YM348

Cat. No.: HY-100330 Purity: 99.15%: FAQs
Data Sheet SDS COA Handling Instructions

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YM348 is a potent and orally active 5-HT_2C receptor agonist, which shows a high affinity for cloned human 5-HT_2C receptor (K_i: 0.89 nM).

For research use only. We do not sell to patients.

YM348 Chemical Structure

CAS No. : 372163-84-3

Size	Price	Stock	Quantity
5 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 680	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1350	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2200	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3400	In-stock	Estimated Time of Arrival: December 31
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Biological Activity
Protocol
Purity & Documentation
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Description

YM348 is a potent and orally active 5-HT_2C receptor agonist, which shows a high affinity for cloned human 5-HT_2C receptor (K_i: 0.89 nM).

IC₅₀ & Target

Ki: 0.89±0.05 nM (5-HT_2C receptor), 2.5±0.5 nM (5-HT_2B receptor), 13±2 nM (5-HT_2A receptor)^[1]
EC50: 1.0±0.2 nM (5-HT_2C receptor), 3.2±3 (5-HT_2B receptor) , 93±10 nM (5-HT_2A receptor)^[1]

In Vitro

YM348 has high affinity for cloned human 5-HT_2C receptors with a K_i value of 0.89 nM and lower affinities for human-cloned 5-HT_2B (K_i: 2.5 nM) and 5-HT_2A receptors (K_i: 13 nM). To assess the binding specificity of YM348, a broad evaluation of an additional 46 binding sites including several other 5-HT receptor subtypes (1A, 1B, 1D, 3, 4, 5A, 6, 7) is performed. IC₅₀ values of YM348 are found to be >1 μM for all of the binding sites except for the human 5-HT_1A receptors (K_i: 130 nM), bovine 5-HT_1D receptors (K_i: 481 nM), human 5-HT₇ receptors (K_i: 177 nM), and human α_2A receptors (K_i: 126 nM).YM348 exhibits a full-agonistic activity on human 5-HT_2A and 5-HT_2B receptors. The EC₅₀ values of YM348 for 5-HT_2C, 5-HT_2A, and 5-HT_2B receptors are 1.0, 93 and 3.2 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Oral administration of YM348 induces penile erections and hypolocomotion in rats, being completely inhibited by a selective 5-HT_2C receptor antagonist, SB242084. YM348 inhibits spontaneous activity in a dose-dependent manner with a minimum effective dose of 0.203 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

243.30

Formula

C₁₄H₁₇N₃O

CAS No.

372163-84-3

Appearance

Oil

Color

Light yellow to brown

SMILES

C[C@H](N)CN(N=C1)C2=C1C=CC3=C2C=C(CC)O3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (411.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.1102 mL	20.5508 mL	41.1015 mL
5 mM	0.8220 mL	4.1102 mL	8.2203 mL
10 mM	0.4110 mL	2.0551 mL	4.1102 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.28 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (10.28 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.15%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (250 KB) HNMR (248 KB) RP-HPLC (263 KB) MS (140 KB)

Handling Instructions (2659 KB)

Kinase Assay
^[1]

Experiments are performed with membranes obtained from Chinese Hamster Ovary (CHO) cells expressing human 5-HT_2C or 5-HT_2A receptors and Human Embryonic Kidney 293-Epstein-Barr virus nuclear antigen (HEK293-EBNA) cells expressing human 5-HT_2B receptors. Binding assays with [³H] 5-HT are carried out. The reaction medium (50 mM Tris-HCl buffer (pH 7.4) containing 4 mM CaCl₂, 10 M pargyline and 0.1 mg/ml L-(+)-ascorbic acid) containing [³H] 5-HT, membrane preparation and test compounds are incubated at 37°C for 30 min. Nonspecific binding is determined in the presence of 10 M 5-HT, and specific binding is calculated as the total binding minus the nonspecific binding. After incubation, 4 mL of 50 mM Tris-HCl buffer (pH 7.4) containing 4 mM CaCl₂ is added, and the medium is filtrated under decompression through a Whatman GF/B glass filter pretreated with 0.1% polyethyleneimine. The filter is washed with the same buffer solution (4 mL×3). The glass filter is immersed in 6 mL of liquid scintillator (Packard, Aquasol-2), and the radioactivity is measured with a liquid scintillation counter. The amount of protein is measured. The dissociation constants (K_d values) are obtained by Scatchard analysis using SAS (ver. 6.11). The concentrations of compounds showing 50% inhibition of receptor binding, IC₅₀ values, are obtained by nonlinear analysis using SAS (ver. 6.11). The Ki values indicating affinity for receptors are calculated^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
^[1]

Rats^[1]
Male Wistar rats (215-350 g) are used. Rats are administered YM348 (0.0677, 0.203, 0.677, and 2.03 mg/kg) orally and moved again to their home cages. After 20 min, thereafter, the rats are individually placed in transparent acrylic plastic cages (35×30×18 cm), and their motor activity is measured for 40 min. The measurements are carried out using a SUPER-MEX sensor. SB242084 (0.1-3 mg/kg i.p.) is administered 30 min before YM348 treatment.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.1102 mL	20.5508 mL	41.1015 mL	102.7538 mL
	5 mM	0.8220 mL	4.1102 mL	8.2203 mL	20.5508 mL
	10 mM	0.4110 mL	2.0551 mL	4.1102 mL	10.2754 mL
	15 mM	0.2740 mL	1.3701 mL	2.7401 mL	6.8503 mL
	20 mM	0.2055 mL	1.0275 mL	2.0551 mL	5.1377 mL
	25 mM	0.1644 mL	0.8220 mL	1.6441 mL	4.1102 mL
	30 mM	0.1370 mL	0.6850 mL	1.3701 mL	3.4251 mL
	40 mM	0.1028 mL	0.5138 mL	1.0275 mL	2.5688 mL
	50 mM	0.0822 mL	0.4110 mL	0.8220 mL	2.0551 mL
	60 mM	0.0685 mL	0.3425 mL	0.6850 mL	1.7126 mL
	80 mM	0.0514 mL	0.2569 mL	0.5138 mL	1.2844 mL
	100 mM	0.0411 mL	0.2055 mL	0.4110 mL	1.0275 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YM348372163-84-3YM 348YM-348Inhibitorinhibitorinhibit

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