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67526-95-8

中文名稱 毒胡蘿卜素
英文名稱 THAPSIGARGIN
CAS 67526-95-8
分子式 C34H50O12
MDL 編號 MFCD00083511
分子量 650.75
MOL 文件 67526-95-8.mol
更新日期 2024/06/12 17:31:30
67526-95-8 結(jié)構(gòu)式 67526-95-8 結(jié)構(gòu)式

基本信息

中文別名
毒胡蘿卜素, 來源于毒胡蘿卜
毒胡蘿卜素(>95% (HPLC),BC)
英文別名
THAPSIGARGIN
所屬類別
原料藥:抑制劑

物理化學(xué)性質(zhì)

沸點597.77°C (rough estimate)
密度1.1521 (rough estimate)
RTECS號RH0325700
折射率1.6390 (estimate)
儲存條件−20°C
儲存條件-20°C
溶解度DMSO: soluble
溶解度可溶于DMSO
酸度系數(shù)(pKa)10.57±0.70(Predicted)
形態(tài)liquid or film
顏色無色
敏感性感光
穩(wěn)定性DMSO或乙醇溶液可在-20°下穩(wěn)定儲存1周。
CAS 數(shù)據(jù)庫67526-95-8(CAS DataBase Reference)

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictogramsGHS hazard pictograms
GHS07,GHS08
警示詞危險
危險性描述H315-H319-H334-H335
危險品標(biāo)志Xn,T
危險類別碼36/37/38-42
危險類別碼R36/37/38-R42
安全說明26-36/37/39
安全說明S26-S36/37/39
危險品運輸編號UN 2811 6.1/PG 2
危險品運輸編號UN 2811 6.1/PG 2
WGK Germany3
WGK Germany3
海關(guān)編碼29181990

常見問題列表

用途
毒胡蘿卜素是廣泛使用的肌細(xì)胞內(nèi)質(zhì)網(wǎng)Ca(2 +)-ATPases抑制劑。 它充當(dāng)有效的,可滲透細(xì)胞的,不依賴IP3的細(xì)胞內(nèi)鈣釋放劑,可阻止血管生成抑制素和內(nèi)皮抑素誘導(dǎo)的細(xì)胞內(nèi)Ca2 +的瞬時增加。 它通過破壞細(xì)胞內(nèi)游離Ca2 +水平誘導(dǎo)細(xì)胞凋亡。
生物活性
Thapsigargin 是一種有效的、非競爭性的 the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) 的抑制劑,對carbachol誘導(dǎo)的[Ca2+]i瞬變在存不存在KCl預(yù)刺激條件下的IC50值分別為0.353 nM和0.448 nM。Thapsigargin 可誘導(dǎo)細(xì)胞凋亡。Thapsigargin 提取自植物Thapsia garganica。
靶點
TargetValue
SERCA
()
體外研究

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
體內(nèi)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.

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