YM 58483
YM 58483, also known as BTP2, is a SOCE blocker. SOCE has been found in macrophages, basophils, dendritic cells, and mast cells as well as T cells. The SOCE-related channels include the Ca2+ release-activated Ca2+ (CRAC) channel which is a highly Ca2+-selective channel, and the non-selective, Ca2+-permeable transient receptor potential (TRP) channels, which regulate the activation of non-excitable cells such as lymphocytes. YM 58483 has been reported to inhibit cytokine production and proliferation in T cells, and may serve as a potential medicinal candidate for treatment of bronchial asthma.?
References:
1.?Ohga K, Takezawa R, Arakida Y, et al. Characterization of YM-58483/BTP2, a novel store-operated Ca2+ entry blocker, on T cell-mediated immune responses in vivo. International Immunopharmacology, 2008, 8(13-14): 1787-1792.
2.?Ishikawa J, Ohga K, Yoshino T, et al. A pyrazole derivative, YM-58483, potently inhibits store-operated sustained Ca2+ influx and IL-2 production in T lymphocytes. Journal of Immunology, 2003, 170(9): 4441-4449.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 421.32 |
| Cas No. | 223499-30-7 |
| Formula | C15H9F6N5OS |
| Solubility | insoluble in H2O; ≥50 mg/mL in EtOH; ≥90 mg/mL in DMSO |
| Chemical Name | N-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-4-methyl-1,2,3-thiadiazole-5-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | FC(F)(C1=CC(C(F)(F)F)=NN1C(C=C2)=CC=C2NC(C3=C(C)N=NS3)=O)F |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[2] | |
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Cell lines |
Jurkat cells |
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Reaction Conditions |
0.0003 ~ 1 μM YM 58483 |
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Applications |
YM 58483 dose-dependently inhibited PHA-induced IL-2 production in Jurkat cells, with an IC50 value of 17 ± 3.2 nM. Moreover, YM 58483 potently inhibited NF-AT-driven promoter activity, but not AP-1-driven promoter activity in Jurkat cells. |
| Animal experiment:[1] | |
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Animal models |
Mouse graft-versus-host disease (GVHD) model |
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Dosage form |
1 ~ 30 mg/kg Once daily by oral route (p.o.) for 10 days |
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Applications |
YM 58483 (1 ~ 30 mg/kg, p.o.) and cyclosporine A (1 ~ 30 mg/kg, p.o.) inhibited donor anti-host cytotoxic T lymphocyte (CTL) activity and IFN-γ production, and also reduced the number of donor T cells, especially donor CD8+ T cells, in the spleen. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Ohga K, Takezawa R, Arakida Y, et al. Characterization of YM-58483/BTP2, a novel store-operated Ca2+ entry blocker, on T cell-mediated immune responses in vivo. International Immunopharmacology, 2008, 8(13-14): 1787-1792. 2. Ishikawa J, Ohga K, Yoshino T, et al. A pyrazole derivative, YM-58483, potently inhibits store-operated sustained Ca2+ influx and IL-2 production in T lymphocytes. Journal of Immunology, 2003, 170(9): 4441-4449. |
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Quality Control & MSDS
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Chemical structure
