| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
5-HT3 receptor ( Ki = 0.091 nM )
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|---|---|
| ln Vitro |
Ramosetron Hydrochloride (YM-060) has very low afinity for nicotinic and GABA receptors. YM060 also exhibits low affinity for histamine H1 and H2 receptors, alpha-1, atpha-2, beta-1, beta-2, and 5-HT1-like and 5-HT2 receptors, according to in vitro research. Anticipated 5-HT4 receptor blocking activity of YM-060 is negative[2].
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| ln Vivo |
Ramosetron has been shown to potently inhibit abnormal defecation in animals that is caused by stress. Ramosetron has potent, rapid-onset, and long-lasting inhibitory effects on rats' CFS-induced defecation, but has no effect on regular defecation. Ramosetron's inhibitory effect started to take effect right away after dosage and persisted for several hours[1].
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| Animal Protocol |
Sprague-Dawley rats
0.01, 0.03, 0.1 mg/kg oral For the CFS-induced defecation model, male Sprague-Dawley rats were used. Rats were conditioned with electric shocks (max 2 mA, 5 s/min, 15 times) accompanied by a warning beep and illumination. About 24 hours later, CFS was evoked by re-exposing the rats to the same chamber for 30 minutes with the warning beep and illumination but without electric shock. Test compounds were administered orally 1 hour before CFS initiation. For time-course studies, compounds were administered orally at 10 min, 1, 4, 8, and 12 h before CFS. Ramosetron hydrochloride was dissolved in distilled water and then diluted with 0.5% (w/v) methylcellulose (MC) solution. The dosing volume was not specified, but all oral administrations were performed [1]. For the normal defecation study, rats without fasting were housed individually immediately after oral administration of test compounds during 21:30 - 22:30. Feces were collected 12 and 24 hours after administration to measure total stool weights [1]. |
| References | |
| Additional Infomation |
Ramosetron hydrochloride belongs to the indole class of drugs. Ramosetron hydrochloride is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity. After administration, ramosetron selectively binds to and blocks the activity of 5-HT3 receptors located at vagal nerve endings and the vomiting center in the central nervous system (CNS), thereby inhibiting chemotherapy-induced nausea and vomiting.
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| Molecular Formula |
C17H18CLN3O
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|---|---|
| Molecular Weight |
315.801
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| Exact Mass |
315.113
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| Elemental Analysis |
C, 64.66; H, 5.75; Cl, 11.23; N, 13.31; O, 5.07
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| CAS # |
132907-72-3
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| Related CAS # |
132907-72-3 (HCl); 132036-88-5
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| PubChem CID |
107999
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| Appearance |
White to off-white solid powder
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| Boiling Point |
579.7ºC at 760mmHg
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| Melting Point |
244-246°C
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| Flash Point |
304.4ºC
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| Vapour Pressure |
1.96E-13mmHg at 25°C
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| LogP |
3.691
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
413
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| Defined Atom Stereocenter Count |
1
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| SMILES |
Cl[H].O=C(C1=C([H])N(C([H])([H])[H])C2=C([H])C([H])=C([H])C([H])=C12)[C@@]1([H])C([H])([H])C2=C(C([H])([H])C1([H])[H])N=C([H])N2[H]
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| InChi Key |
XIXYTCLDXQRHJO-RFVHGSKJSA-N
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| InChi Code |
InChI=1S/C17H17N3O.ClH/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);1H/t11-;/m1./s1
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| Chemical Name |
(1-methylindol-3-yl)-[(5R)-4,5,6,7-tetrahydro-3H-benzimidazol-5-yl]methanone;hydrochloride
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| Synonyms |
YM-060; YM 060; YM060; Ramosetron hydrochloride; Ramosetron HCl
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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: 32~63 mg/mL (101.3~199.5 mM)
Water: ~63 mg/mL Ethanol: ~1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (79.16 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1666 mL | 15.8328 mL | 31.6656 mL | |
| 5 mM | 0.6333 mL | 3.1666 mL | 6.3331 mL | |
| 10 mM | 0.3167 mL | 1.5833 mL | 3.1666 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 |
| NCT06166615 | Not yet recruiting | Drug: Ramosetron Drug: Psyllium |
Fecal Incontinence | Seoul National University Hospital | December 15, 2023 | Phase 2 Phase 3 |
| NCT05577845 | Recruiting | Drug: Ramosetron | LARS - Low Anterior Resection Syndrome |
Seoul National University Hospital |
March 27, 2023 | Not Applicable |
| NCT03278522 | Completed | Drug: Ramosetron | PONV Prolonged QTc Interval |
Konkuk University Medical Center | July 1, 2017 | Phase 4 |
| NCT02076529 | Completed | Drug: Ramosetron 0.3mg Drug: Ramosetron 0.45mg Drug: Ramosetron 0.6mg |
Colon Cancer | Chonnam National University Hospital |
October 2012 | Not Applicable |
| NCT01392794 | Completed | Drug: YM060 | Healthy Plasma Concentration of YM060 |
Astellas Pharma Inc | April 2011 | Phase 1 |
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