1. Membrane Transporter/Ion Channel
  2. CRAC Channel
  3. YM-58483

YM-58483 (Synonyms: BTP2)

Cat. No.: HY-100831 Purity: 98.77%
Handling Instructions

YM-58483 is the first selective and potent inhibitor of CRAC channels and subsequent Ca2+ signals.

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

YM-58483 Chemical Structure

YM-58483 Chemical Structure

CAS No. : 223499-30-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 83 In-stock
Estimated Time of Arrival: December 31
2 mg USD 50 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
25 mg USD 320 In-stock
Estimated Time of Arrival: December 31
50 mg USD 530 In-stock
Estimated Time of Arrival: December 31
100 mg USD 940 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

YM-58483 is the first selective and potent inhibitor of CRAC channels and subsequent Ca2+ signals.

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[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

Intrathecal YM-58483 at the concentration of 300 μM (1.5 nmol) and 1000 μM (10 nmol) produces a significant central analgesic effect on the SNL rats[1]. In the mouse graft-versus-host disease (GVHD) model, YM-58483 (1-30 mg/kg, p.o.) and cyclosporine A (1-30 mg/kg, p.o.) inhibit donor anti-host cytotoxic T lymphocyte (CTL) activity and IFN-γ production, and also reduce the number of donor T cells, especially donor CD8+ T cells, in the spleen. YM-58483 (1-10 mg/kg, p.o.) and cyclosporine A (2, 10 mg/kg, p.o.) inhibit the sheep red blood cell (SRBC)-induced delayed type hypersensitivity (DTH) response[2]. M-58483 (30 mg/kg, p.o.) significantly suppresses ovalbumin (OVA)-induced bronchoconstriction in OVA-sensitized guinea pigs, whereas prednisolone does not. YM-58483 (3-30 mg/kg, p.o.) and prednisolone (100 mg/kg, p.o.) both significantly and completely suppress airway hyperresponsiveness (AHR) caused by OVA exposure[3]. YM-58483 inhibits antigen-induced eosinophil infiltration into airways, and decreases IL-4 and cysteinyl-leukotrienes content in inflammatory airways induced in actively sensitized Brown Norway rats. Orally administered YM-58483 prevents antigen-induced late phase asthmatic broncoconstriction and eosinophil infiltration in actively sensitized guinea pigs[4].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (75.95 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3735 mL 11.8675 mL 23.7349 mL
5 mM 0.4747 mL 2.3735 mL 4.7470 mL
10 mM 0.2373 mL 1.1867 mL 2.3735 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

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).

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

References
Molecular Weight

421.32

Formula

C₁₅H₉F₆N₅OS

CAS No.

223499-30-7

SMILES

O=C(C1=C(C)N=NS1)NC2=CC=C(N3N=C(C(F)(F)F)C=C3C(F)(F)F)C=C2

Shipping

Room temperature in continental US; may vary elsewhere

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YM-58483
Cat. No.:
HY-100831
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YM-58483

Cat. No.: HY-100831