| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
YM-344484 effectively inhibited CCR3 ligand-induced calcium ion influx in B300-19 cells expressing human CCR3, with a Kβ value ranging from 0.69 nM to 2.5 nM, depending on the ligand [1]. YM-344484 inhibited CCL11-induced calcium ion influx in cells expressing mouse CCR3, with a Kβ value of 88 nM [1]. YM-344484 inhibited histamine H1 receptor-mediated calcium ion influx in PC3 cells, with a Kβ value of 47 nM [1]. YM-344484 (10 μM) showed only weak inhibitory activity against 5-HT2A receptor-mediated calcium ion influx in C6 cells, with an inhibition rate of only 25% [1]. YM-344484 can effectively inhibit the chemotaxis induced by CCR3 ligand in human CCR3-expressing B300-19 cells, and its IC50 value varies depending on the ligand, ranging from 2.0 nM to 8.0 nM[1]. YM-344484 can inhibit the release of eosinophil-derived neurotoxins induced by CCL11 from human peripheral blood eosinophils, and its IC50 value is 19 nM[1].
|
|---|---|
| ln Vivo |
YM-344484 (3-30 mg/kg; orally; single dose) inhibited histamine-induced vascular permeability by 82% in mice with a single oral dose of 10 mg/kg, and completely inhibited it at a dose of 30 mg/kg [1]. In an ovalbumin-induced mouse asthma model, YM-344484 (100-600 mg/kg; orally; every 8 hours; 6 doses) inhibited eosinophil infiltration by 74% at a dose of 300 mg/kg, and completely inhibited it at a dose of 600 mg/kg [1].
|
| Animal Protocol |
Animal/Disease Models:Balb/c (female, 6 weeks old) [1]
Doses: 3 mg/kg; 10 mg/kg; 30 mg/kg Route of Administration: Oral; Single dose Experimental Results: Dose-dependent inhibition of histamine-induced vascular permeability. Statistically significant inhibition was achieved at 10 mg/kg (82%). Complete inhibition was achieved at 30 mg/kg. Animal/Disease Models:Balb/c (female) [1] Doses: 100 mg/kg; 300 mg/kg; 600 mg/kg Route of Administration: Oral; every 8 hours; 6 times Experimental Results: The 100 mg/kg dose failed to reduce eosinophil count. The 300 mg/kg dose significantly reduced eosinophil infiltration, with an inhibition rate of 74%. The 600 mg/kg dose achieved 100% inhibition of eosinophil infiltration. No inhibitory effect was observed on neutrophil or monocyte counts in bronchoalveolar lavage fluid. |
| References |
| Molecular Formula |
C28H30FN5O2
|
|---|---|
| Molecular Weight |
487.57
|
| CAS # |
671205-14-4
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
FC(C=C1)=CC(C=C2)=C1C=C2CN3C[C@@H](CC3)NC(/C=C4CCN(CC/4)C(C5=CC=C(N=N5)C)=O)=O
|
| 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 | 2.0510 mL | 10.2549 mL | 20.5099 mL | |
| 5 mM | 0.4102 mL | 2.0510 mL | 4.1020 mL | |
| 10 mM | 0.2051 mL | 1.0255 mL | 2.0510 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
