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Merck

Y4895

Sigma-Aldrich

YM-58483

≥98% (HPLC)

别名:

4-甲基-4′-[3,5-双(三氟甲基)-1H-吡唑-1-基]-1,2,3-噻二唑-5-甲酰苯胺

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About This Item

经验公式(希尔记法):
C15H9F6N5OS
分子量:
421.32
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 10 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

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 密鑰

XPRZIORDEVHURQ-UHFFFAOYSA-N

應用

YM-58483已被用于心肌细胞和肺动脉内皮细胞中存在的钙通道的抑制研究。

生化/生理作用

YM-58483是一种选择性的Ca++释放激活的Ca++(CRAC)[即库操纵性Ca++(SOC)通道],可介导Ca++流入T细胞和其他炎症细胞。CRAC通道抑制剂在自身免疫性疾病、移植排斥、气道过敏和支气管哮喘中具有潜在的临床应用。YM-58483也被推广为一种CRAC研究的工具;可用作金标准。

特點和優勢

该化合物在受体分类和信号转导手册的钙通道页面上有重点介绍。如需浏览其他手册页面,请点击此处

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

dust mask type N95 (US), Eyeshields, Gloves


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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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