2. Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. TNF Receptor Interleukin Related Toll-like Receptor (TLR) NF-κB NOD-like Receptor (NLR) Apoptosis Caspase Bcl-2 Family Reactive Oxygen Species
  4. L6H21

L6H21 是 Chalcone (HY-121054) 衍生物，是一种口服有效的特异性骨髓分化蛋白 (MD-2) 抑制剂。L6H21 高亲和力地直接与 MD-2 蛋白结合，KD 值为 33.3 μM，阻断 LPS-TLR4/MD-2 复合物形成。L6H21 抑制 LPS 诱导的 RAW264.7 巨噬细胞中 TNF-α 和 IL-6 的表达，IC50 分别为 6.58 和 8.59 μM。L6H21 可用于酒精性肝病、代谢紊乱和神经炎症的研究。

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L6H21 Chemical Structure

L6H21 Chemical Structure

CAS No. : 24533-47-9

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10 mM * 1 mL in DMSO ￥880
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Customer Review

L6H21 相关抗体

Top Publications Citing Use of Products

查看 TNF Receptor 亚型特异性产品:

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TNFRSF1A/CD120a TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

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TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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NLRP3 NLRP1 NOD1 NOD2

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

L6H21, a Chalcone (HY-121054) derivative, is an orally active, potent and specific myeloid differentiation 2 (MD-2) inhibitor. L6H21 directly binds to MD-2 protein with a high affinity and low KD value of 33.3 μM, blocking the formation of the LPS-TLR4/MD-2 complex. L6H21 inhibits LPS-induced expression of TNF-α and IL-6 in RAW264.7 macrophages, with IC50 values of 6.58 and 8.59 μM, respectively. L6H21 can be used for alcoholic liver disease, metabolic disturbance and neuroinflammation research[1][2][3].

IC50 & Target

IL-6

8.59 μM (IC50)

TLR4

 

NF-κB

 

NLRP3 inflammasome

 

IL-1β

 

Caspase 3

 

Bcl-2

 

Bax

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HT-29 IC50
41.74 μM
Compound: 27
Cytotoxicity against Homo sapiens (human) HT-29 cells after 72 hr by MTT assay
Cytotoxicity against Homo sapiens (human) HT-29 cells after 72 hr by MTT assay
10.1007/s00044-011-9549-9
Peritoneal macrophage IC50
10 μM
Compound: L6H21
Inhibition of LPS-induced IL-6 secretion in mouse primary peritoneal macrophages by ELISA
Inhibition of LPS-induced IL-6 secretion in mouse primary peritoneal macrophages by ELISA
[PMID: 36399795]
Peritoneal macrophage IC50
10 μM
Compound: L6H21
Inhibition of LPS-induced TNF-alpha secretion in mouse primary peritoneal macrophages by ELISA
Inhibition of LPS-induced TNF-alpha secretion in mouse primary peritoneal macrophages by ELISA
[PMID: 36399795]
SGC-7901 IC50
13.08 μM
Compound: 27
Cytotoxicity against Homo sapiens (human) SGC7901 cells after 72 hr by MTT assay
Cytotoxicity against Homo sapiens (human) SGC7901 cells after 72 hr by MTT assay
10.1007/s00044-011-9549-9
体外研究
(In Vitro)

L6H21 (10 μM, 2 h) inhibits EtOH + LPS-induced apoptosis and mitochondrial damage in RAW264.7 cells[1].
L6H21 (10 μM, 2 h) attenuates EtOH + LPS-induced ROS formation and TLR4–NF-κB activation, and decreases NLRP3 inflammasome activation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

L6H21 相关抗体:

Apoptosis Analysis[1]

Cell Line: RAW264.7 cells (mouse macrophage cell line)
Concentration: 10 μM
Incubation Time: 2 hours
Result: Markedly decreased apoptotic cell numbers; completely inhibited EtOH + LPS-induced increase in Bax/Bcl-2; markedly decreased EtOH + LPS-induced elevation in cleaved caspase-3 protein.

Western Blot Analysis[1]

Cell Line: RAW264.7 cells (mouse macrophage cell line)
Concentration: 10 μM
Incubation Time: 2 hours
Result: Reduced EtOH + LPS-induced TLR4–NF-κB signaling; completely inhibited the increase in TLR4 and NF-κB p65 nuclear level induced by EtOH and LPS. Attenuated EtOH + LPS-induced expression of NLRP3 inflammasome; inhibited the elevated NLRP3 and IL-1β protein expression; decreased the expression of p20, an active form of caspase-1.

Cell Viability Assay[1]

Cell Line: RAW264.7 cells (mouse macrophage cell line)
Concentration: 10 and 20 μM
Incubation Time: 2 hours
Result: The loss of cell viability by EtOH + LPS was prevented by L6H21 pretreatment. Slightly decreased cell viability a higher dose of 20 μM.
体内研究
(In Vivo)

L6H21 (10 mg/kg, Oral gavage, daily) effectively inhibits EtOH + LPS-induced hepatic fat accumulation, hepatic steatosis and liver injury[1].
L6H21 (0-40 mg/kg, Orally, daily for 4 weeks) attenuates metabolic disturbance, restores cognition and attenuates brain pathologies dose and time-dependently in HFD-fed rats, and shows neuroprotective effect in a model of prediabetes[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL6 mice (8-10 weeks old, n = 36, 8 mice in each group, 25-30 g, with EtOH and LPS)[1]
Dosage: 10 mg/kg
Administration: Oral gavage, daily, before EtOH feeding
Result: Decreased hepatic triglyceride (TG) concentration, markedly decreased serum alanine transaminase (ALT) and aspartate transaminase (AST) levels; Significantly decreased inflammation in liver tissue induced by EtOH + LPS.
Animal Model: Male Wistar rats (6-7 weeks old, 250 g, a normal diet (ND) (n=8) or a high-fat diet (HFD) (n=104) for 16 weeks)[2]
Dosage: 0, 10, 20, and 40 mg/kg
Administration: Orally, daily for 1, 2 or 4 weeks
Result: Ameliorated brain mitochondrial dysfunction in HFD-fed rats at 2-week administration time point; improved brain mitochondrial function in a dose-dependent manner for 4 weeks. Reduced hippocampal apoptosis in prediabetes for 4 weeks. Attenuated the reduction of dendritic spine volume and density for 4 weeks. Preserved microglial morphology in a dose-dependent manner.
分子量

298.34

Formula

C18H18O4
CAS 号
性状

固体

颜色

White to off-white

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (335.19 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3519 mL 16.7594 mL 33.5188 mL
5 mM 0.6704 mL 3.3519 mL 6.7038 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (8.38 mM); 澄清溶液; 超声助溶

    此方案可获得 2.5 mg/mL的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (8.38 mM); 澄清溶液; 超声助溶

    此方案可获得 2.5 mg/mL的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

L6H21 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3519 mL 16.7594 mL 33.5188 mL 83.7970 mL
5 mM 0.6704 mL 3.3519 mL 6.7038 mL 16.7594 mL
10 mM 0.3352 mL 1.6759 mL 3.3519 mL 8.3797 mL
15 mM 0.2235 mL 1.1173 mL 2.2346 mL 5.5865 mL
20 mM 0.1676 mL 0.8380 mL 1.6759 mL 4.1899 mL
25 mM 0.1341 mL 0.6704 mL 1.3408 mL 3.3519 mL
30 mM 0.1117 mL 0.5586 mL 1.1173 mL 2.7932 mL
40 mM 0.0838 mL 0.4190 mL 0.8380 mL 2.0949 mL
50 mM 0.0670 mL 0.3352 mL 0.6704 mL 1.6759 mL
60 mM 0.0559 mL 0.2793 mL 0.5586 mL 1.3966 mL
80 mM 0.0419 mL 0.2095 mL 0.4190 mL 1.0475 mL
100 mM 0.0335 mL 0.1676 mL 0.3352 mL 0.8380 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

L6H2124533-47-9TNF ReceptorInterleukin RelatedToll-like Receptor (TLR)NF-κBNOD-like Receptor (NLR)ApoptosisCaspaseBcl-2 FamilyReactive Oxygen SpeciesTumor Necrosis Factor ReceptorTNFRILNuclear factor-κBNuclear factor-kappaBAlcoholic Liver DiseaseLipopolysaccharideNLRP3 Inflammasomeneuroinflammationmetabolic disturbanceobesityRAW264.7MD-2myeloid differentiation factor 2cognitive deficitsInhibitorinhibitorinhibit

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