毒胡萝卜素

用途生物活性靶点体外研究体内研究毒胡萝卜素试剂级价格

毒胡萝卜素

CAS号:67526-95-8
英文名:Thapsigargin
中文名:毒胡萝卜素
CBNumber:CB4768595
分子式:C34H50O12
分子量:650.75
MOL File:67526-95-8.mol

毒胡萝卜素化学性质

沸点 :597.77°C (rough estimate)
密度 :1.1521 (rough estimate)
折射率 :1.6390 (estimate)
RTECS号 :RH0325700
储存条件 :-20°C
溶解度 :DMSO: soluble
形态 :liquid or film
酸度系数(pKa) :10.57±0.70(Predicted)
颜色 :Colorless
敏感性 :Light Sensitive
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 week.
CAS 数据库 :67526-95-8(CAS DataBase Reference)

安全信息

危险品标志 :Xn,T
危险类别码 :36/37/38-42
安全说明 :26-36/37/39
危险品运输编号 :UN 2811 6.1/PG 2
WGK Germany :3
海关编码 :29181990

毒胡萝卜素性质、用途与生产工艺

用途毒胡萝卜素是广泛使用的肌细胞内质网Ca（2 +）-ATPases抑制剂。它充当有效的，可渗透细胞的，不依赖IP3的细胞内钙释放剂，可阻止血管生成抑制素和内皮抑素诱导的细胞内Ca2 +的瞬时增加。它通过破坏细胞内游离Ca2 +水平诱导细胞凋亡。
生物活性 Thapsigargin 是一种有效的、非竞争性的 the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) 的抑制剂，对carbachol诱导的[Ca2+]i瞬变在存不存在KCl预刺激条件下的IC50值分别为0.353 nM和0.448 nM。Thapsigargin 可诱导细胞凋亡。Thapsigargin 提取自植物Thapsia garganica。
靶点
Target Value
SERCA
()

体外研究

Thapsigargin (0.001- 1 μM; for 2 and 4 days) arrests cell proliferations in MH7A human rheumatoid arthritis synovial cells in a time- and dose-dependent manner.
Thapsigargin (0.001- 1 μM; for 2 and 4 days) induces cell apoptosis in MH7A cells in a time- and dose-dependent manner.
Thapsigargin (0.001- 1 μM; for 2 and 4 days) impairs mTOR activity and leads to cyclin D1 expressions in MH7A cells.
Thapsigargin inhibits Ca ²⁺ entry into human neutrophil granulocytes.
Thapsigargin inhibits the carbachol-evoked [Ca ²⁺ ]i-transients with (IC ₅₀ =0.353 nM) or without (IC ₅₀ =0.448 nM) a KCl-prestimulation, but an additional small component, with a much lower sensitivity (IC ₅₀ =4814 nM), is observed in the absence of a KCl-prestimulation. In contrast, the KCl-evoked [Ca ²⁺ ]i-transients displayed only one component with a very low sensitivity to Thapsigargin in both absence (IC ₅₀ =3343 nM) and presence (IC ₅₀ =6858 nM) of a carbachol-prestimulation.

Cell Proliferation Assay

Cell Line:	MH7A human rheumatoid arthritis synovial cells
Concentration:	0.001, 0.1, and 1 μM
Incubation Time:	For 2 and 4 days
Result:	Arrested cell proliferations in a time- and dose-dependent manner.

Apoptosis Analysis

Cell Line:	MH7A human rheumatoid arthritis synovial cells
Concentration:	0.001, 0.1, and 1 μM
Incubation Time:	For 2 and 4 days
Result:	Induces cell apoptosis in a time- and dose-dependent manner.

Western Blot Analysis

Cell Line:	MH7A human rheumatoid arthritis synovial cells
Concentration:	0.001, 0.1, and 1 μM
Incubation Time:	For 2 and 4 days
Result:	Impairs mTOR activity and leads to cyclin D1 expressions

体内研究

Thapsigargin (Injection; 0.25 ug/g, 0.5 ug/g and 1 ug/g; 24 hours) significant increases of 2 to 5-fold in chemokine and pro-inflammatory expression. Thapsigargin is more sensitive to inducing a systemic immune response.

Animal Model:	Male Balb/c mice (20-25 g)
Dosage:	0.25 ug/g, 0.5 ug/g and 1 ug/g
Administration:	Injection; 24 hours
Result:	Increased of 2 to 5-fold in chemokine and pro-inflammatory expression.