Cat. No.: HY-100831

YM-58483

Name: YM-58483
Brand: MedChemExpress
SKU: HY-100831
Price: 55.00 USD
Availability: InStock
Rating: 5 (24 reviews)

(Synonyms: BTP2)

24 Cited Publications

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Based on 24 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).

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Pureté : 99.38%
CAS No.: 223499-30-7
Formule: C₁₅H₉F₆N₅OS
Masse moléculaire:421.32

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

YM-58483 Chemical Structure

CAS No.: 223499-30-7

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (24)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole (1)
Pureté et documentation
Références
Help & FAQs
Classifications
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Activité biologique

Description

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)^[1]^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	4.21 μM Compound: 29; YM-58483	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	[PMID: 30943030]
Jurkat	IC₅₀	0.15 μM Compound: 6	Inhibition of CRAC channel-mediated calcium influx in human Jurkat cells Inhibition of CRAC channel-mediated calcium influx in human Jurkat cells	[PMID: 18835179]
Jurkat	IC₅₀	10 nM Compound: 1, YM	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	[PMID: 25690784]
Jurkat	IC₅₀	17 nM Compound: 6	Inhibition of PHA-induced IL2 production in human Jurkat T lymphocytes Inhibition of PHA-induced IL2 production in human Jurkat T lymphocytes	[PMID: 18835179]
Jurkat	IC₅₀	75 nM Compound: 1, YM	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	[PMID: 25690784]
MDA-MB-231	IC₅₀	2.8 μM Compound: 1; YM-58483	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	[PMID: 27856238]
PC-12	IC₅₀	4.7 μM Compound: 6	Inhibition of VOC channel-mediated calcium influx in mouse PC12-h5 cells Inhibition of VOC channel-mediated calcium influx in mouse PC12-h5 cells	[PMID: 18835179]

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 (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. Further protocols information, click here.

In Vivo

YM-58483 (5 and 10 nmol/L, i.t.) produces significant central analgesic effects in SNL rats^[1].
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

CAS No. 223499-30-7
Appearance Solid
Masse moléculaire 421.32
Formule C₁₅H₉F₆N₅OS
Color White to off-white
SMILES

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

BTP2
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (24)

All IFFlow CytometryWBCell Imaging/StainingRT-PCRCell Proliferation/Viability Assay

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Journal Impact Factor

Cell Death Differ

OR2T6 modulates autophagy through the PPP3CA-mediated pathways to suppress gastric cancer. [Abstract]

2025 Nov 10. PMID: 41214150
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.
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.
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
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.
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
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

Identification and regulation of EMT cells in vivo by laser stimulation. [Abstract]

2025 May 27;9(2):026119. PMID: 40438388
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
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
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
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.
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
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

The actin cytoskeleton is important for pseudorabies virus infection. [Abstract]

2024 Dec:600:110233. PMID: 39255726
Physiol Rep

Monosodium glutamate-mediated Ca2+-dependent intestinal epithelial ion transports in health and IBS-D in male mice. [Abstract]

2026 Jun;14(11):e70975. PMID: 42281391
ETH Zurich

2026.
Elife

Sustained store-operated calcium entry utilizing activated chromatin state leads to instability in iTregs. [Abstract]

2023 Dec 6:12:RP88874. PMID: 38055613
bioRxiv

2023 Jun 6.

Solvant et solubilité

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

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Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

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.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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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

Protocole

All Cell Biology

Ca²⁺ Staining Technique
Ca²⁺ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca²⁺ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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YM-58483

24 Cited Publications

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YM-58483

Publications Citing Use of MedChemExpress (MCE) YM-58483