| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
5-HT4 Receptor
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|---|---|
| ln Vitro |
Tegaserod (3-5 μM; 24-72 hours) significantly increases apoptosis in a time- and dose-dependent manner [1]. Tegaserod lowers p-S6 and p-p70 S6 (Thr421/Ser424)[1] at 3-5 μM over 8–18 hours. According to 5-HT2B receptor antagonist activity, tegaserod (0.1-3 μM; 24 hours) efficiently suppresses 5-HT-mediated contraction of the rat gastric fundus in vitro (pA2=8.3) [3].
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| ln Vivo |
Tegaserod (5 mg/kg/day; intraperitoneal injection; five days in a row) inhibits p-S6 in vivo, decreases metastasis, and delays the formation of tumors [1]. Tegaserod (0.1-2.0 mg/kg; i.p. 15 min before gastric loading) dramatically increases the rate at which gastric glucose is emptied from the stomach in db/db mice and maintains it at 0.1 mg/kg for 30 minutes. This results in an 80% reduction in the amount of food consumed[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 h Experimental Results: There was a significant time and dose-dependent increase in apoptosis in all cell lines. Western Blot Analysis[1] Cell Types: RPMI, SH4 and B16F10 cells Tested Concentrations: 3, 5 μM Incubation Duration: 8 or 18 h Experimental Results: diminished phosphorylation of the kinase directly upstream of S6, p70 S6 at Thr421/Ser424. |
| Animal Protocol |
Animal/Disease Models: C57BL/6 J mice were subcutaneously (sc) injected with B16F10 cells[1]
Doses: 5 mg/ kg Route of Administration: Administered intraperitoneally (ip) (ip) daily for five days Experimental Results: Treatment Dramatically diminished tumor growth and resulted in only slight decreases in weight following 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 min prior to gastric loading Experimental Results: Produced a dramatic decrease in the fraction of the meal remaining in the stomach for doses as low as 0.1 mg/kg (0.1 mg/kg). Accelerated gastric emptying, with a reduction of nearly 80% in the fraction remaining at 30 min (P < 0.0001) (0.1 mg/kg). Induced a significant decrease in the gastric emptying rate as the amount of the meal remaining at 30 min was Dramatically greater (2.0 mg/kg). Resulted in inhibition of tegaserod-induced increased gastric emptying (0.1 mg/kg). |
| References |
[1]. Wei Liu, et al. Repurposing the serotonin agonist Tegaserod as an anticancer agent in melanoma: molecular mechanisms and clinical implications. J Exp Clin Cancer Res. 2020 Feb 21;39(1):38.
[2]. M D Crowell, et al. The effects of tegaserod, a 5-HT receptor agonist, on gastric emptying in a murine model of diabetes mellitus. Neurogastroenterol Motil. 2005 Oct;17(5):738-43. [3]. D T Beattie, et al. The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol. 2004 Nov;143(5):549-60. |
| Molecular Formula |
C16H23N5O
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|---|---|
| Molecular Weight |
301.39
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| CAS # |
145158-71-0
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| Related CAS # |
Tegaserod maleate;189188-57-6
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
COC1=CC2=C(NC=C2/C=N/NC(NCCCCC)=N)C=C1
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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 |
| 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 : ~50 mg/mL (~165.90 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (16.59 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 50.0 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: ≥ 5 mg/mL (16.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (16.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3180 mL | 16.5898 mL | 33.1796 mL | |
| 5 mM | 0.6636 mL | 3.3180 mL | 6.6359 mL | |
| 10 mM | 0.3318 mL | 1.6590 mL | 3.3180 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.
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