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My CartCAS：220119-17-5
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 220119-17-5 |
| Name | Selamectin |
| Molecular Formula | C43H63NO11 |
| Molecular Weight | 769.96 |
| Solubility | Soluble in DMSO ≥10mg/mL |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD31621085 |
| SMILES | CC1CCC2(CC3CC(O2)CC=C(C(C(C=CC=C4COC5C4(C(C=C(C5=NO)C)C(=O)O3)O)C)OC6CC(C(C(O6)C)O)OC)C)OC1C7CCCCC7 |
| InChIKey | AFJYYKSVHJGXSN-XHKIUTQPSA-N |
| InChI | InChI=1S/C43H63NO11/c1-24-11-10-14-30-23-50-40-36(44-48)27(4)19-33(43(30，40)47)41(46)52-32-20-31(16-15-25(2)38(24)53-35-21-34(49-6)37(45)28(5)51-35)54-42(22-32)18-17-26(3)39(55-42)29-12-8-7-9-13-29/h10-11，14-15，19，24，26，28-29，31-35，37-40，45，47-48H，7-9，12-13，16-18，20-23H2，1-6H3/b11-10+，25-15+，30-14+，44-36-/t24-，26-，28-，31+，32-，33-，34-，35-，37-，38-，39-，40+，42+，43+/m0/s1 |
| PubChem CID | 9578507 |
| Target Point | Parasite;Chloride Channel;P-glycoprotein |
| Passage | Anti-infection;Membrane Transporter&Ion Channel |
| Background | Selamectin is a macrolide with antiparasitic activity. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent filariasis, lymphatic filariasis, and nematode infection. Selamectin is an active P-glycoprotein substrate and inhibitor. |
| Biological Activity | Selamectin 是一种半合成大环内酯，是一种强效杀寄生虫剂和驱虫药。可激活神经元和咽部肌肉中的谷氨酸门控氯离子通道，预防心丝虫、淋巴丝虫和线虫感染，还是一种强效的 P 糖蛋白底物和 P 糖蛋白抑制剂，IC50 为 120 nM。[1-2] |
| In Vitro | 放射性标记的塞拉菌素通过 Caco-2 单层膜的转运表明，塞拉菌素是强效的P-gp抑制剂，其IC50值为0.1微米。塞拉菌素强效的是 P-gp 底物，其分泌/吸收比为 4.7 。P-gp抑制剂维拉帕米可阻断[3H]-伊维菌素和[3H]-塞拉菌素的分泌转运。[2] |
| In Vivo | 每两个月单次施用 6 毫克/千克的局部塞拉菌素可有效预防马来丝虫感染。每年两次外用塞拉菌素可阻断循环中的微丝蚴。[1] |
| Data Literature Source | [1]. Sarasombath PT，et al. First study of topical selamectin efficacy for treating cats naturally infected with Brugia malayi and Brugia pahangi under field conditions. Parasitol Res. 2019 Apr;118(4):1289-1297. [2]. Griffin J，et al. Selamectin is a potent substrate and inhibitor of human and canine P-glycoprotein. J Vet Pharmacol Ther. 2005 Jun;28(3):257-65. |
| Unit | Bottle |
| Specification | 5mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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