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Y4895

Sigma-Aldrich

YM-58483

≥98% (HPLC)

Synonym(s):

4-methyl-4′-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]-1,2,3-thiadiazole-5-carboxanilide

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About This Item

Empirical Formula (Hill Notation):
C15H9F6N5OS
CAS Number:
223499-30-7
Molecular Weight:
421.32
MDL number:
MFCD00220976
UNSPSC Code:
12352200
PubChem Substance ID:
329831590
NACRES:
NA.77

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

SMILES string

Cc1nnsc1C(=O)Nc2ccc(cc2)-n3nc(cc3C(F)(F)F)C(F)(F)F

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)

InChI key

XPRZIORDEVHURQ-UHFFFAOYSA-N

Application

YM-58483 has been used in the inhibition studies of calcium channels present in cardiomyocytes and pulmonary arterial endothelial cells.

Biochem/physiol Actions

YM-58483 is a selective Ca++ release-activated Ca++ (CRAC) [a.k.a. store-operated Ca++ (SOC) channels] that mediate Ca++ influx in T cells and other inflammatory cells. CRAC channel inhibitors have potential clinical applications in autoimmune disease, transplant rejection, allergic airway inflammation and bronchial asthma. YM-58483 is also promoted as a tool for CRAC studies; may be used as a gold standard.

Features and Benefits

This compound is featured on the Calcium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Sodium entry through endothelial store-operated calcium entry channels: regulation by Orai1
Xu N, et al.
American Journal of Physiology. Cell Physiology, 308(4), C277-C288 (2014)
Data on calcium increases depending on stretch in dystrophic cardiomyocytes
Aguettaz E et al.
Data in Brief, 8, 1443-1447 (2016)
Estella Zuccolo et al.
Stem cells and development, 27(1), 23-34 (2017-11-11)
Stromal cell-derived factor-1α (SDF-1α) drives endothelial colony-forming cell (ECFC) homing and incorporation within neovessels, thereby restoring tissue perfusion in ischemic tissues and favoring tumor vascularization and metastasis. SDF-1α stimulates ECFC migration by activating the G
Ningyong Xu et al.
American journal of physiology. Cell physiology, 308(4), C277-C288 (2014-11-28)
Orai1 interacts with transient receptor potential protein of the canonical subfamily (TRPC4) and contributes to calcium selectivity of the endothelial cell store-operated calcium entry current (ISOC). Orai1 silencing increases sodium permeability and decreases membrane-associated calcium, although it is not known
Hyunji Moon et al.
Nature communications, 11(1), 5489-5489 (2020-11-01)
Calcium flux regulating intracellular calcium levels is essential and modulated for efficient efferocytosis. However, the molecular mechanism by which calcium flux is modulated during efferocytosis remains elusive. Here, we report that Orai1, a Crbn substrate, is upregulated via its attenuated
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