YM-58483
Based on 22 publication(s) in Google Scholar
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).
For research use only. We do not sell to patients.
- Purity: 99.38%
- CAS No.: 223499-30-7
- Formula: C15H9F6N5OS
- Molecular Weight:421.32
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Immunology/Inflammation Compound Library
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Publications Citing Use of MedChemExpress (MCE) YM-58483
More- Cell Death Differ. 2025 Nov 10. [Abstract]
- J Hazard Mater. 2021 Sep 5:417:126025. [Abstract]
- Acta Pharmacol Sin. 2024 May;45(5):975-987. [Abstract]
- Phytomedicine. 2025 Jul:142:156632. [Abstract]
- Free Radic Biol Med. 2023 Aug 20:205:25-46. [Abstract]
- Br J Pharmacol. 2026 Jul;183(13):3651-3665. [Abstract]
- J Med Chem. 2025 Apr 17. [Abstract]
- Elife. 2023 Dec 6:12:RP88874. [Abstract]
- Inflamm Res. 2024 Jun;73(6):945-960. [Abstract]
- Int J Mol Sci. 2023 Apr 6;24(7):6818. [Abstract]
- Am J Physiol Cell Physiol. 2025 Apr 29. [Abstract]
- APL Bioeng. 2025 May 27;9(2):026119. [Abstract]
- Front Mol Biosci. 2021 Sep 14;8:646730. [Abstract]
- Biomedicines. 2023 Jun 4;11(6):1637. [Abstract]
- Sci Rep. 2017 Oct 16;7(1):12881. [Abstract]
- Toxicol Appl Pharmacol. 2025 Oct:503:117465. [Abstract]
- Saudi Pharm J. 2023 Feb;31(2):245-254. [Abstract]
- Mol Biol Rep. 2025 Feb 12;52(1):223. [Abstract]
- Genes (Basel). 2022 May 13;13(5):874. [Abstract]
- J Pain Res. 2021 Oct 18;14:3289-3299. [Abstract]
- Virology. 2024 Dec:600:110233. [Abstract]
- bioRxiv. 2023 Jun 6.
Customer Validation & Images
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WB
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WB
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IF
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Cell Imaging/Staining
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RT-PCR
Biological Activity
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
4.21 μM
Compound: 29; YM-58483
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Inhibition of YFP-tagged TRPC3 (unknown origin) expressed in HEK293 cells assessed as reduction carbhocol-induced receptor operated Calcium influx after 5 mins by fura-2-AM dye based assay
Inhibition of YFP-tagged TRPC3 (unknown origin) expressed in HEK293 cells assessed as reduction carbhocol-induced receptor operated Calcium influx after 5 mins by fura-2-AM dye based assay
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[PMID: 30943030] |
| Jurkat | IC50 |
0.15 μM
Compound: 6
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Inhibition of CRAC channel-mediated calcium influx in human Jurkat cells
Inhibition of CRAC channel-mediated calcium influx in human Jurkat cells
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[PMID: 18835179] |
| Jurkat | IC50 |
10 nM
Compound: 1, YM
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Inhibition of Orai channel in phytohemagglutinin-stimulated human Jurkat E6-1 cells assessed as NFAT-induced transcription measured as IL-2 level after 20 hrs by ELISA
Inhibition of Orai channel in phytohemagglutinin-stimulated human Jurkat E6-1 cells assessed as NFAT-induced transcription measured as IL-2 level after 20 hrs by ELISA
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[PMID: 25690784] |
| Jurkat | IC50 |
17 nM
Compound: 6
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Inhibition of PHA-induced IL2 production in human Jurkat T lymphocytes
Inhibition of PHA-induced IL2 production in human Jurkat T lymphocytes
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[PMID: 18835179] |
| Jurkat | IC50 |
75 nM
Compound: 1, YM
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Inhibition of Orai-mediated calcium entry in human Jurkat E6-1 cells after 1 hr by FLIPR assay
Inhibition of Orai-mediated calcium entry in human Jurkat E6-1 cells after 1 hr by FLIPR assay
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[PMID: 25690784] |
| MDA-MB-231 | IC50 |
2.8 μM
Compound: 1; YM-58483
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Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-ba
Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-ba
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[PMID: 27856238] |
| PC-12 | IC50 |
4.7 μM
Compound: 6
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Inhibition of VOC channel-mediated calcium influx in mouse PC12-h5 cells
Inhibition of VOC channel-mediated calcium influx in mouse PC12-h5 cells
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[PMID: 18835179] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 223499-30-7
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Appearance Solid
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Molecular Weight 421.32
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Formula C15H9F6N5OS
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Color White to off-white
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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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Synonyms
BTP2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (22)
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Journal Impact Factor
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Most Recent
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Cell Death Differ
OR2T6 modulates autophagy through the PPP3CA-mediated pathways to suppress gastric cancer. [Abstract]2025 Nov 10. PMID: 41214150 -
J Hazard Mater
Polystyrene microplastics trigger hepatocyte apoptosis and abnormal glycolytic flux via ROS-driven calcium overload. [Abstract]2021 Sep 5:417:126025. PMID: 34229379
YM-58483 purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2021 Sep 5:417:126025. [Abstract]
YM-58483 (BTP2, pre-treated for 90 min with 5 μM or 10 μM). Suppressed Oari1 inhibited microplastics-induced Ca2+ overload in vitro. Fluorescence immunostaining of Fura-3AM in L02 cells (scale bar=50 µm).
YM-58483 purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2021 Sep 5:417:126025. [Abstract]
YM-58483 (BTP2, pre-treated for 90 min with 5 μM or 10 μM). Flow cytometry analysis of the concentrations of Ca2+ in L02 cells.
YM-58483 purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2021 Sep 5:417:126025. [Abstract]
YM-58483 (BTP2, pre-treated for 90 min with 5 μM or 10 μM). The protein expression levels of Orai1, Stim1 and SERCA in L02 cells were detected using western blotting. The intensity of each nuclear envelope protein was normalized to GAPDH intensity.
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Acta Pharmacol Sin
Endothelial cell Orai1 is essential for endothelium-dependent contraction of mouse carotid arteries in normotensive and hypertensive mice. [Abstract]2024 May;45(5):975-987. PMID: 38279042 -
Phytomedicine
Curcuminoids WM03 inhibits ovarian cancer cisplatin-resistant cells proliferation and reverses cisplatin resistance by targeting DYRK2. [Abstract]2025 Jul:142:156632. PMID: 40315643
YM-58483 purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Jul:142:156632. [Abstract]
YM-58483 (BTP2, 10 μM) to treat A2780DR and HO8910PMDR cells and detected Akt phosphorylation (p-Akt) during the time course. Western blotting image for Akt phosphorylation in control and calcium and calcium channel blockers.
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Free Radic Biol Med
β-carotene targets IP3R/GRP75/VDAC1-MCU axis to renovate LPS-induced mitochondrial oxidative damage by regulating STIM1. [Abstract]2023 Aug 20:205:25-46. PMID: 37270031
YM-58483 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2023 Aug 20:205:25-46. [Abstract]
Effects of YM-58483 (BTP2, 20 μM, 2 h) on endoplasmic reticulum stress and mitochondrial damage induced by LPS in BMECs. The protein expressions of STIM1, ORAI1, PERK, ATF6, IRE1α, GRP78 and CHOP.
YM-58483 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2023 Aug 20:205:25-46. [Abstract]
Effects of YM-58483 (BTP2, 20 μM, 2 h) on endoplasmic reticulum stress and mitochondrial damage induced by LPS in BMECs. Immunofluorescence results of ER-Tracker (the bar = 20 μm), Ca2+ (the bar = 100 μm).
YM-58483 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2023 Aug 20:205:25-46. [Abstract]
Effects of YM-58483 (BTP2, 20 μM, 2 h) on endoplasmic reticulum stress and mitochondrial damage induced by LPS in BMECs. Fluorescence results of mitochondrial ROS, the bar = 100 μm.
YM-58483 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2023 Aug 20:205:25-46. [Abstract]
YM-58483 (BTP2, 5, 10, or 20 μM, 2 h).The mRNA expression of ER stress and mitochondrial damage related genes. The results are presented as the means ± SEM. *P<0.05, **P<0.01, representing significant difference compared with control group.
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Br J Pharmacol
A potential mechanism and strategy for accelerating recovery of neurocognitive function after general anaesthesia through store-operated Orai1 channels. [Abstract]2026 Jul;183(13):3651-3665. PMID: 41918371 -
J Med Chem
A Novel Compound 3a-M1, from Metabolites of Sinomenine Derivative 3a, Exerts Potent Anti-Aplastic Anemia Activity via IP3R/ORAI-Mediated CTL Ferroptosis. [Abstract]2025 Apr 17. PMID: 40243551 -
Elife
Sustained store-operated calcium entry utilizing activated chromatin state leads to instability in iTregs. [Abstract]2023 Dec 6:12:RP88874. PMID: 38055613 -
Inflamm Res
Quercetin and Kaempferol inhibit HMC-1 activation via SOCE/NFATc2 signaling and suppress hippocampal mast cell activation in lipopolysaccharide-induced depressive mice. [Abstract]2024 Jun;73(6):945-960. PMID: 38587532 -
Int J Mol Sci
Role of Orai3-Mediated Store-Operated Calcium Entry in Radiation-Induced Brain Microvascular Endothelial Cell Injury. [Abstract]2023 Apr 6;24(7):6818. PMID: 37047790 -
Am J Physiol Cell Physiol
Orai channel pharmacological manipulation reduces metabolic flexibility in cardiac fibroblasts. [Abstract]2025 Apr 29. PMID: 40298968 -
APL Bioeng
2025 May 27;9(2):026119. PMID: 40438388 -
Front Mol Biosci
X-Ray Causes mRNA Transcripts Change to Enhance Orai2-Mediated Ca2+ Influx in Rat Brain Microvascular Endothelial Cells. [Abstract]2021 Sep 14;8:646730. PMID: 34595206 -
Biomedicines
Targeting Store-Operated Calcium Entry Regulates the Inflammation-Induced Proliferation and Migration of Breast Cancer Cells. [Abstract]2023 Jun 4;11(6):1637. PMID: 37371732 -
Sci Rep
Unveiling some FDA-approved drugs as inhibitors of the store-operated Ca2+ entry pathway. [Abstract]2017 Oct 16;7(1):12881. PMID: 29038464 -
Toxicol Appl Pharmacol
Hepatocyte mitochondrial DNA activated store-operated Ca2+ entry via Stim1/Orai1-induced podocyte injury in trichloroethylene sensitized mice: A new insight in liver and kidney crosstalk. [Abstract]2025 Oct:503:117465. PMID: 40669774 -
Saudi Pharm J
Blockade of store-operated calcium entry sensitizes breast cancer cells to cisplatin therapy via modulating inflammatory response. [Abstract]2023 Feb;31(2):245-254. PMID: 36942275
YM-58483 purchased from MedChemExpress. Usage Cited in: Saudi Pharm J. 2023 Feb;31(2):245-254. [Abstract]
Combining BTP2 (YM-58483) with cisplatin significantly potentiates the antiproliferative effect of cisplatin in both MDA-MB-231 and MCF7 cells for 24 h.
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Mol Biol Rep
Mechanism of Ca2+ overload caused by STIM1/ORAI1 activation of store-operated Ca2+ entry (SOCE) in hydrogen peroxide-induced mitochondrial damage and apoptosis in human primary melanocytes. [Abstract]2025 Feb 12;52(1):223. PMID: 39937331 -
Genes (Basel)
STIM1-Orai1 Interaction Exacerbates LPS-Induced Inflammation and Endoplasmic Reticulum Stress in Bovine Hepatocytes through Store-Operated Calcium Entry. [Abstract]2022 May 13;13(5):874. PMID: 35627260 -
J Pain Res
Store-Operated Calcium Channels Contribute to Remifentanil-Induced Postoperative Hyperalgesia via Phosphorylation of CaMKIIα in Rats. [Abstract]2021 Oct 18;14:3289-3299. PMID: 34703304 -
Virology
2024 Dec:600:110233. PMID: 39255726 -
Solvent & Solubility
DMSO : 125 mg/mL (296.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3735 mL | 11.8675 mL | 23.7349 mL | 59.3373 mL |
| 5 mM | 0.4747 mL | 2.3735 mL | 4.7470 mL | 11.8675 mL | |
| 10 mM | 0.2373 mL | 1.1867 mL | 2.3735 mL | 5.9337 mL | |
| 15 mM | 0.1582 mL | 0.7912 mL | 1.5823 mL | 3.9558 mL | |
| 20 mM | 0.1187 mL | 0.5934 mL | 1.1867 mL | 2.9669 mL | |
| 25 mM | 0.0949 mL | 0.4747 mL | 0.9494 mL | 2.3735 mL | |
| 30 mM | 0.0791 mL | 0.3956 mL | 0.7912 mL | 1.9779 mL | |
| 40 mM | 0.0593 mL | 0.2967 mL | 0.5934 mL | 1.4834 mL | |
| 50 mM | 0.0475 mL | 0.2373 mL | 0.4747 mL | 1.1867 mL | |
| 60 mM | 0.0396 mL | 0.1978 mL | 0.3956 mL | 0.9890 mL | |
| 80 mM | 0.0297 mL | 0.1483 mL | 0.2967 mL | 0.7417 mL | |
| 100 mM | 0.0237 mL | 0.1187 mL | 0.2373 mL | 0.5934 mL |
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