBM and CSBM compared to the placebo.
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