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| 50mg |
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| 100mg |
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Tegaserod maleate (HTF-919; SDZ-HTF-919) is an oral and potent 5-HT4 agonist that can activate serotonin receptor 4 (HTR4; 5-HT4R) and inhibit 5-HT2B receptor. It exhibits antitumor and anti-IBS/irritable bowel syndrome activity.
| ln Vitro |
Cells significantly increase in response to teserod maleate (SDZ-HTF-919; 3-5 μM; 24-72 hours) in both time and dose [1]. p-S6 and p-p70 S6 (Thr421/Ser424) are reduced by tesazerod maleate (0.1-3 μM; 8–18 hours)[1]. Within 24 hours, Tegaserod maleate (0.1-3 μM) efficiently suppresses 5-HT-mediated
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| ln Vivo |
Tegaserod maleate (SDZ-HTF-919; intraperitoneal injection; 5 mg/kg/day; five consecutive days) suppresses p-S6 in vivo and delays, shrinks, and grows tumors[1]. The rate of gastric emptying in db/db mice was dramatically increased by tegaserod lecithin (0.1-2.0 mg/kg; intraperitoneally administered 15 minutes before gastric burden), reducing the time to 30 minutes at 0.1 mg/kg. This resulted in an 80% reduction in the portion of the meal in the stomach [2].
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| Cell Assay |
apoptosis analysis [1]
Cell Types: A375, RPMI-7951 (RPMI), SH4, B16F10, MeWo and MEL-JUSO Tested Concentrations: 3, 5 μM Incubation Duration: 24, 48, 72 hrs (hours) Experimental Results: Significant time- and dose-dependent increase in apoptosis in all cell lines. Western Blot Analysis [1] Cell Types: RPMI, SH4 and B16F10 Cell Tested Concentrations: 3, 5 μM Incubation Duration: 8 or 18 hrs (hours) Experimental Results: diminished phosphorylation of kinases at Thr421/Ser424 upstream of S6, p70 S6. |
| Animal Protocol |
Animal/Disease Models: C57BL/6 J mice were injected subcutaneously (sc) (sc) with B16F10 cells [1].
Doses: 5 mg/kg. Route of Administration: intraperitonealadministration every day for five days. Experimental Results: The treatment Dramatically diminished tumor growth, and the body weight was only slightly There was a decline after treatment. Animal/Disease Models: Female C57BLKS/J db/db mice [2] Doses: 0.1, 0.5, 1.0, 2.0 mg/kg Route of Administration: IP; 15 minutes before gastric loading Experimental Results: Doses as low as 0.1 mg/kg (0.1 mg /kg), the proportion of meal remaining in the stomach was Dramatically diminished. Accelerates gastric emptying, with the remainder diminished by nearly 80% (P < 0.0001) at 30 minutes (0.1 mg/kg). The gastric emptying rate was Dramatically diminished due to a significant increase in the amount of meal remaining at 30 minutes (2.0 mg/kg). Causes inhibition of tegaserod-induced increase in gastric emptying (0.1 mg/kg). |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation No information is available on the clinical use of tegaserod during breastfeeding. Because of the potential for serious adverse reactions in the breastfed infant, an alternate drug is preferred. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References |
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| Additional Infomation |
See also: Tegaserod (has active moiety).
Drug Indication Zelnorm is indicated for the repeated symptomatic short-term treatment of women with Irritable Bowel Syndrome (IBS) whose predominant bowel habit is constipation, associated with abdominal pain/discomfort or bloating (see section 4. 2). |
| Molecular Formula |
C20H27N5O5
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|---|---|
| Molecular Weight |
417.466
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| Exact Mass |
417.201
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| CAS # |
189188-57-6
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| Related CAS # |
Tegaserod;145158-71-0;Tegaserod-13C,d3 maleate
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| PubChem CID |
135413539
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| Appearance |
Light yellow to yellow solid powder
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| Boiling Point |
661.4ºC at 760 mmHg
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| Melting Point |
180-183ºC
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| Flash Point |
353.8ºC
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| Vapour Pressure |
2.15E-18mmHg at 25°C
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| LogP |
3.101
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
30
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| Complexity |
504
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCN=C(N)N/N=C/C1=CNC2=C1C=C(C=C2)OC.C(=C\C(=O)O)\C(=O)O
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| InChi Key |
CPDDZSSEAVLMRY-FEQFWAPWSA-N
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| InChi Code |
InChI=1S/C16H23N5O.C4H4O4/c1-3-4-5-8-18-16(17)21-20-11-12-10-19-15-7-6-13(22-2)9-14(12)155-3(6)1-2-4(7)8/h6-7,9-11,19H,3-5,8H2,1-2H3,(H3,17,18,21)1-2H,(H,5,6)(H,7,8)/b20-11+2-1-
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| Chemical Name |
(E)-2-((5-methoxy-1H-indol-3-yl)methylene)-N-pentylhydrazine-1-carboximidamide maleate
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| Synonyms |
Zelnorm ZelmacSDZ-HTF-919 SDZHTF-919SDZ-HTF919 HTF919 HTF-919 SDZ-HTF 919 SDZ HTF-919HTF 919 Tegaserod
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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. |
| 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) |
DMSO : ≥ 35 mg/mL (~83.84 mM)
H2O : ~1 mg/mL (~2.40 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3954 mL | 11.9769 mL | 23.9538 mL | |
| 5 mM | 0.4791 mL | 2.3954 mL | 4.7908 mL | |
| 10 mM | 0.2395 mL | 1.1977 mL | 2.3954 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 |
| NCT00511771 | NO LONGER AVAILABLE | Drug: Tegaserod | Chronic Idiopathic Constipation Irritable Bowel Syndrome With Constipation |
Novartis |
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