TLR9

当用阿吉莫德钠 (ODN 7909) (10 μg/mL) 处理 24 和 48 小时时，放射抗性人肺腺癌细胞系变得更加放射敏感，因为它会导致 TLR9 过度表达 [1]。

[1]. CpG-ODN 7909 increases radiation sensitivity of radiation-resistant human lung adenocarcinoma cell line by overexpression of Toll-like receptor 9. Cancer Biother Radiopharm. 2013 Sep;28(7):559-64.

[2]. Safety and immunogenicity of CPG 7909 injection as an adjuvant to Fluarix influenza vaccine. Vaccine. 2004 Aug 13;22(23-24):3136-43.

Agatolimod Sodium is the tricosasodium salt of a synthetic 24-mer oligonucleotide containing 3 CpG motifs with potential antineoplastic and immunostimulatory activity. Agatolimod selectively targets Toll-like receptor 9 (TLR9), thereby activating dendritic and B cells and stimulating cytotoxic T cell and antibody responses against tumor cells bearing tumor antigens.

C238H291N75O127P23S23-23.23[NA+]

8212.94

8202.251

541547-35-7

Agatolimod;525625-52-9

70687254

White to off-white solid powder

3390

32

168

140

508

23200

72

O=C1N(C2CC(OP(=S)(OCC3C(OP(=S)(OCC4OC(N5C=NC6=C5N=C(NC6=O)N)CC4OP(=S)(OCC4OC(N5C(=O)NC(=O)C(C)=C5)CC4OP(=S)(OCC4C(OP(OCC5C(OP(=S)(OCC6C(OP(OCC7OC(N8C(=O)NC(=O)C(C)=C8)CC7O)([O-])=S)CC(N7C(=O)NC(=O)C(C)=C7)O6)[O-])CC(N6C7=C(C(=O)NC(N)=N7)N=C6)O5)([O-])=S)CC(N5C=CC(N)=NC5=O)O4)[O-])[O-])[O-])CC(N4C(=O)N=C(N)C(C)=C4)O3)[O-])C(COP(OC3CC(N4C=C(C)C(N)=NC4=O)OC3COP(=S)(OC3CC(N4C(=O)N=C(N)C(C)=C4)OC3COP(=S)(OC3CC(N4C=NC5=C4N=C(N)NC5=O)OC3COP(OC3CC(N4C=CC(N)=NC4=O)OC3COP(=S)(OC3CC(N4C(=O)NC(=O)C(C)=C4)OC3COP(OC3C(COP(OC4CC(N5C=C(C)C(=O)NC5=O)OC4COP(=S)(OC4C(COP(=S)(OC5C(COP(OC6CC(N7C(=O)N=C(N)C(C)=C7)OC6COP(OC6C(COP(OC7CC(N8C(=O)N=C(N)C=C8)OC7COP(OC7CC(N8C=C(C)C(=O)NC8=O)OC7COP(OC7C(COP(=S)(OC8C(COP(OC9CC(N%10C(=O)NC(=O)C(C)=C%10)OC9CO)([O-])=S)OC(N9C(=O)N=C(N)C=C9)C8)[O-])OC(N8C9=C(C(=O)NC(=N9)N)N=C8)C7)([O-])=S)([O-])=S)([O-])=S)OC(N7C=NC(C(NC(N)=C)=O)=C7C)C6)([O-])=S)([O-])=S)OC(N6C=C(C)C(N)=NC6=O)C5)[O-])OC(N5C=C(C)C(=O)NC5=O)C4)[O-])([O-])=S)OC(N4C=NC5=C4N=C(NC5=O)N)C3)([O-])=S)[O-])([O-])=S)[O-])[O-])([O-])=S)O2)C=C(C)C(N)=N1.[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]

QUWFSKKBMDKAHK-SBOJBMMISA-A

InChI=1S/C236H303N70O133P23S23.23Na/c1-91-47-287(223(333)269-193(91)309)157-23-105(308)130(394-157)62-370-440(347,463)418-107-25-158(283-19-15-153(237)253-219(283)329)395-131(107)63-372-457(364,480)434-123-41-175(301-85-247-181-187(301)257-213(241)263-207(181)323)412-148(123)80-388-452(359,475)429-118-36-170(296-56-100(10)202(318)278-232(296)342)400-136(118)68-376-442(349,465)419-109-27-160(285-21-17-155(239)255-221(285)331)397-133(109)65-374-459(366,482)436-125-43-177(303-87-249-183-189(303)259-215(243)265-209(183)325)413-149(125)81-389-455(362,478)432-121-39-173(299-59-103(13)205(321)281-235(299)345)407-143(121)75-383-447(354,470)424-114-32-166(292-52-96(6)198(314)274-228(292)338)403-139(114)71-379-445(352,468)422-113-31-165(291-51-95(5)197(313)273-227(291)337)406-142(113)74-382-450(357,473)427-117-35-169(295-55-99(9)201(317)277-231(295)341)410-146(117)78-386-462(369,485)439-128-46-180(306-90-252-186-192(306)262-218(246)268-212(186)328)416-152(128)84-392-454(361,477)431-120-38-172(298-58-102(12)204(320)280-234(298)344)402-138(120)70-378-444(351,467)421-110-28-161(286-22-18-156(240)256-222(286)332)398-134(110)66-375-460(367,483)437-126-44-178(304-88-250-184-190(304)260-216(244)266-210(184)326)414-150(126)82-390-456(363,479)433-122-40-174(300-60-104(14)206(322)282-236(300)346)408-144(122)76-384-448(355,471)425-115-33-167(293-53-97(7)199(315)275-229(293)339)404-140(115)72-380-446(353,469)423-112-30-164(290-50-94(4)196(312)272-226(290)336)405-141(112)73-381-449(356,472)426-116-34-168(294-54-98(8)200(316)276-230(294)340)409-145(116)77-385-461(368,484)438-127-45-179(305-89-251-185-191(305)261-217(245)267-211(185)327)415-151(127)83-391-453(360,476)430-119-37-171(297-57-101(11)203(319)279-233(297)343)401-137(119)69-377-443(350,466)420-108-26-159(284-20-16-154(238)254-220(284)330)396-132(108)64-373-458(365,481)435-124-42-176(302-86-248-182-188(302)258-214(242)264-208(182)324)411-147(124)79-387-451(358,474)428-111-29-163(289-49-93(3)195(311)271-225(289)335)399-135(111)67-371-441(348,464)417-106-24-162(393-129(106)61-307)288-48-92(2)194(310)270-224(288)334;;;;;;;;;;;;;;;;;;;;;;;/h15-22,47-60,85-90,105-152,157-180,307-308H,23-46,61-84H2,1-14H3,(H,347,463)(H,348,464)(H,349,465)(H,350,466)(H,351,467)(H,352,468)(H,353,469)(H,354,470)(H,355,471)(H,356,472)(H,357,473)(H,358,474)(H,359,475)(H,360,476)(H,361,477)(H,362,478)(H,363,479)(H,364,480)(H,365,481)(H,366,482)(H,367,483)(H,368,484)(H,369,485)(H2,237,253,329)(H2,238,254,330)(H2,239,255,331)(H2,240,256,332)(H,269,309,333)(H,270,310,334)(H,271,311,335)(H,272,312,336)(H,273,313,337)(H,274,314,338)(H,275,315,339)(H,276,316,340)(H,277,317,341)(H,278,318,342)(H,279,319,343)(H,280,320,344)(H,281,321,345)(H,282,322,346)(H3,241,257,263,323)(H3,242,258,264,324)(H3,243,259,265,325)(H3,244,260,266,326)(H3,245,261,267,327)(H3,246,262,268,328);;;;;;;;;;;;;;;;;;;;;;;/q;23*+1/p-23/t105-,106-,107-,108-,109-,110-,111-,112-,113-,114-,115-,116-,117-,118-,119-,120-,121-,122-,123-,124-,125-,126-,127-,128-,129+,130+,131+,132+,133+,134+,135+,136+,137+,138+,139+,140+,141+,142+,143+,144+,145+,146+,147+,148+,149+,150+,151+,152+,157+,158+,159+,160+,161+,162+,163+,164+,165+,166+,167+,168+,169+,170+,171+,172+,173+,174+,175+,176+,177+,178+,179+,180+,440?,441?,442?,443?,444?,445?,446?,447?,448?,449?,450?,451?,452?,453?,454?,455?,456?,457?,458?,459?,460?,461?,462?;;;;;;;;;;;;;;;;;;;;;;;/m0......................./s1

tricosasodium;1-[(2R,4S,5R)-5-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-2-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-2-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-2-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-2-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-2-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-2-[[[(2R,3S,5R)-2-[[[(2R,3S,5R)-2-(hydroxymethyl)-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-3-yl]oxy-oxidophosphinothioyl]oxymethyl]-4-hydroxyoxolan-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

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

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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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。