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| 产品编号 | 产品名称 | 产品包装 | 产品价格 |
| SM5156-10mM | 古伦宾(98%, HPLC) | 10mM×0.2ml | 104.00元 |
| SM5156-5mg | 古伦宾(98%, HPLC) | 5mg | 101.00元 |
| SM5156-25mg | 古伦宾(98%, HPLC) | 25mg | 420.00元 |
| SM5156-100mg | 古伦宾(98%, HPLC) | 100mg | 1428.00元 |
化学信息：
| 中文名 | 古伦宾 |
| 英文名 | Columbin |
| 中文别名 | 咖伦宾；青牛胆苦素 |
| 英文别名 | Tinosporin |
| 来源 | 青牛胆Tinospora sagittata (Oliv.) Gagnep. |
| 化合物类型 | 萜类(Terpenoids)>二萜 |
| 化学式 | C20H22O6 |
| 分子量 | 358.39 |
| CAS号 | 546-97-4 |
| 纯度 | 98%, HPLC |
| 溶剂/溶解度 | DMSO: ≥ 100 mg/ml (279.03 mM); Water: < 0.1 mg/ml (insoluble) |
| 溶液配制 | 5mg加入1.40ml DMSO，或者每3.58mg加入1ml DMSO，配制成10mM溶液。 |
生物信息
| 产品描述 | Columbin is an orally active diterpenoid furanolactone from Calumbae radix, has anti-inflammatory and anti-trypanosomal effects. Columbin selectively inhibits COX-2 (EC50=53.1 μM) over COX-1 (EC50=327 μM). | ||||
| 信号通路 | - | ||||
| 靶点 | COX-2 | COX-1 | - | - | - |
| IC50 | 53.1 μM | 327 μM | - | - | - |
| 体外研究 | 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. | ||||
| 体内研究 | 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. | ||||
| 临床实验 | N/A | ||||
1. Ibrahim Abdelwahab S, et al. Eur J Pharmacol. 2012,678(1-3):61-70.
2. A J Nok, et al. J Enzyme Inhib Med Chem. 2005,20(4):365-8.
3. Yang G, et al. J Chromatogr B Analyt Technol Biomed Life Sci. 2015,1002:13-8.
包装清单：| 产品编号 | 产品名称 | 包装 |
| SM5156-10mM | 古伦宾(98%, HPLC) | 10mM×0.2ml |
| SM5156-5mg | 古伦宾(98%, HPLC) | 5mg |
| SM5156-25mg | 古伦宾(98%, HPLC) | 25mg |
| SM5156-100mg | 古伦宾(98%, HPLC) | 100mg |
| - | 说明书 | 1份 |
-20℃保存，至少一年有效。固体粉末4℃保存，至少一个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：本产品可能对人体有一定的毒害作用，请注意适当防护，以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
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