1. Anti-infection Apoptosis Immunology/Inflammation
  2. Parasite Bacterial TNF Receptor Interleukin Related
  3. Diethylcarbamazine

Diethylcarbamazine is an orally active microfilaricidal agent used originally in onchocerciasis and lymphatic filiariasis. Diethylcarbamazine reduces eosinophil trafficking to the lung tissue and exerts anti-allergic effects. Diethylcarbamazine reduces serum levels of leptin, TNF-α, IL-6, MCP-1, glucose, insulin, and triglycerides, and ameliorates insulin resistance without altering body, liver, or adipose tissue weights. Diethylcarbamazine enhances reactive oxygen intermediate expression by polymorphonuclear neutrophils, increases lymphocyte proliferation, and inhibits actinomycetoma lesion development. Diethylcarbamazine can be used for the researches of bronchial asthma, insulin resistance and infection.

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Diethylcarbamazine

Diethylcarbamazine 構造式

CAS 番号 : 90-89-1

容量 価格(税別) 在庫状況 数量
Solid or liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 38 在庫あり
Solution
10 mM * 1 mL in DMSO USD 38 在庫あり
Solid or liquid
100 mg $35 在庫あり
500 mg $85 在庫あり
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Based on 1 publication(s) in Google Scholar

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製品説明

Diethylcarbamazine is an orally active microfilaricidal agent used originally in onchocerciasis and lymphatic filiariasis. Diethylcarbamazine reduces eosinophil trafficking to the lung tissue and exerts anti-allergic effects. Diethylcarbamazine reduces serum levels of leptin, TNF-α, IL-6, MCP-1, glucose, insulin, and triglycerides, and ameliorates insulin resistance without altering body, liver, or adipose tissue weights. Diethylcarbamazine enhances reactive oxygen intermediate expression by polymorphonuclear neutrophils, increases lymphocyte proliferation, and inhibits actinomycetoma lesion development. Diethylcarbamazine can be used for the researches of bronchial asthma, insulin resistance and infection[1][2][3].

IC50 & Target[1]

IL-6

 

体外実験

Diethylcarbamazine (0-40 mM; 60 min) cross-reacts with rabbit anti-MPCA-BSA polyclonal IgG antibodies in an inhibition ELISA[1].

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

体内実験

Diethylcarbamazine (citrate) (12 mg/kg; p.o.) exerts anti-allergic effects in Ovalbumin (HY-W250978)-induced asthmatic mice, with pre-treatment with 40 mg/kg quercetin significantly potentiating these effects, as evidenced by reduced serum Th2 cytokines, BALF IgE, lung eosinophil markers, and complete resolution of histopathological lung damage[1].
Diethylcarbamazine (12-200 mg/kg; p.o.; twice weekly; 12 weeks) significantly ameliorates high-fat diet-induced insulin resistance in male Swiss mice via suppression of adipose tissue inflammation at the optimal 50 mg/kg dose, without affecting body or tissue weights, with significant reductions in serum glucose, insulin, triglycerides, proinflammatory mediators, liver cyclooxygenase activity, and NF-κBp65 nuclear translocation[2].
Diethylcarbamazine (6 mg/kg; p.o.; daily; 1 week) inhibits actinomycetoma development in BALB/c mice, with a statistically significant reduction in lesion size, and enhances cellular immune responses including neutrophil reactive oxygen intermediate production and lymphocyte proliferation[3].

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

Animal Model: white albino mice (6 to 8-week-old female, 18-20 g, intradermal sensitization + aerosol exposure Ovalbumin-induced asthma)[1]
Dosage: 12 mg/kg
Administration: p.o.;
Result: Reduced serum IL-4 and IL-5, total BALF IgE and specific anti-ovalbumin IgE, lung tissue EPO and eotaxin2, and reduced inflammatory cell infiltration and thickened alveolar walls compared to untreated asthmatic mice.
Showed no significant changes in serum IL-4, IL-5, BALF IgE, lung EPO, or eotaxin2, and similar histopathological improvement compared to DEC alone when preceded by anti-DEC antibody.
Showed no significant changes in serum IL-4, IL-5, lung EPO, or eotaxin2, and partial reduction in inflammatory cell infiltration and alveolar wall thickening compared to DEC alone when preceded by 10 mg/kg Quercetin.
Significantly reduced serum IL-4 and IL-5, increased IFN-γ/IL-4 ratio to near control levels, decreased total BALF IgE, and reduced inflammatory cell infiltration compared to DEC alone when preceded by 20 mg/kg and 40 mg/kg Quercetin.
Animal Model: Swiss mice (male, 5 weeks old, initial 10 g body weight, high-fat diet-induced insulin resistance)[2]
Dosage: 12 mg/kg; 50 mg/kg; 200 mg/kg
Administration: p.o.; twice weekly; 12 weeks (from 6 to 18 week)
Result: Reduced serum glucose levels at all oral glucose tolerance test time points (0, 30, 60, 120 min) with a statistically significant reduction in area under the curve at 50 mg/kg.
Reduced serum triglyceride levels at 50 mg/kg.
Reduced serum insulin levels and HOMA-IR score at 50 mg/kg.
Reduced serum leptin levels at 50 mg/kg.
Reduced serum levels of TNF-α, IL-6, and MCP-1 at 50 mg/kg.
Significantly reduced liver cyclooxygenase activity at 50 mg/kg.
Significantly inhibited nuclear localization of NF-κBp65 with increased cytoplasmic retention at 50 mg/kg.
Showed no statistically significant reductions in serum glucose, triglycerides, insulin, HOMA-IR, leptin, TNF-α, IL-6, MCP-1, or liver cyclooxygenase activity relative to untreated high-fat diet-fed mice at 12 mg/kg and 200 mg/kg.
Exhibited less potent effects on NF-κBp65 nuclear localization at 12 mg/kg and 200 mg/kg compared to 50 mg/kg.
Caused no significant changes to body, adipose tissue, or liver weights at 50 mg/kg.
Animal Model: BALB/c (male, 10-12 weeks old, 37-45 g, actinomycetoma model via footpad inoculation with Nocardia brasiliensis)[3]
Dosage: 6 mg/kg
Administration: p.o.; daily; 1 week
Result: Reduced actinomycetoma lesion size with statistical significance compared to untreated infected controls.
Resolved fistulae, granule discharge, hyperemia, and erythema by day 20 post-infection, and prevented mycetoma establishment through day 90.
Reduced cellular infiltrate, eliminated granuloma layer formation, restored epidermal integrity, and reorganized damaged striated muscle fibers by day 28 post-infection.
Enhanced polymorphonuclear neutrophil reactive oxygen intermediate production with statistical significance at day 3 post-infection.
Increased lymphocyte proliferation in response to N.
brasiliensis cellular crude extract with statistical significance at day 21 post-infection.
Increased lymphocyte proliferation in response to concanavalin A with statistical significance at day 28 post-infection.
Caused no significant changes in IgG or IgM antibody production against N.
brasiliensis P24 antigen.
分子量

199.29

分子式

C10H21N3O

CAS 番号
Appearance

Solid-Liquid Mixture

Color

Off-white to light yellow

SMILES

O=C(N1CCN(C)CC1)N(CC)CC

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

RT, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (RT, sealed storage, away from moisture and light)

溶剤 & 溶解度
体外: 

DMSO : 200 mg/mL (1003.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.0178 mL 25.0891 mL 50.1781 mL
5 mM 1.0036 mL 5.0178 mL 10.0356 mL
10 mM 0.5018 mL 2.5089 mL 5.0178 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.0178 mL 25.0891 mL 50.1781 mL 125.4453 mL
5 mM 1.0036 mL 5.0178 mL 10.0356 mL 25.0891 mL
10 mM 0.5018 mL 2.5089 mL 5.0178 mL 12.5445 mL
15 mM 0.3345 mL 1.6726 mL 3.3452 mL 8.3630 mL
20 mM 0.2509 mL 1.2545 mL 2.5089 mL 6.2723 mL
25 mM 0.2007 mL 1.0036 mL 2.0071 mL 5.0178 mL
30 mM 0.1673 mL 0.8363 mL 1.6726 mL 4.1815 mL
40 mM 0.1254 mL 0.6272 mL 1.2545 mL 3.1361 mL
50 mM 0.1004 mL 0.5018 mL 1.0036 mL 2.5089 mL
60 mM 0.0836 mL 0.4182 mL 0.8363 mL 2.0908 mL
80 mM 0.0627 mL 0.3136 mL 0.6272 mL 1.5681 mL
100 mM 0.0502 mL 0.2509 mL 0.5018 mL 1.2545 mL
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    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.

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製品名:
Diethylcarbamazine
製品番号:
HY-12642A
数量:
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