Motolimod|926927-61-9|(VTX-2337; VTX-378)-陌孚医药/Medlife

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Motolimod (Synonyms: VTX-2337; VTX-378)

目录号: PL12319 纯度: ≥99%

CAS No. :926927-61-9

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PL12319-100mg	100mg	询价	询价
PL12319-200mg	200mg	询价	询价
PL12319-10mM*1mLinDMSO	10mM*1mLinDMSO	¥2431.00	请登录

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中文名称	Motolimod
中文别名	Motolimod(VTX-2337) 抑制剂
英文名称	Motolimod
英文别名	2-amino-N,N-dipropyl-8-[4-(pyrrolidine-1-carbonyl)phenyl]-3H-1-benzazepine-4-carboxamide;VTX-2337;SureCN254984;UNII-WP6PY72ZH3;AGN-PC-00S5DG;VTX-378;KB-146010;3H-1-Benzazepine-4-carboxamide, 2-amino-n,N-dipropyl-8-(4-(1-pyrrolidinylcarbonyl)phenyl)-;Motolimod;2-amino-N,N-dipropyl-8-(4-(pyrrolidine-1-carbonyl)phenyl)-3H-benzo[b]azepine-4-carboxamide;Motolimod (VTX-2337);3H-1-Benzazepine-4-carboxamide,2-amino-n,N-dipropyl-8-(4-(1-pyrrolidinylcarbonyl)phenyl);VTX 2337;WP6PY72ZH3;AK171372;Motolimod [USAN:INN];Motolimod (USAN/INN);GTPL9026;BCP16667;s7161;SB16930;DB12303;J3.657.311B;D10716;Q27087722;2-Amino-N,N-dipropyl-8-[4-(1-pyrrolidinylcarbonyl);2-Amino-N,N-dipropyl-8-[4-(1-pyrrolidinylcarbonyl)phenyl]-3H-1-benzazepine-4-carboxamide (ACI);2-Amino-N,N-dipropyl-8-[4-(pyrrolidine-1-carbonyl)phenyl]-3H-1-benzazepine-4-carboxamide;2-Amino-N,N-dipropyl-8-[4-(pyrrolidine-1-carbonyl)phenyl]-3H-benzo[b]azepine-4-carboxamide;VTX 378
Cas No.	926927-61-9
分子式	C₂₈H₃₄N₄O₂
分子量	458.60
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Motolimod (VTX-2337;VTX-378) 是选择性的Toll样受体 8 (TLR8) 激动剂，EC₅₀约为 100 nM。

生物活性

Motolimod (VTX-2337;VTX-378) is a selective Toll-like receptor 8 (TLR8) agonist, with an EC 50 of approximately 100 nM.

性状

Solid

IC50 & Target[1][2]

EC50: 100 nM (TLR8)

体外研究(In Vitro)

Among the TLRs tested (TLR2, 3, 4, 5, 7, 8, and 9), Motolimod (VTX-2337) selectively activates TLR8. Motolimod stimulates the production of both TNFα (EC50=140±30 nM based on 10 donors) and IL-12 (EC50=120±30 nM based on 10 donors) in PBMCs. The EC50 value for MIP-1β induction is 60 nM for Motolimod. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Monkeys receive a subcutaneous injection of Motolimod (1 or 10 mg/kg), and plasma is collected predose, 6, 12, 24, and 96 h post-injection. For the 10 mg/kg dose, mean plasma levels of IL-1β increase from baseline levels of 0.5 pg/mL, up to 9.12±2.7 ng/mL (p<0.05, t-test) at 6 h post-administration of Motolimod (10 mg/kg). Circulating levels of IL-18 also increase from a baseline of ~ 1 pg/mL to 68.7±4.4 pg/mL (p<0.05, t-test) at 6 h in response to the Motolimod (VTX-2337) treatment (10 mg/kg). Levels of IL-6 are monitored, as this mediator is induced in response to TLR8 activation, but the release is independent of NLRP3 inflammasome activation. In addition, plasma levels of IFNγ are assessed as a measure of NK cell activation in response to Motolimod treatment. has not independently confirmed the accuracy of the

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Lu H, et al. VTX-2337 is a novel TLR8 agonist that activates NK cells and augments ADCC. Clin Cancer Res. 2012 Jan 15;18(2):499-509.
[2]. Dietsch GN, et al. Coordinated Activation of Toll-Like Receptor8 (TLR8) and NLRP3 by the TLR8 Agonist, VTX-2337, Ignites Tumoricidal Natural Killer Cell Activity. PLoS One. 2016 Feb 29;11(2):e0148764.

溶解度数据	In Vitro: DMSO : 50 mg/mL (109.03 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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