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40045-50-9

中文名稱 2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑
英文名稱 5-[(5-Nitro-2-thiazolyl)thio]-1,3,4thiadiazol-2-amine
CAS 40045-50-9
分子式 C5H3N5O2S3
分子量 261
MOL 文件 40045-50-9.mol
更新日期 2024/12/30 10:31:05
40045-50-9 結構式 40045-50-9 結構式

基本信息

中文別名
化合物SU3327
5-((5-硝基噻唑-2-基)硫基)-1,3,4-噻二唑-2-胺
2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑
英文別名
Halicin
SU 3327
JNK Inhibitor XIII - CAS 40045-50-9 - Calbiochem
5-[(5-Nitro-2-thiazolyl)thio]-1,3,4thiadiazol-2-amine
5-((5-Nitrothiazol-2-yl)thio)-1,3,4-thiadiazol-2-amine
2-Amino-5-[(5-nitro-2-thiazolyl)thio]-1,3,4-thiadiazole
1,3,4-Thiadiazol-2-amine, 5-[(5-nitro-2-thiazolyl)thio]-
5-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3,4-thiadiazol-2-amine
JNK,Thiadiazole,SU-3327,TNF-α,Inhibitor,inhibit,SU 3327,p38α,SU3327,insulin,phosphorylation,substrate-competitive,JIP,protein-protein,PPI
所屬類別
有機原料:雜環(huán)化合物

物理化學性質

熔點160 °C(dec.)
沸點549.8±42.0 °C(Predicted)
密度1.88±0.1 g/cm3(Predicted)
儲存條件Store at RT
溶解度DMSO : 62.5 mg/mL (239.19 mM; Need ultrasonic)
酸度系數(shù)(pKa)0.65±0.10(Predicted)
形態(tài)淡黃色固體
顏色淡黃色至琥珀色至深綠色
InChIInChI=1S/C5H3N5O2S3/c6-3-8-9-5(14-3)15-4-7-1-2(13-4)10(11)12/h1H,(H2,6,8)
InChIKeyNQQBNZBOOHHVQP-UHFFFAOYSA-N
SMILESS1C(SC2=NC=C([N+]([O-])=O)S2)=NN=C1N

安全數(shù)據

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H315-H319
海關編碼2934100090

常見問題列表

生物活性
SU3327 是一種有效的,選擇性的且具有底物競爭性的 JNK 抑制劑,IC50 為 0.7 μM。SU3327 還以 IC50 值為 239 nM 抑制 JNK 和 JIP 之間的蛋白相互作用。SU3327 對 p38α 和 Akt 激酶的活性較低。
靶點

IC50: 0.7 μM (JNK); 239 nM (JNK-JIP interactions)

體外研究

SU3327 (compound 9) is able to inhibit TNF-α stimulated phosphorylation of c-Jun in HeLa cells (EC 50 = 6.23 μM).
SU3327 (25 nM) pretreatment of human-derived cerebral microvascular endothelial cells (hCMEC/D3) effectively reduces LPS-induced polymorphonuclear leukocytes (PMN) rolling/adhesion to hCMEC/D3, prevents activation of AP-1, and significantly reduces expression of VCAM-1.

體內研究

SU3327 (Compound 9; 25 mg/kg; intraperitoneal injection; male BKS.Cg-+Lepr db /+Lepr db /OlaHsd db/db mice) treatment possesses the ability to restore insulin sensitivity in mice models of diabetes.
SU3327 (Compound 9) has favorable microsomal and plasma stability (T 1/2 = 27 min).

Animal Model: Male BKS.Cg-+Lepr db /+Lepr db /OlaHsd db/db mice (11-week-old ) injected with insulin
Dosage: 25 mg/kg
Administration: Intraperitoneal injection
Result: Resulted in a statistically significant reduction in blood glucose levels.
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