Miravirsen (SPC-3649)

miR-122[1]

Miravirsen 的主要作用机制被认为是与成熟的 miR-122 杂交并防止其与 HCV RNA 相互作用； pri- 和 pre-miR-122 均包含其靶序列[1]。 miravirsen 具有纳摩尔亲和力，可与 pri-和 pre-miR-122 的茎环结构结合，阻止 Drosha 和 Dicer 处理 miR-122 前体[1]。

在小鼠中，miravirsen（SPC-3649；2.5–25 mg/kg；静脉注射；每天一次，持续 3 天）可抑制 miR-122 活性[2]。

动物/疾病模型： NMRI雌性小鼠（27 g）[2]
剂量： 2.5、6.25、12.5和25 mg/kg
给药途径： 静脉注射；每日一次，连续3天
实验结果： 以剂量依赖的方式抑制miR-122活性。

[1]. Miravirsen (SPC3649) can inhibit the biogenesis of miR-122. Nucleic Acids Res. 2014 Jan;42(1):609-21.

[2]. Antagonism of microRNA-122 in mice by systemically administered LNA-antimiR leads to up-regulation of a large set of predicted target mRNAs in the liver. Nucleic Acids Res. 2008 Mar;36(4):1153-62.

Miravirsen 已被研究用于治疗丙型肝炎和慢性丙型肝炎。

C151H185N49O83P14S14

4896.90576338768

4894.421

1072874-90-8

56843415

Off-white to light yellow solid powder

-12.2

2150

32

111

86

311

14200

0

S=P(O)(OCC12COC(C(N3C(NC(C(C)=C3)=O)=O)O1)C2OP(O)(OCC1C(CC(N2C(N=C(C=C2)N)=O)O1)OP(O)(OCC1C(CC(N2C=NC3C(N)=NC=NC2=3)O1)OP(O)(OCC12COC(C(N3C(N=C(C=C3)N)=O)O1)C2OP(O)(OCC1C(CC(N2C=NC3C(N)=NC=NC2=3)O1)OP(O)(OCC12COC(C(N3C(N=C(C=C3)N)=O)O1)C2OP(O)(OCC1C(CC(N2C(NC(C(C)=C2)=O)=O)O1)OP(O)(OCC12COC(C(N3C(N=C(C=C3)N)=O)O1)C2OP(O)(OCC12COC(C(N3C(N=C(C=C3)N)=O)O1)C2O)=S)=S)=S)=S)=S)=S)=S)=S)OC1C2C(N3C=NC4C(NC(N)=NC3=4)=O)OC1(COP(O)(OC1CC(N3C(NC(C(C)=C3)=O)=O)OC1COP(O)(OC1CC(N3C(NC(C(C)=C3)=O)=O)OC1COP(O)(OC1C3C(N4C=NC5C(N)=NC=NC4=5)OC1(COP(O)(OC1CC(N4C(N=C(C=C4)N)=O)OC1COP(O)(OC1C4C(N5C(N=C(C=C5)N)=O)OC1(CO)CO4)=S)=S)CO3)=S)=S)=S)CO2

OSOOBMBDIGGTCP-UHFFFAOYSA-N

InChI=1S/C151H185N49O83P14S14/c1-60-26-193(140(215)182-119(60)203)87-21-66(74(258-87)34-245-290(225,304)281-110-102-130(199-58-171-94-114(161)165-55-168-117(94)199)268-150(110,44-239-102)50-252-291(226,305)272-65-20-86(187-13-6-79(153)174-134(187)209)256-72(65)33-243-286(221,300)277-105-97-125(262-144(105,37-201)38-234-97)189-15-8-81(155)176-136(189)211)271-285(220,299)241-30-73-67(22-88(257-73)194-27-61(2)120(204)183-141(194)216)273-293(228,307)253-51-151-45-240-103(131(269-151)200-59-172-95-118(200)180-132(162)181-123(95)207)111(151)283-297(232,311)254-52-149-43-238-101(129(267-149)196-29-63(4)122(206)185-143(196)218)109(149)280-289(224,303)244-32-71-64(19-85(255-71)186-12-5-78(152)173-133(186)208)270-284(219,298)242-31-76-69(24-90(260-76)197-56-169-92-112(159)163-53-166-115(92)197)275-294(229,308)249-47-147-41-236-99(127(265-147)191-17-10-83(157)178-138(191)213)107(147)279-288(223,302)247-36-77-70(25-91(261-77)198-57-170-93-113(160)164-54-167-116(93)198)276-295(230,309)250-48-146-40-235-98(126(264-146)190-16-9-82(156)177-137(190)212)106(146)278-287(222,301)246-35-75-68(23-89(259-75)195-28-62(3)121(205)184-142(195)217)274-292(227,306)251-49-148-42-237-100(128(266-148)192-18-11-84(158)179-139(192)214)108(148)282-296(231,310)248-46-145-39-233-96(104(145)202)124(263-145)188-14-7-80(154)175-135(188)210/h5-18,26-29,53-59,64-77,85-91,96-111,124-131,201-202H,19-25,30-52H2,1-4H3,(H,219,298)(H,220,299)(H,221,300)(H,222,301)(H,223,302)(H,224,303)(H,225,304)(H,226,305)(H,227,306)(H,228,307)(H,229,308)(H,230,309)(H,231,310)(H,232,311)(H2,152,173,208)(H2,153,174,209)(H2,154,175,210)(H2,155,176,211)(H2,156,177,212)(H2,157,178,213)(H2,158,179,214)(H2,159,163,166)(H2,160,164,167)(H2,161,165,168)(H,182,203,215)(H,183,204,216)(H,184,205,217)(H,185,206,218)(H3,162,180,181,207)

1-[4-[[3-[[3-(2-amino-6-oxo-1H-purin-9-yl)-7-[[7-[[5-(4-amino-2-oxopyrimidin-1-yl)-3-[[3-[[3-(4-amino-2-oxopyrimidin-1-yl)-7-[[3-[[3-(4-amino-2-oxopyrimidin-1-yl)-7-[[3-[[3-(4-amino-2-oxopyrimidin-1-yl)-7-[[3-(4-amino-2-oxopyrimidin-1-yl)-7-hydroxy-2,5-dioxabicyclo[2.2.1]heptan-1-yl]methoxy-hydroxyphosphinothioyl]oxy-2,5-dioxabicyclo[2.2.1]heptan-1-yl]methoxy-hydroxyphosphinothioyl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphinothioyl]oxy-2,5-dioxabicyclo[2.2.1]heptan-1-yl]methoxy-hydroxyphosphinothioyl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphinothioyl]oxy-2,5-dioxabicyclo[2.2.1]heptan-1-yl]methoxy-hydroxyphosphinothioyl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphinothioyl]oxyoxolan-2-yl]methoxy-hydroxyphosphinothioyl]oxy-3-(5-methyl-2,4-dioxopyrimidin-1-yl)-2,5-dioxabicyclo[2.2.1]heptan-1-yl]methoxy-hydroxyphosphinothioyl]oxy-2,5-dioxabicyclo[2.2.1]heptan-1-yl]methoxy-hydroxyphosphinothioyl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphinothioyl]oxy-5-[[[1-[[[5-(4-amino-2-oxopyrimidin-1-yl)-2-[[[3-(4-amino-2-oxopyrimidin-1-yl)-1-(hydroxymethyl)-2,5-dioxabicyclo[2.2.1]heptan-7-yl]oxy-hydroxyphosphinothioyl]oxymethyl]oxolan-3-yl]oxy-hydroxyphosphinothioyl]oxymethyl]-3-(6-aminopurin-9-yl)-2,5-dioxabicyclo[2.2.1]heptan-7-yl]oxy-hydroxyphosphinothioyl]oxymethyl]oxolan-2-yl]-5-methylpyrimidine-2,4-dione

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : 100 mg/mL (20.13 mM)

配方 1 中的溶解度: 14.29 mg/mL (2.88 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶。

---

请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。