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Purity: ≥98%
YM-58483, formerly known as BTP 2, is a potent inhibitor of CRAC channels, blocking thapsigargin-induced sustained calcium influx, Th2 cytokine production, and NF-AT-driven promoter activity in T lymphocytes (IC50 = 100 nM).
| ln Vitro |
Without changing the expression of CD11b and GFAP, YM-58483 can lower the levels of P-ERK and P-CREB. Moreover, intestinal IL-1β, TNF-α, and PGE2 production are inhibited by YM-58483 [1]. In a one-way mixed solution reaction (mLR), YM-58483 and cyclosporine A both inhibit T cell growth with IC50 values of 330 and 12.7 nM, respectively [2]. With IC50 values of 460 and 310 nM, YM-58483 suppresses the synthesis of IgE-stimulated leukotriene (LT) and histamine in RBL-2H3 cells (a gradient alkaline dilution cell line). With IC50 values of 125 and 148 nM, respectively, YM-58483 also suppresses the production of IL-5 and IL-13 in human peripheral blood cells triggered by phytohemagglutinin-P (PHA), a mechanism that is around five times less potent than prednisolone [3]. In human whole blood cells stimulated with phytohemagglutinin, YM-58483 reduces the production of IL-5 and IL-4 in murine Th2 T cell clones (D10.G4) stimulated with leucine. The IC50 value is similar to the published CRAC channel inhibition value (about 100 nM) [4].
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| ln Vivo |
Intrathecal injection of YM-58483 at doses of 300 μM (1.5 nmol) and 1000 μM (10 nmol) produced strong central analgesic effects on SNL [1]. , YM-58483 (1-30 mg/kg, po) and cyclosporine A (1-30 mg/kg, po) suppress donor anti-cytotoxic T (CTL) activity and IFN-γ production, and Reduce the amount of donor T cells in the spleen, specifically donor CD8+ T cells. YM-58483 (1-10 mg/kg, po) and cyclosporine A (2, 10 mg/kg, po) reduce the delayed-type hypersensitivity (DTH) response elicited by sheep red blood cells (SRBC) [2]. M-58483 (30 mg/kg, elbow) significantly decreased ovalbumin (OVA)-induced delayed-type contractions in OVA-sensitized guinea pigs, whereas YM-58483 (3-30 mg/kg, face) and Prednisolone (100 mg/kg, facial) considerably and totally inhibited the airway hyperresponsiveness (AHR) generated by OVA [3]. YM-58483 buffers eosinophils caused by breathing into the airways and lowers IL-4 and cysteine foam leukotriene levels in activated airways induced by active sensitization of brown Norwegian Scotch centers. Pathway YM-58483 prevents powerful induction of late death and eosinophilic respiration in actively sensitized guinea pigs [4].
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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
[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 [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 [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 |
| Molecular Formula |
C15H9F6N5OS
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|---|---|
| Molecular Weight |
421.3214
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| Exact Mass |
421.0432
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| CAS # |
223499-30-7
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| Related CAS # |
223499-30-7;
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| SMILES |
O=C(C1=C(C)N=NS1)NC2=CC=C(N3N=C(C(F)(F)F)C=C3C(F)(F)F)C=C2
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| InChi Key |
XPRZIORDEVHURQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H9F6N5OS/c1-7-12(28-25-23-7)13(27)22-8-2-4-9(5-3-8)26-11(15(19,20)21)6-10(24-26)14(16,17)18/h2-6H,1H3,(H,22,27)
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| Chemical Name |
N-[4-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl-1,2,3-thiadiazole-5-carboxamide
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| Synonyms |
YM-58483 YM 58483 YM58483 BTP 2 BTP-2 BTP2.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ~125 mg/mL (~296.69 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.93 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 (5.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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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