秋水仙鹼(Colchicine) | CAS#64-86-8 APExBIO貨號 A3324

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APExBIO系列商品->>秋水仙鹼(Colchicine) CAS#64-86-8
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秋水仙鹼(Colchicine) | CAS#64-86-8 APExBIO貨號 A3324
產品介紹
秋水仙鹼(Colchicine)是一種微管蛋白抑制劑 (tubulin inhibitor),透過與微管蛋白(microtubules) 結合來阻斷微管聚合(IC50 = 3.2 μM)。微管蛋白(microtubules) 是球狀蛋白小家族的幾個成員之一。微管蛋白超家族包含五個不同的家族。為了形成微管,α-和β-微管蛋白的二聚體與GTP結合,並在GTP結合狀態下組裝到微管的(+)端。 [1] β-微管蛋白亞基暴露在微管的正端,而α-微管蛋白亞基則暴露在負端。二聚體被整合到微管後,與β-微管蛋白亞基結合的GTP分子最終透過沿著微管原絲的二聚體間接觸水解為GDP。 [2] 這就是GTP循環,它對於微管的動態不穩定性至關重要。秋水仙鹼(Colchicine)透過與微管的主要成分之一微管蛋白結合來抑制微管聚合。微管蛋白的可用性對於有絲分裂至關重要,因此秋水仙鹼有效地發揮了「有絲分裂毒」或紡錘體毒的作用。 [3] 因此,有絲分裂可以在細胞週期中期(特別是中期)完成之前停止。除了抑制有絲分裂外,秋水仙鹼還能抑制嗜中性球的運動和活性,在小鼠痛風性關節炎模型中,5 μmol/kg 劑量的秋水仙鹼可產生淨抗發炎作用,並抑制尿酸沉積,這是痛風治療的關鍵方面。 [4] 副作用包括胃腸不適和嗜中性白血球減少症。高劑量也會損害骨髓(bone marrow ),導致貧血( anemia)和掉髮。

References:
1. Heald R, Nogales E. “Microtubule dynamics”. J. Cell. Sci. 2002,115 (Pt 1): 3–4.
2. Howard J, Hyman A. “Dynamics and mechanics of the microtubule plus end”. Nature 2003,422 (6933): 753–8.
3. “Information for Healthcare Professionals: New Safety Information for Colchicine (marketed as Colcrys)”. U.S. Food and Drug Administration.
4. Chen LX, Schumacher HR. “Gout: an evidence-based review”. J Clin Rheumatol 2008, 14: S55–62.
5. Colchicine. National Institute for Occupational Safety and Health. Emergency Response Safety and Health Database, August 22, 2008. Retrieved December 23, 2008.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 399.44 |
| Cas No. | 64-86-8 |
| Formula | C22H25NO6 |
| Solubility | ≥19.97 mg/mL in DMSO; ≥45.5 mg/mL in H2O with gentle warming; ≥50.8 mg/mL in EtOH with gentle warming |
| Chemical Name | N-[(7S)-1,2,3,10-tetramethoxy-9-oxo-6,7-dihydro-5H-benzo[a]heptalen-7-yl]acetamide |
| SDF | Download SDF |
| Canonical SMILES | COC1=C(C(C([C@@H](NC(C)=O)CC2)=C3)=CC=C(OC)C3=O)C2=CC(OC)=C1OC |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
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