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YM-58483

MCE China：YM-58483

Brand：MedChemExpress (MCE)

Cat. No.HY-100831

CAS：223499-30-7

Synonyms：BTP2

Purity：99.38%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：YM-58483 (BTP2) is the first selective and potent inhibitor of CRAC channels and subsequent Ca2+ signals. YM-584832 is a blocker of store-operated Ca2+ entry (SOCE).

In Vitro：YM-58483 can decrease the levels of P-ERK and P-CREB, without affecting the expression of CD11b and GFAP. YM-58483 also inhibits the release of spinal cord IL-1β, TNF-α, and PGE2[1]. YM-58483 and cyclosporine A inhibits T cell proliferation in a one-way mixed lymphocyte reaction (mLR) with IC50 values of 330 and 12.7 nM, respectively[2]. YM-58483 inhibits DNP antigen-induced histamine release from and leukotrienes (LTs) production in IgE-primed RBL-2H3 cells, a rat basophilic leukemia cell line, with IC50 values of 460 and 310 nM, respectively. YM-58483 also inhibits phytohemagglutinin-P (PHA)-stimulated IL-5 and IL-13 production in human peripheral blood cells with IC50 values of 125 and 148 nM, respectively, which is approximately 5 times less potent than Prednisolone (HY-17463)[3]. YM-58483 inhibits IL-4 and IL-5 production in a conalbumine-stimulated murine Th2 T cell clone (D10.G4.1), and IL-5 production in phytohemagglutinin-stimulated human whole blood cells with IC50 values comparable to those reported for its CRAC channel inhibition (around 100 nM)[4].

In Vivo：YM-58483 (5 and 10 nmol/L, i.t.) produces significant central analgesic effects in SNL rats[1]. YM-58483 (1-30 mg/kg, p.o.) inhibits donor anti-host cytotoxic T lymphocyte (CTL) activity and IFN-γ production in a mouse graft-versus-host disease (GVHD) model and reduces the number of donor T cells in the spleen, especially donor CD8+ T cells[2]. YM-58483 (1-10 mg/kg, p.o.) inhibits sheep red blood cell (SRBC)-induced delayed-type hypersensitivity (DTH) reactions[2]. M-58483 (30 mg/kg, p.o.) significantly inhibits bronchoconstriction induced by Ovalbumins (HY-W250978) in OVA-sensitized guinea pigs[3]. YM-58483 (3-30 mg/kg, p.o.) completely inhibits airway hyperresponsiveness (AHR) induced by Ovalbumins (HY-W250978) exposure[3]. YM-58483 inhibits antigen-induced eosinophil infiltration into the airways and reduced IL-4 and cysteinyl-leukotrienes levels in inflammatory airways induced in actively sensitized Brown Norway rats[4].

Animal Administration：Male Balb/c mice are immunized by subcutaneous injection of SRBC (2×107 cells) on day 0. Immunized mice are challenged with 30 μL of 1×108 SRBC into the left hind footpad on day 5. Footpad swelling is measured 24 h after the challenge using a thickness gauge and expressed as the difference between the thickness of the left footpad and that of the right one, which receives an equal volume of 0.9% saline. As a negative control, male Balb/c mice are injected with 0.9% saline and challenged with SRBC. YM-58483 and cyclosporine A are administered orally once daily from day 0 to day 5 (6 consecutive days).

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References：

[1]. Qi Z, et al. The Central Analgesic Mechanism of YM-58483 in Attenuating Neuropathic Pain in Rats. Cell Mol Neurobiol. 2016 Oct;36(7):1035-43  [Content Brief]

[2]. Ohga K, et al. Characterization of YM-58483/BTP2, a novel store-operated Ca2+ entry blocker, on T cell-mediated immune responses in vivo. Int Immunopharmacol. 2008 Dec 20;8(13-14):1787-9  [Content Brief]

[3]. Ohga K, et al. The suppressive effects of YM-58483/BTP-2, a store-operated Ca2+ entry blocker, on inflammatory mediator release in vitro and airway responses in vivo. Pulm Pharmacol Ther. 2008;21(2):360-9  [Content Brief]

[4]. Yoshino T, et al. YM-58483, a selective CRAC channel inhibitor, prevents antigen-induced airway eosinophilia and late phase asthmatic responses via Th2 cytokine inhibition in animal models. Eur J Pharmacol. 2007 Apr 10;560(2-3):225-33  [Content Brief]