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Compound 48/80 (hydrochloride) (Synonyms: C48/80 trihydrochloride)

Katalog-Nr.GC43305

Compound 48/80 (Hydrochlorid) (C48/80 Trihydrochlorid) ist eine Mischung aus Kondensationsprodukten von N-Methyl-p-methoxyphenethylamin mit Formaldehyd.

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Compound 48/80 (hydrochloride) Chemische Struktur

Cas No.: 848035-21-2

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Bone-Marrow Derived Mast Cells

Preparation Method

Bone-Marrow Derived Mast Cells were stimulated with LPS (1 µg/ml) for 24 h and subsequently incubated with or without treatment of Compound 48/80 (50 µg/ml) for 5 min. Cells and culture supernatants were collected for the further analysis.

Reaction Conditions

Compound 48/80 (50 µg/ml);5min

Applications

Time-course analysis of dTCTP secretion by Compound 48/80 treatment demonstrated a rapid release of dTCTP within 5 min after Compound 48/80 treatment and persistent release of dTCTP during mast cell degranulation induced by Compound 48/80 [1].

Animal experiment [2]:

Animal models

Female BALB/c mice weighing 20–22 g

Preparation Method

Female BALB/c mice were randomly divided into the following 4 groups: the control, model.Thirty minutes after gavage, Compound 48/80 (0.3 mg/kg) was injected through the tail vein, and body temperature was recorded using a biological function experimental system, in which a probe was inserted into the anus of each mouse for 30 min.

Dosage form

0.3 mg/kg

Applications

In the analysis of Active Systemic Anaphylaxis, compared with the control group, the body temperature of the model group(Compound 48/80) decreased significantly.

References:

[1]. Cho H, Park J, et,al. Dimerized Translationally Controlled Tumor Protein-Binding Peptide 2 Attenuates Systemic Anaphylactic Reactions Through Direct Suppression of Mast Cell Degranulation. Front Pharmacol. 2021 Oct 19;12:764321. doi: 10.3389/fphar.2021.764321. PMID: 34737708; PMCID: PMC8560797.

[2]. Zhang P, Wang Y, et,al. Allantoin Inhibits Compound 48/80-Induced Pseudoallergic Reactions In Vitro and In Vivo. Molecules. 2022 May 27;27(11):3473. doi: 10.3390/molecules27113473. PMID: 35684410; PMCID: PMC9182162.

Background

Compound 48/80 Trihydrochlorid ist eine Mischung aus Kondensationsprodukten von N-Methyl-p-methoxyphenethylamin mit Formaldehyd[1]. Compound 48/80 Trihydrochlorid ist auch ein Histamin-Freisetzer und Mastzelldegranulator[2]. Compound 48/80 wurde erstmals 1951 als aktiver Histamin-Freisetzungsmittel beschrieben[3], das Rötungen, Juckreiz und Jucken der menschlichen Haut verursachen kann [4]. Später wurde Compound 48/80 als klassischer Mastzellaktivator für IgE-unabhängige G-Proteine verwendet und ist die am häufigsten verwendete Aktivierungsmethode in Pseudoallergie-Studien[5]. Von Mastzellen sezerniertes HIS führt zu Vasodilatation, Ödemen, Pruritus und Hypothermie. Compound 48/80 Trihydrochlorid (C48 / 80 Trihydrochlorid) hemmt sowohl zytoplasmatische als auch partikuläre Phosphatidylinositol-spezifische Phospholipase-C-Aktivitäten mit ähnlicher Effizienz; IC50-Werte betragen 2,1 μg/ml (Überstand) bzw. 5,0 μg/ml (partikulärer Anteil). Die Aggregation von menschlichen Blutplättchen induziert durch ADP und PAF-acether wird durch Compound 48/80 gehemmt [1] .Compound-48 / -80 hemmt die phosphatidylinositol-spezifische Phospholipase-C-Aktivität von menschlichen Blutplättchen[6].

In vitro zeigte die zeitliche Analyse der dTCTP-Sekretion durch Compound-48/80-Behandlung eine schnelle Freisetzung von dTCTP innerhalb von 5 Minuten nach der Behandlung mit Compound 48/80 und anhaltende Freisetzung von dTCTP während der Mastzelldegranulation, die durch Compound 48/80 induziert wurde. [7].

Im In-vivo-Modell zeigte die Analyse einer systemischen Anaphylaxie, dass die Körpertemperatur der Versuchsgruppe (Compound 48/80) signifikant niedriger war als die der Kontrollgruppe. Compound 48/80 führte zu erhöhten Serumkonzentrationen von HIS, TNF-α und IL-8[8]. Die durch Compound 48/80 ausgelöste MC-Degranulation hatte antikonvulsive Effekte gegen PTZ-induzierte epileptische Anfälle, indem sie den Beginn sowohl des myoklonischen Ruckens als auch des generalisierten tonisch-klonischen Anfalls verlängerte und die Dauer des generalisierten tonisch-klonischen Anfalls verkürzte[9].

References:
[1]: Bronner C, Wiggins C, et,al. Compound 48/80 is a potent inhibitor of phospholipase C and a dual modulator of phospholipase A2 from human platelet. Biochim Biophys Acta. 1987 Aug 15;920(3):301-5. doi: 10.1016/0005-2760(87)90108-1. PMID: 3607084.
[2]: Schemann M, Kugler EM, et,al.The mast cell degranulator compound 48/80 directly activates neurons. PLoS One. 2012;7(12):e52104. doi: 10.1371/journal.pone.0052104. Epub 2012 Dec 18. PMID: 23272218; PMCID: PMC3525567.
[3]: Wang J, Zhang Y, et,al.Resveratrol inhibits MRGPRX2-mediated mast cell activation via Nrf2 pathway. Int Immunopharmacol. 2021 Apr;93:107426. doi: 10.1016/j.intimp.2021.107426. Epub 2021 Feb 4. PMID: 33550032.
[4]: Ding Y, Che D, et,al.Quercetin inhibits Mrgprx2-induced pseudo-allergic reaction via PLCγ-IP3R related Ca2+ fluctuations. Int Immunopharmacol. 2019 Jan;66:185-197. doi: 10.1016/j.intimp.2018.11.025. Epub 2018 Nov 21. PMID: 30471617.
[5]: Wang J, Zhang Y, et,al.Paeoniflorin inhibits MRGPRX2-mediated pseudo-allergic reaction via calcium signaling pathway. Phytother Res. 2020 Feb;34(2):401-408. doi: 10.1002/ptr.6531. Epub 2019 Oct 31. PMID: 31667930.
[6]: Kaida S, Ohta Y, Imai Y, Ohashi K, Kawanishi M. Compound 48/80 causes oxidative stress in the adrenal gland of rats through mast cell degranulation. Free Radic Res. 2010 Feb;44(2):171-80. doi: 10.3109/10715760903380466. PMID: 19886753.
[7]: Cho H, Park J, et,al. Dimerized Translationally Controlled Tumor Protein-Binding Peptide 2 Attenuates Systemic Anaphylactic Reactions Through Direct Suppression of Mast Cell Degranulation. Front Pharmacol. 2021 Oct 19;12:764321. doi: 10.3389/fphar.2021.764321. PMID: 34737708; PMCID: PMC8560797.
[8]:Zhang P, Wang Y, et,al. Allantoin Inhibits Compound 48/80-Induced Pseudoallergic Reactions In Vitro and In Vivo. Molecules. 2022 May 27;27(11):3473. doi: 10.3390/molecules27113473. PMID: 35684410; PMCID: PMC9182162. et,al.
[9]:Kilinc E, Torun IE, et,al. Mast cell activation ameliorates pentylenetetrazole-induced seizures in rats: The potential role for serotonin. Eur J Neurosci. 2022 May;55(9-10):2912-2924. doi: 10.1111/ejn.15145. Epub 2021 Feb 23. PMID: 33565644.

Chemical Properties

Cas No. 848035-21-2 SDF
Überlieferungen C48/80 trihydrochloride
Chemical Name 4-methoxy-3,5-bis[[2-methoxy-5-[2-(methylamino)ethyl]phenyl]methyl]-N-methyl-benzeneethanamine, trihydrochloride
Canonical SMILES COC1=CC=C(CCNC)C=C1CC2=CC(CCNC)=CC(CC3=C(OC)C=CC(CCNC)=C3)=C2OC.Cl.Cl.Cl
Formula C32H45N3O33HCl M.Wt 629.1
Löslichkeit 100mM in water Storage Store at -20°C, sealed storage, away from moisture ,protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
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 0.159 mL 0.7948 mL 1.5896 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 17 reference(s) in Google Scholar.)

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