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| 10mg | ||
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| 100mg |
Purity: ≥98%
Dolcanatide (formerly SP-333; SP333; SP 333) is the second uroguanylin analog currently being developed for ulcerative colitis by Synergy Pharmaceuticals which is a biopharmaceutical company focused on the development and commercialization of novel gastrointestinal (GI) therapies. Analogs of uroguanylin, a naturally occurring human GI peptide, have the potential for the treatment of functional GI disorders and inflammatory bowel disease. Plecanatide (Trade name Trulance; formerly SP-304), a 16 amino acid peptide, is a drug approved by the FDA for the treatment of chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation. Plecanatide is an agonist of guanylate cyclase-C. It works as a laxative by drawing water into the gastrointestinal tract thereby softening stool and encouraging its natural passage. Plecanatide increases intestinal transit and fluid through a buildup of cGMP. As of January 2017, Plecanatide is approved in the United States for the treatment of chronic idiopathic constipation in adults. As of January 2017, Plecanatide is approved in the United States for the treatment of chronic idiopathic constipation in adults.
| ln Vitro |
In T84 cells, dolcanatide (0-10 μM; 30 minutes) increases cGMP production and GC-C receptors in a dose-dependent manner [2]. In Caco-2 and T84 cells, lipopolysaccharide-induced paracellular permeability is inhibited by dolcanatide (1 μM; 16 hours) [1].
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| ln Vivo |
Oral dolcanatide (0.01 and 0.05 mg/kg; once) decreases rectal allodynia in rats induced by TNBS [1]. Oral dolcanatide (0.01 and 0.05 mg/kg; once) decreases colorectal hypersensitivity (CRD) in rats induced by stress [1].
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| Cell Assay |
Cell viability assay [2]
Cell Types: T84 Cell Tested Concentrations: 0-10 μM Incubation Duration: 30 minutes Experimental Results: Shows EC50 value of 0.28 μM. |
| Animal Protocol |
Animal/Disease Models: TNBS-induced rectal allodynia in rats [1]
Doses: 0.01 and 0.05 mg/kg Route of Administration: oral; Route of Administration: oral. 0.01 and 0.05 mg/kg; Experimental Results:Attenuated the increased number of abdominal contractions caused by TNBS (inflation pressure up to 60 mmHg). Animal/Disease Models: Wistar rat stress visceral hypersensitivity [1] Doses: 0.01 and 0.05 mg/kg 0.01 and 0.05 mg/kg; Experimental Results: As CRD (colorectal distension) pressure increases, PRS (partial restraint stress) ) caused a significant reduction in abdominal contraction rate. |
| References |
[1]. Boulete IM, et al. Oral treatment with plecanatide or dolcanatide attenuates visceral hypersensitivity via activation of guanylate cyclase-C in rat models. World J Gastroenterol. 2018 May 7;24(17):1888-1900.
[2]. Shailubhai K, et al. Plecanatide and dolcanatide, novel guanylate cyclase-C agonists, ameliorate gastrointestinal inflammation in experimental models of murine colitis. World J Gastrointest Pharmacol Ther. 2015 Nov 6;6(4):213-22. |
| Molecular Formula |
C65H104N18O26S4
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| Molecular Weight |
1681.89
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| CAS # |
1092457-65-2
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| SMILES |
CC1C(=O)NC2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(CSSCC(NC(=O)CNC(=O)C(NC2=O)C(C)O)C(=O)NC(CC(C)C)C(=O)O)C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)C(C)C)CC(=O)N)C(C)C)CC(C )C)CCC(=O)O)NC(=O)C(CCC(=O)O)NC(=O)C(CC(=O)O)NC(=O)C(CC(=O)N)N |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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.
 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. |
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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. |
 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. |
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