| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Compound 48/80 triHCl targets mast cells, triggering degranulation and histamine release. It activates G-protein-coupled receptors, particularly MRGPRX2, triggering allergic and inflammatory responses. The compound acts at the mast cell membrane to stimulate trimeric G-proteins and induces degranulation via phospholipase C and D. It also inhibits the activity of phosphatidylinositol-specific phospholipase C in human platelets. Its mechanism makes it a valuable tool for studying mast cell function and allergic responses.
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| ln Vitro |
Compound 48/80 trihydrochloride, also known as C48/80 trihydrochloride, exhibits a comparable level of efficacy in inhibiting phosphatidylphospholipidase C activity in the cytosol; its IC50 values are 2.1 μg/mL for the supernatant and 5.0 μg/mL for the granular compound. Additionally, it has been observed that C48/80 trihydrochloride inhibits human focal aggregation induced by ADP and PAF ether [1].
Compound 48/80 triHCl exhibits in vitro activity as a mast cell degranulator and histamine releaser. It causes histamine degranulation from mast cells. The compound inhibits the activity of phosphatidylinositol-specific phospholipase C in human platelets. It activates G-protein-coupled receptors, particularly MRGPRX2, triggering allergic and inflammatory responses. These in vitro activities confirm its utility as a tool for studying mast cell biology and allergic inflammation. |
| ln Vivo |
Serotonin, histamine, and corticosterone levels are increased by compound 48/80 trihydrochloride (0.75 mg/kg; intraperitoneal; killed after 0.5, 3, or 6 h); however, the amount of these increases decreases after 0.5 h [3]. Compound 48/80 trihydrochloride induces redox through mast cell degranulation [3].
Compound 48/80 triHCl is used in vivo as a mast cell activator in animal and tissue models. It is widely used as a “selective” mast cell activator to study allergic and inflammatory responses. The compound induces histamine release and degranulation in vivo, providing a model for studying mast cell-mediated diseases. Its effects are dose-dependent and mediated through activation of G-protein-coupled receptors. |
| Enzyme Assay |
In vitro assays for Compound 48/80 triHCl involve measuring mast cell degranulation and histamine release. Mast cells are cultured and treated with varying concentrations of the compound. Histamine release is measured by ELISA or other analytical methods. Degranulation is assessed by measuring the release of β-hexosaminidase or other granule contents. These assays confirm the compound’s activity as a mast cell degranulator.
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| Cell Assay |
In vitro cellular assays for Compound 48/80 triHCl are conducted in mast cell cultures. Cells are treated with the compound at various concentrations, and degranulation is assessed by measuring histamine release or β-hexosaminidase activity. Calcium flux is measured to assess G-protein activation. Platelet phospholipase C activity is measured in platelet preparations. These assays characterize the compound’s cellular effects.
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| Animal Protocol |
Animal/Disease Models: 7weeks old Wistar male rats (fasted for 24 hrs (hrs (hours))) [3]
Doses: 0.75 mg/kg]. Route of Administration: intraperitoneal (ip) injection; sacrificed after 0.5, 3 or 6 hrs (hrs (hours)). Experimental Results: 0.5 hrs (hrs (hours)) after treatment, serum histamine and serotonin concentrations were Dramatically higher than untreated control rats. Serum histamine and serotonin concentrations increased in rats and subsequently diminished in a time-dependent manner. In vivo animal experiments with Compound 48/80 triHCl are conducted in rodent models of allergic inflammation. The compound is administered via injection, and mast cell degranulation and histamine release are assessed in tissues. Endpoints include vascular permeability, edema, and inflammatory cell infiltration. These studies evaluate the compound’s effects on mast cell-mediated responses in vivo. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for Compound 48/80 triHCl are limited, as the compound is primarily used as a research tool. The compound has a molecular weight of 629.10 and is soluble in DMSO. Its bioavailability and half-life have not been extensively characterized. The compound is typically stored at -20°C.
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| Toxicity/Toxicokinetics |
Compound 48/80 triHCl is considered to have low toxicity based on its use as a research compound. However, comprehensive toxicological evaluations have not been extensively published. The compound is intended for research use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
Compound 48/80 triHCl is a potent mast cell degranulator and histamine releaser. It is also known as C48/80 trihydrochloride. The compound activates G-protein-coupled receptors, particularly MRGPRX2, triggering allergic and inflammatory responses. It inhibits phosphatidylinositol-specific phospholipase C in human platelets. Compound 48/80 triHCl is widely used in animal and tissue models as a mast cell activator. It is available in high purity for research applications.
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| Molecular Formula |
C32H48CL3N3O3
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| Molecular Weight |
629.100826263428
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| Exact Mass |
627.276
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| CAS # |
848035-21-2
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| Related CAS # |
Compound 48/80;94724-12-6
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| PubChem CID |
118797323
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
41
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| Complexity |
577
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.Cl.Cl.O(C)C1C(=CC(CCNC)=CC=1CC1C(=CC=C(CCNC)C=1)OC)CC1C(=CC=C(CCNC)C=1)OC
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| InChi Key |
KIAWAQJORBNOIF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H45N3O3.3ClH/c1-33-14-11-23-7-9-30(36-4)26(17-23)21-28-19-25(13-16-35-3)20-29(32(28)38-6)22-27-18-24(12-15-34-2)8-10-31(27)37-5;;;/h7-10,17-20,33-35H,11-16,21-22H2,1-6H3;3*1H
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| Chemical Name |
2-[4-methoxy-3-[[2-methoxy-3-[[2-methoxy-5-[2-(methylamino)ethyl]phenyl]methyl]-5-[2-(methylamino)ethyl]phenyl]methyl]phenyl]-N-methylethanamine;trihydrochloride
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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) |
H2O : ~25 mg/mL (~39.74 mM)
DMSO : ~10 mg/mL (~15.90 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.97 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 (3.97 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5896 mL | 7.9479 mL | 15.8957 mL | |
| 5 mM | 0.3179 mL | 1.5896 mL | 3.1791 mL | |
| 10 mM | 0.1590 mL | 0.7948 mL | 1.5896 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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