251992-66-2
中文名稱
4-[(4-甲基苯基)硫基]噻吩并[2,3-C]吡啶-2-甲酰胺
英文名稱
A 205804
CAS
251992-66-2
分子式
C15H12N2OS2
分子量
300.405
MOL 文件
251992-66-2.mol
更新日期
2024/06/12 17:31:26
251992-66-2 結(jié)構(gòu)式
基本信息
中文別名
4-(對(duì)甲苯硫基)噻吩并[2,3-C]吡啶-2-甲酰胺4-(P-甲苯基硫)噻吩并[2,3-C]吡啶-2-甲酰胺
4-[(4-甲基苯基)硫基]噻吩并[2,3-C]吡啶-2-甲酰胺
4-(P-甲苯基硫)噻吩并[2,3-C]吡啶-2-甲酰胺
英文別名
CS-635A 205804
A-205804
A 205804
A 205804 USP/EP/BP
A205804
A 205804
A-205804
IKK-16 (IKK Inhibitor VII)
4-(p-tolylthio)thieno[2,3-c]pyridine-2-carboxamide
4-[(4-Methylphenyl)thio]thieno[2,3-c]pyridine-2-carboxamide
Thieno[2,3-c]pyridine-2-carboxamide, 4-[(4-methylphenyl)thio]-
4-[(4-methylphenyl)sulfanyl]thieno[2,3-c]pyridine-2-carboxam...
所屬類別
生物化工：Integrin 抑制劑物理化學(xué)性質(zhì)
熔點(diǎn)198-199℃
沸點(diǎn)581.3±45.0 °C(Predicted)
密度1.40±0.1 g/cm3(Predicted)
儲(chǔ)存條件Sealed in dry,2-8°C
儲(chǔ)存條件Store at +4°C
溶解度≥30 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
酸度系數(shù)(pKa)15.12±0.30(Predicted)
形態(tài)粉末晶體
顏色白色至橙色再至綠色
常見(jiàn)問(wèn)題列表
生物活性
A-205804 是抑制 E-selectin 和 ICAM-1 表達(dá)的口服有效的，高效、選擇性的先導(dǎo)抑制劑，對(duì) E-selectin 和 ICAM-1 作用的 IC50 分別為 20 nM 和 25 nM。A-205804 可用于慢性炎癥疾病的研究。靶點(diǎn)
IC50: 20 nM (E-selectin), 25 nM (ICAM-1)
體外研究
A-205804 exhibits Cellular Toxicities for HUVEC with an IC
50
of 152 μM.
A-205804 is an effective inhibitor of cell-cell adhesion in an in vitro flow experiment, demonstrating relevance in a model physiological system.
體內(nèi)研究
A-205804 (5 mg/kg; p.o.) shows a half-life of 1 hour for rat.
A-205804 (10 mg/kg; p.o.; 3 times per week; for 2 weeks) attenuates the E-selectin expression on the endothelial vascular niche cells in mice.
| Animal Model: | C57BL/6 mice |
| Dosage: | 10 mg/kg |
| Administration: | Oral administration, 3 times per week, for 2 weeks |
| Result: | Efficiently decreased the expression of E-selectin on the endothelial vascular niche cells |
| Animal Model: | Rat |
| Dosage: | 5 mg/kg (Pharmacokinetic Analysis) |
| Administration: | Oral administration |
| Result: | t 1/2 = 1 hour |