| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
YM348 exhibits a high affinity of 0.89 nM for the cloned human 5-HT2C receptor and a low affinity of 2.5 nM for the cloned human 5-HT2B and 13 nM for the cloned human 5-HT2A receptors. An thorough evaluation was conducted on 46 binding sites, which included various other 5-HT receptor subtypes (1A, 1B, 1D, 3, 4, 5A, 6, 7) in order to assess the binding specificity of YM348. The human 5-HT1A receptor (Ki: 130 nM), human 5-HT7 receptor (Ki: 177 nM), and bovine 5-HT1D receptor (Ki: 481 nM) are the exceptions. At human 5-HT2A and 5-HT2B receptors, YM348 demonstrates complete agonistic action. YM348's EC50 values for the 5-HT2C, 5-HT2A, and 5-HT2B receptors are, respectively, 1.0, 93, and 3.2 nM[1].
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| ln Vivo |
The selective 5-HT2C receptor antagonist SB242084 totally blocked the penile erection and hypokinesia that rats experienced after oral YM348 treatment. A minimum effective dose of 0.203 mg/kg is required for YM348 to reduce spontaneous activity in a dose-dependent manner [1].
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| References |
[1]. Kimura Y, et al. Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist. Eur J Pharmacol. 2004 Jan 1;483(1):37-43
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| Molecular Formula |
C14H17N3O
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|---|---|
| Molecular Weight |
243.31
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| Exact Mass |
243.137
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| CAS # |
372163-84-3
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| PubChem CID |
3045225
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.28g/cm3
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| Boiling Point |
395.2ºC at 760 mmHg
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| Flash Point |
192.8ºC
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| Index of Refraction |
1.652
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| LogP |
3.392
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
299
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@H](N)CN(N=C1)C2=C1C=CC3=C2C=C(CC)O3
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| InChi Key |
QLOOWOVVZLBYHU-VIFPVBQESA-N
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| InChi Code |
InChI=1S/C14H17N3O/c1-3-11-6-12-13(18-11)5-4-10-7-16-17(14(10)12)8-9(2)15/h4-7,9H,3,8,15H2,1-2H3/t9-/m0/s1
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| Chemical Name |
(2S)-1-(7-ethylfuro[2,3-g]indazol-1-yl)propan-2-amine
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| Synonyms |
YM 348 YM-348YM348
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~411.02 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.28 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 (10.28 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 | 4.1100 mL | 20.5499 mL | 41.0998 mL | |
| 5 mM | 0.8220 mL | 4.1100 mL | 8.2200 mL | |
| 10 mM | 0.4110 mL | 2.0550 mL | 4.1100 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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