| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
5-HT3 Receptor
|
|---|---|
| ln Vitro |
Ramosetron (1 μM) inhibits 5-HT3 receptor-dependent 5-HT release in guinea pig colonic mucosa [3].
|
| ln Vivo |
Ramosetron (0.01-0.1 mg/kg, orally, twice daily for 5 days) alleviates 5-fluorouracil (5-FU)-induced intestinal mucositis in C57BL/6 mice [2].
|
| References | |
| Additional Infomation |
Lamosetron belongs to the indole class of drugs. Lamosetron is a 5-HT3 receptor antagonist commonly used to treat nausea, vomiting, and certain diarrheal conditions. It is believed to be more potent than other first-generation 5-HT3 receptor antagonists (such as ondansetron) and has a longer-lasting antiemetic effect. Currently, lamosetron is only approved for use in Japan and some Southeast Asian countries. Lamosetron is a selective 5-HT3 receptor antagonist with potential antiemetic activity. After administration, lamosetron selectively binds to and blocks the activity of 5-HT3 receptors located at the vagal nerve endings and the vomiting center in the central nervous system (CNS), thereby inhibiting chemotherapy-induced nausea and vomiting. See also: Ondansetron hydrochloride (related drugs). Lamosetron hydrochloride (active fraction).
Drug Indication It is used to treat irritable bowel syndrome in men, characterized by nausea, vomiting, and diarrhea. |
| Molecular Formula |
C17H17N3O
|
|---|---|
| Molecular Weight |
279.34
|
| Exact Mass |
279.137
|
| CAS # |
132036-88-5
|
| PubChem CID |
108000
|
| Appearance |
Typically exists as solids at room temperature
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
579.7±50.0 °C at 760 mmHg
|
| Flash Point |
304.4±30.1 °C
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
| Index of Refraction |
1.708
|
| LogP |
1.99
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
21
|
| Complexity |
413
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CN1C2C(=CC=CC=2)C(C(C2CC3NC=NC=3CC2)=O)=C1
|
| InChi Key |
NTHPAPBPFQJABD-LLVKDONJSA-N
|
| InChi Code |
InChI=1S/C17H17N3O/c1-20-9-13(12-4-2-3-5-16(12)20)17(21)11-6-7-14-15(8-11)19-10-18-14/h2-5,9-11H,6-8H2,1H3,(H,18,19)/t11-/m1/s1
|
| Chemical Name |
(1-methylindol-3-yl)-[(5R)-4,5,6,7-tetrahydro-3H-benzimidazol-5-yl]methanone
|
| Synonyms |
YM060 free base
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 3.5799 mL | 17.8993 mL | 35.7987 mL | |
| 5 mM | 0.7160 mL | 3.5799 mL | 7.1597 mL | |
| 10 mM | 0.3580 mL | 1.7899 mL | 3.5799 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.
Link: https://clinicaltrials.gov/ct2/show/NCT02612649
Conditions:Diarrhea-predominant Irritable Bowel SyndromeLink: https://clinicaltrials.gov/ct2/show/NCT06166615
Conditions:Fecal IncontinenceLink: https://clinicaltrials.gov/ct2/show/NCT05577845
Conditions:LARS - Low Anterior Resection Syndrome
Title:Ramosetron OD Tablet and Postdischarge Nausea and Vomiting
Status:Unknown status
updateDate:2021-12-22
Ctid:NCT04297293
Link: https://clinicaltrials.gov/ct2/show/NCT04297293
Conditions:Day SurgeryLink: https://clinicaltrials.gov/ct2/show/NCT03232125
Conditions:Prostate CancerLink: https://clinicaltrials.gov/ct2/show/NCT02625181
Conditions:Postoperative Nausea and VomitingLink: https://clinicaltrials.gov/ct2/show/NCT03017222
Conditions:Abdominal MassLink: https://clinicaltrials.gov/ct2/show/NCT03409835
Conditions:HysteroscopyLink: https://clinicaltrials.gov/ct2/show/NCT03278522
Conditions:PONV|Prolonged QTc IntervalLink: https://clinicaltrials.gov/ct2/show/NCT02480088
Conditions:Postoperative Nausea and VomitingLink: https://clinicaltrials.gov/ct2/show/NCT02597907
Conditions:Postoperative Nausea and VomitingLink: https://clinicaltrials.gov/ct2/show/NCT00272285
Conditions:Vomiting|NauseaLink: https://clinicaltrials.gov/ct2/show/NCT02849483
Conditions:Postoperative Nausea and VomitingLink: https://clinicaltrials.gov/ct2/show/NCT02869984
Conditions:Anterior Resection SyndromeLink: https://clinicaltrials.gov/ct2/show/NCT02830906
Conditions:Postoperative Nausea and VomitingLink: https://clinicaltrials.gov/ct2/show/NCT01806948
Conditions:Postoperative Nausea and VomitingLink: https://clinicaltrials.gov/ct2/show/NCT02416115
Conditions:Postoperative Nausea and VomitingLink: https://clinicaltrials.gov/ct2/show/NCT02617121
Conditions:Postoperative Nausea and VomitingLink: https://clinicaltrials.gov/ct2/show/NCT02139241
Conditions:Coronary Artery Bypass Graft Triple Vessel|HypotensionLink: https://clinicaltrials.gov/ct2/show/NCT02604797
Conditions:C.Delivery; Surgery (Previous), GynecologicalLink: https://clinicaltrials.gov/ct2/show/NCT00918411
Conditions:Irritable Bowel SyndromeLink: https://clinicaltrials.gov/ct2/show/NCT02444897
Conditions:Gastric CancerLink: https://clinicaltrials.gov/ct2/show/NCT01637545
Conditions:Facial Bones FractureLink: https://clinicaltrials.gov/ct2/show/NCT01788605
Conditions:Hematologic MalignanciesLink: https://clinicaltrials.gov/ct2/show/NCT01225237
Conditions:Irritable Bowel SyndromeLink: https://clinicaltrials.gov/ct2/show/NCT02076529
Conditions:Colon CancerLink: https://clinicaltrials.gov/ct2/show/NCT01825733
Conditions:Postoperative Nausea and VomitingLink: https://clinicaltrials.gov/ct2/show/NCT02011659
Conditions:Uterine Myoma, Ovary Neoplasm, AdenomyosisLink: https://clinicaltrials.gov/ct2/show/NCT01536691
Conditions:Cancer|MalignancyLink: https://clinicaltrials.gov/ct2/show/NCT01669213
Conditions:Hypotension|Shivering|Nausea and Vomiting|VasopressorLink: https://clinicaltrials.gov/ct2/show/NCT01102491
Conditions:Osteoarthritis, KneeLink: https://clinicaltrials.gov/ct2/show/NCT01476280
Conditions:Postoperative Nausea and VomitingLink: https://clinicaltrials.gov/ct2/show/NCT01169805
Conditions:Laparoscopic Marsupialization of Renal CystLink: https://clinicaltrials.gov/ct2/show/NCT01427127
Conditions:Postoperative Nausea and VomitingLink: https://clinicaltrials.gov/ct2/show/NCT00971399
Conditions:Radiotherapy Induced Nausea and VomitingLink: https://clinicaltrials.gov/ct2/show/NCT01041183
Conditions:Nausea|Vomiting|Laparoscopic CholecystectomyProducts are for research use only; We do not sell to patients
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