546-97-4
基本信息
古伦宾
古伦宾对照品
非洲防己苦素
古伦宾, 来源于青牛胆
COLUMBIN 古伦宾
青牛胆苦素、黄藤内酯、防己内酯、非洲防己苦素
Columbin USP/EP/BP
Columbin >=95% (LC/MS-ELSD)
Columbin, 98%, from limacia sagittata
(1R,2S,3S,5S,8R,11R,12R)-5-(3-Furyl)-12-hydroxy-3,11-dimethyl-6,14-dioxatetracyclo[10.2.2.02,11.03,8]hexadec-15-ene-7,13-dione
(1s,2s,3s,5s,8r,11r,12s)-5-(3-furyl)-12-hydroxy-3,11-dimethyl-6,14-dioxatetracyclo[10.2.2.02,11.03,8]hexadec-15-ene-7,13-dione
(1R,4R,4aR,6aR,9S,10aS,10bS)-9-(3-Furanyl)decahydro-4-hydroxy-4a,10a-dimethyl-1,4-etheno-3H,7H-benzo[1,2-c:3,4-c']dipyran-3,7-dione
(1R,2S,3S,5S,8R,11R,12R)-5-(3-Furyl)-12-hydroxy-3,11-dimethyl-6,14-dioxatetracyclo[10.2.2.02,11.03,8]hexadec-15-ene-7,13-dione
(1R,4R,4aR,6aR,9S,10aS,10bS)-9-(3-Furanyl)-1,4,4a,5,6,6a,9,10,10a,10b-decahydro-4-hydroxy-4a,10a-dimethyl-1,4-etheno-3H,7H-benzo[1,2-c:3,4-c']dipyran-3,7-dione
1,4-Etheno-3H,7H-benzo[1,2-c:3,4-c']dipyran-3,7-dione, 9-(3-furanyl)-1,4,4a,5,6,6a,9,10,10a,10b-decahydro-4-hydroxy-4a,10a-dimethyl-, (1R,4R,4aR,6aR,9S,10aS,10bS)-
物理化学性质
| 外观性状 | 白色针状结晶，易溶于甲醇、乙酸乙酯，几乎不溶于水，来源于金国榄。 |
| 熔点 | 190-191℃ |
| 比旋光度 | D +52.5° (pyridine) |
| 沸点 | 410.82°C (rough estimate) |
| 密度 | 1.36 |
| 折射率 | 1.4450 (estimate) |
| 储存条件 | ?20°C |
| 溶解度 | DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 0.03 mg/ml |
| 酸度系数(pKa) | 12.14±0.70(Predicted) |
| 形态 | Cryst. |
| 颜色 | White to off-white |
应用领域
安全数据
| WGK Germany | 3 |
| 海关编码 | 29322090 |
常见问题列表
|
COX-2 53.1 μM (EC 50 ) |
COX-1 327 μM (EC 50 ) |
Treatment with columbin or l-NAME inhibits LPS/IFN-γ-induced NO production without affecting the viability of RAW264.7. Pre-treatment of stimulated cells with columbin does not inhibit the translocation of NF-κB to the nucleus in LPS-stimulated cells. COX-1 and COX-2 inhibitory activities of columbin are 63.7±6.4% and 18.8±1.5% inhibition at 100μM, respectively. The interaction of columbin with Tyr385 and Arg120 signifies its higher activity in COX-2, as Tyr385 is reported to be involved in the abstraction of hydrogen from C-13 of arachidonate, and Arg120 is critical for high affinity arachidonate binding.
Columbin inhibits oedema formation in mice paw. At doses of 300 mg/kg and 700 mg/kg, columbin inhibits inflammation from 0 to 5 h and the results are comparable to that of aspirin as a standard anti-inflammatory drug. The inhibitory effect of columbin on carrageenan induced paw oedema in mice may be due to the suppression of the release of mediators responsible for inflammation including prostaglandin. Columbin is poorly bioavailable (2.8% p.o. and 14% i.p.) in rats, but its transport is rapid across the Caco-2 cell monolayers, suggesting that extensive first-pass metabolism in the liver is the likely reason for its poor bioavailability.
古伦宾价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/08/19 | S9167 | 古伦宾 Columbin | 546-97-4 | 1mg | 1204.64元 |