YM-58483-BTP2-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEYM-58483Cat. No.: HY-100831CAS No.: 223499-30-7Synonyms: BTP2分式: CHFNOS分量: 421.32作靶點: CRAC Channel作通路: Membrane Transporter/Ion Channel儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 32 mg/

2、mL (75.95 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.3735 mL 11.8675 mL 23.7349 mL5 mM 0.4747 mL 2.3735 mL 4.7470 mL10 mM 0.2373 mL 1.1867 mL 2.3735 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?，再依次添加助溶?為保

3、證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.93 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.93 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師ww

4、w.MedChemEBIOLOGICAL ACTIVITY物活性 YM-58483種有效的 CRAC channels 抑制劑，能夠抑制 Ca2+ 信號。體外研究 YM-58483 can decrease the levels of P-ERK and P-CREB, without affecting the expression of CD11b andGFAP. YM-58483 also inhibits the release of spinal cord IL-1, TNF-, and PGE2 1. YM-58483 andcyclosporine A inhibits T c

5、ell proliferation in a one-way mixed lymphocyte reaction (mLR) with IC50 values of330 and 12.7 nM, respectively 2. YM-58483 inhibits DNP antigen-induced histamine release from andleukotrienes (LTs) production in IgE-primed RBL-2H3 cells, a rat basophilic leukemia cell line, with IC50values of 460 an

6、d 310 nM, respectively. YM-58483 also inhibits phytohemagglutinin-P (PHA)-stimulated IL-5and 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 productionin

7、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 channelinhibition (around 100 nM) 4.體內(nèi)研究 Intrathecal YM-58483 at the concentration of 300 M (1.5 nmol)

8、and 1000 M (10 nmol) produces asignificant 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 Tlymphocyte (CTL) activity and IFN- production, and also redu

9、ce the number of donor T cells, especiallydonor CD8+ T cells, in the spleen. YM-58483 (1-10 mg/kg, p.o.) and cyclosporine A (2, 10 mg/kg, p.o.) inhibitthe sheep red blood cell (SRBC)-induced delayed type hypersensitivity (DTH) response 2. M-58483 (30mg/kg, p.o.) significantly suppresses ovalbumin (O

10、VA)-induced bronchoconstriction in OVA-sensitized guineapigs, whereas prednisolone does not. YM-58483 (3-30 mg/kg, p.o.) and prednisolone (100 mg/kg, p.o.) bothsignificantly and completely suppress airway hyperresponsiveness (AHR) caused by OVA exposure 3. YM-58483 inhibits antigen-induced eosinophi

11、l infiltration into airways, and decreases IL-4 and cysteinyl-leukotrienes content in inflammatory airways induced in actively sensitized Brown Norway rats. Orallyadministered YM-58483 prevents antigen-induced late phase asthmatic broncoconstriction and eosinophilinfiltration in actively sensitized

12、guinea pigs 4.PROTOCOLAnimal Male Balb/c mice are immunized by subcutaneous injection of SRBC (2107 cells) on day 0. ImmunizedAdministration 2 mice are challenged with 30 L of 1108 SRBC into the left hind footpad on day 5. Footpad swelling ismeasured 24 h after the challenge using a thickness gauge

13、and expressed as the difference between thethickness of the left footpad and that of the right one, which receives an equal volume of 0.9% saline. As anegative control, male Balb/c mice are injected with 0.9% saline and challenged with SRBC. YM-58483 andcyclosporine A are administered orally once da

14、ily from day 0 to day 5 (6 consecutive days).MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Sci Rep. 2017 Oct 16;7(1):12881.See more customer validations on HYPERLINK / www.MedChemEREFERENCES

15、1. Qi Z, et al. The Central Analgesic Mechanism of YM-58483 in Attenuating Neuropathic Pain in Rats. Cell Mol Neurobiol. 2016Oct;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 invivo. Int Immunopharmac

16、ol. 2008 Dec 20;8(13-14):1787-923. Ohga K, et al. The suppressive effects of YM-58483/BTP-2, a store-operated Ca2+ entry blocker, on inflammatory mediator release invitro 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 asthmaticresponses via Th2 cytokine inhibition in animal models