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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Purity: ≥98%
Plecanatide (Trade name Trulance; formerly SP304; SP-304), a 16 amino acid peptide and a synthetic analog of uroguanylin, is a drug approved by FDA for the treatment of chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation. Plecanatide functions as an agonist for GCC (guanylate cyclase-C). In order to soften and facilitate the natural passage of stool, it acts as a laxative by drawing water into the digestive system. Plecanatide promotes intestinal transit and fluid by cGMP accumulation. Plecanatide was licensed in the US as of January 2017 to treat adult patients with persistent idiopathic constipation. Plecanatide is now approved in the US for treating adult patients with chronic idiopathic constipation as of January 2017.
Targets |
guanylate cyclase-C ( EC50 = 190 nM )
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ln Vitro |
Plecanatide (1 nM-10 μM) stimulates the synthesis of cyclic guanosine monophosphate (cGMP) in a dose-dependent manner with an EC50 of 190 nM by activating the GC-C receptor[1].
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ln Vivo |
Plecanatide (0.5 and 2.5 mg/kg, p.o.) improves colitis that is chemically and spontaneously induced in BALB/c mice after 7 days of treatment, and in TCRα-/- mice, it takes 14 days[1].
Plecanatide (0.005–5 mg/kg, once daily for seven days) also exhibits anti-inflammatory properties in BDF-1 mice that have colitis induced by trinitrobenzene sulfonic (TNBS) and dextran sulfate sodium (DSS)[1]. |
Animal Protocol |
Female BALB/c mice (2-4 month old) are induced colitis by TNBS
0, 0.5 and 2.5 mg/kg P.o. for 7 days |
References |
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Molecular Formula |
C65H104N18O26S4
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Molecular Weight |
1681.89
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Exact Mass |
1680.63
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Elemental Analysis |
C, 46.42; H, 6.23; N, 14.99; O, 24.73; S, 7.62
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CAS # |
467426-54-6
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Related CAS # |
Plecanatide acetate; 1075732-84-1
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Appearance |
Solid powder
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SMILES |
C[C@H]1C(=O)N[C@H]2CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@H](NC(=O)CNC(=O)[C@@H](NC2=O)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)C(C)C)CC(=O)N)C(C)C)CC(C)C)CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N)N
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InChi Key |
NSPHQWLKCGGCQR-DLJDZFDSSA-N
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InChi Code |
InChI=1S/C65H104N18O26S4/c1-25(2)15-34-55(98)80-41-24-113-110-21-38(58(101)77-37(65(108)109)16-26(3)4)71-44(87)20-69-62(105)50(30(10)84)83-61(104)40(78-51(94)29(9)70-63(106)48(27(5)6)81-57(100)35(18-43(68)86)76-64(107)49(28(7)8)82-60(41)103)23-112-111-22-39(59(102)73-32(53(96)75-34)11-13-45(88)89)79-54(97)33(12-14-46(90)91)72-56(99)36(19-47(92)93)74-52(95)31(66)17-42(67)85/h25-41,48-50,84H,11-24,66H2,1-10H3,(H2,67,85)(H2,68,86)(H,69,105)(H,70,106)(H,71,87)(H,72,99)(H,73,102)(H,74,95)(H,75,96)(H,76,107)(H,77,101)(H,78,94)(H,79,97)(H,80,98)(H,81,100)(H,82,103)(H,83,104)(H,88,89)(H,90,91)(H,92,93)(H,108,109)/t29-,30+,31-,32-,33-,34-,35-,36-,37-,38-,39-,40-,41-,48-,49-,50-/m0/s1
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Chemical Name |
(2S)-2-[[(1R,4S,7S,10S,13S,16R,19S,22S,25R,32S,38R)-10-(2-amino-2-oxoethyl)-25-[[(2S)-4-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-2,4-diamino-4-oxobutanoyl]amino]propanoyl]amino]butanoyl]amino]-22-(2-carboxyethyl)-32-[(1R)-1-hydroxyethyl]-4-methyl-19-(2-methylpropyl)-3,6,9,12,15,18,21,24,30,33,36-undecaoxo-7,13-di(propan-2-yl)-27,28,40,41-tetrathia-2,5,8,11,14,17,20,23,31,34,37-undecazabicyclo[14.13.13]dotetracontane-38-carbonyl]amino]-4-methylpentanoic acid
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.5946 mL | 2.9728 mL | 5.9457 mL | |
5 mM | 0.1189 mL | 0.5946 mL | 1.1891 mL | |
10 mM | 0.0595 mL | 0.2973 mL | 0.5946 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05151328 | Active Recruiting |
Drug: Plecanatide | Functional Constipation | Shandong Luoxin Pharmaceutical Group Stock Co., Ltd. |
March 18, 2022 | Phase 3 |
NCT03596905 | Recruiting | Drug: Plecanatide Drug: Matching placebo |
Irritable Bowel Syndrome With Constipation |
Bausch Health Americas, Inc. | June 30, 2018 | Phase 2 |
NCT02706483 | Completed | Drug: Plecanatide | Irritable Bowel Syndrome | Bausch Health Americas, Inc. | January 2016 | Phase 3 |
NCT02122471 | Completed | Drug: Plecanatide Drug: Placebo |
Chronic Idiopathic Constipation | Bausch Health Americas, Inc. | April 2014 | Phase 3 |
NCT01982240 | Completed | Drug: Plecanatide Drug: Placebo |
Chronic Idiopathic Constipation | Bausch Health Americas, Inc. | November 2013 | Phase 3 |
Effect of plecanatide and dolcanatide on lipopolysaccharide-induced increase in permeability of 4 kDa fluorescein isothiocyanate-dextran across Caco-2 and T84 cell monolayers. Design and results of the TNBS-induced visceral hypersensitivity models.World J Gastroenterol. 2018 May 7; 24(17): 1888–1900. th> |
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Effect of plecanatide and dolcanatide on localization of occludin in epithelial cells. Effect of plecanatide (A) and dolcanatide (B) on lipopolysaccharide-induced increased permeability of 4 kD fluorescein isothiocyanate-dextran across rat colon tissues.World J Gastroenterol. 2018 May 7; 24(17): 1888–1900. td> |
Effect of plecanatide and dolcanatide on localization of ZO-1 in epithelial cells. Design and results of the partial restraint stress-induced visceral hypersensitivity models.World J Gastroenterol. 2018 May 7; 24(17): 1888–1900. td> |