Metabolism / Metabolites
Carbamates are enzymatically hydrolyzed in the liver; degradation products are excreted via the kidneys and liver. (L793)

Toxicity Summary
Methoxycarb is a cholinesterase, or acetylcholinesterase (AChE) inhibitor. Carbamate compounds carbamate esters form unstable complexes with cholinesterase by carbamylation of the enzyme's active site. This inhibition is reversible. Cholinesterase inhibitors suppress the activity of acetylcholinesterase. Because acetylcholinesterase plays an important physiological role, chemicals that interfere with its activity are potent neurotoxins, causing excessive salivation and lacrimation even at low doses. High-dose exposure typically results in symptoms such as headache, salivation, nausea, vomiting, abdominal pain, and diarrhea. Acetylcholinesterase breaks down the neurotransmitter acetylcholine, which is released at the neuromuscular junction, causing muscle or organ relaxation. Inhibition of acetylcholinesterase results in the accumulation and sustained action of acetylcholine, leading to continuous nerve impulse transmission and an inability to stop muscle contractions.

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Toxicity Data
LC50 (Rat) = 475 mg/m3Interactions
This study investigated the combined toxicity of malathion, 2-sec-butylphenyl methylcarbamate, m-toluenemethylcarbamate, and 3,4-xylmethylcarbamate in mice and rats. ICR mice and male Fischer 344 rats were orally exposed to five different concentrations of insecticide suspensions to determine the median lethal dose (LD50); animal mortality was observed for at least 7 days post-administration. … Mice were sacrificed, brain tissue was homogenized, and brain acetylcholinesterase activity was measured. Of all the combinations tested, only the combination of malathion and 2-sec-butylphenyl methylcarbamate showed a significant synergistic effect in acute toxicity in male mice; other combinations with m-toluenemethylcarbamate or 3,4-xylmethylcarbamate did not show a significant enhancing effect on toxicity in male mice. Female mice showed similar synergistic responses to the insecticides. In rats, the strength of this synergistic effect was relatively lower than in mice. Symptoms such as muscle fasciculations, increased salivation, increased urination, convulsions, and dyspnea were similar in mice and rats. Significant differences existed in the time to death after administration between different insecticides and between rats and mice. ...
Succinylcholine, other cholinergic drugs, and aminophylline are contraindicated. /Carbamates and Related Compounds/

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Non-human Toxicity Values
LD50 Male rat, oral: 580 mg/kg
LD50 Female rat, oral: 498 mg/kg
LD50 Mouse, oral: 109 mg/kg
LD50 Rat, dermal: >2,000 mg/kg
For more complete non-human toxicity data on METOLCARB (6 in total), please visit the HSDB record page.

[1]. Jingwei Sun, et al. Development of enzyme linked immunoassay for the simultaneous detection of carbaryl and metolcarb in different agricultural products. Anal Chim Acta. 2010 May 7;666(1-2):76-82.

Metolcarb is a colorless crystalline solid. It is an insecticide used to control rice planthoppers, codling moths, citrus mealybugs, onion thrips, fruit flies, cotton bollworms, and aphids. It is not registered as an insecticide in the United States (EPA, 1998). Metolcarb is a carbamate compound. It has multiple functions, including as an EC 3.1.1.7 (acetylcholinesterase) inhibitor, carbamate insecticide, acaricide, and agrochemical. Its structure is similar to methylcarbamate and m-cresol. Metolcarb is a synthetic carbamate compound and acetylcholinesterase inhibitor used as an insecticide. It is a colorless crystalline solid that can be exposed through inhalation, ingestion, or contact. Metolcarb is a carbamate insecticide. Carbamate insecticides are derived from carbamate and their insecticidal action is similar to that of organophosphate insecticides. They are widely used in homes, gardens, and agriculture. The first carbamate insecticide, Sevin, was introduced in 1956, and its global usage exceeds that of all other carbamate insecticides combined. Due to its relatively low oral and dermal toxicity to mammals and its broad spectrum of application, Sevin is widely used in lawns and gardens. Most carbamate insecticides are highly toxic to hymenopteran insects, therefore precautions must be taken to prevent contact with them by insects such as bees or parasitic wasps. Some carbamate insecticides can be transported within plants, making them effective systemic treatments. (L795)

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Mechanism of Action
Cholinesterase inhibitor.

C9H11NO2

165.19

165.078

1129-41-5

Metolcarb-d3;1777782-68-9

14322

Colorless crystalline solid

1.1±0.1 g/cm3

241.6±23.0 °C at 760 mmHg

74-77 °C

99.9±22.6 °C

0.0±0.5 mmHg at 25°C

1.517

1.63

38.33

1

2

2

12

159

0

CC1=CC(OC(NC)=O)=CC=C1

VOEYXMAFNDNNED-UHFFFAOYSA-N

InChI=1S/C9H11NO2/c1-7-4-3-5-8(6-7)12-9(11)10-2/h3-6H,1-2H3,(H,10,11)

(3-methylphenyl) N-methylcarbamate

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。