Acetaminophen (對乙酰氨基酚)

Acetaminophen (Paracetamol) 是選擇性環(huán)氧合酶-2 (COX-2) 的抑制劑，IC50 值為 25.8 μM。Acetaminophen 是一種有效的肝 N-乙酰轉(zhuǎn)移酶 2 (NAT2) 抑制劑。Acetaminophen 在解熱和止痛劑方面應(yīng)用是比較廣的。

貨號：HY-66005

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號：HY-66005

起訂量：1

規(guī)格:：10g

價格:：￥600

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產(chǎn)品詳情

Acetaminophen (Synonyms: 對乙酰氨基酚）

Acetaminophen (Paracetamol) 是選擇性環(huán)氧合酶-2 (COX-2) 的抑制劑，IC50 值為 25.8 μM。Acetaminophen 是一種有效的肝 N-乙酰轉(zhuǎn)移酶 2 (NAT2) 抑制劑。Acetaminophen 在解熱和止痛劑方面應(yīng)用是比較廣的。

生物活性

Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC₅₀ of 25.8 μM; is a widely used antipyretic and analgesic agent^[1]^[2]^[3]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor^[4]

體外研究(In Vitro)

In vitro, acetaminophen elicites a 4.4-fold selectivity toward COX-2 inhibition (IC₅₀ 113.7 μM for COX-1; IC₅₀ 25.8 μM for COX-2). Following oral administration of the drug, maximal ex vivo inhibitions are 56% (COX-1) and 83% (COX-2). Acetaminophen plasma concentrations remaine above the in vitro IC₅₀ for COX-2 for at least 5 h postadministration. Ex vivo IC₅₀ values (COX-1: 105.2 μM; COX-2: 26.3 μM) of acetaminophen compared favorably with its in vitro IC₅₀ values. In contrast to previous concepts, acetaminophen inhibited COX-2 by more than 80%, i.e., to a degree comparable to nonsteroidal antiinflammatory drugs (NSAIDs) and selective COX-2 inhibitors. However, a >95% COX-1 blockade relevant for suppression of platelet function is not achieved^[1]. MTT assay shows that Acetaminophen (APaP) in a dose of 50 mM significantly (p<0.001) reduces cell viability to 61.5±6.65%. Interestingly, the significant (p<0.01) increase in cell viability to 79.7±2.47% is observed in the Acetaminophen/HV110 co-treated cells, compared to Acetaminophen treated cells^[2].

體內(nèi)研究(In Vivo)

Administering Acetaminophen (250?mg/kg, orally) to the mice causes significant (p<0.001) liver damage and necrosis of cells as evidenced by the elevated serum hepatic enzymes alanine aminotransferase (ALT), aminotransferase (AST), alkaline phosphatase (ALP), and gamma-glutamyl transferase (γGT) compared with normal group. Conversely, effects of pretreatment with different doses of citral (125, 250, and 500?mg/kg) exhibited a significant (p<0.05) decrease in serum activities of ALT (91.79%, 93.07%, and 95.61%, resp.), AST (93.40%, 91.89%, and 96.52%, resp.), ALP (39.29%, 37.07%, and 59.80%, resp.), and γGT (92.83%, 91.59%, and 93.0%, resp.), when compared to the Acetaminophen group. Similar results were found in pretreatment with SLM on the activity of ALT (95.90%), AST (95.03%), ALP (70.52%), and γGT (92.69%)^[3].

分子量：151.16

Formula：C₈H₉NO₂

CAS 號：103-90-2

中文名稱：對乙酰氨基酚；乙酰氨基酚；撲熱息痛；退熱凈；醋氨酚；對醋氨酚；索密痛；乙酰氨基苯酚；二醋洛爾

運輸條件：Room temperature in continental US; may vary elsewhere.

儲存方式

Powder	-20°C	3 years
	4°C	2 years

*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

溶解性數(shù)據(jù)

DMSO : 250 mg/mL (1653.88 mM; Need ultrasonic)

H₂O : 10 mg/mL (66.16 mM; Need ultrasonic)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	6.6155 mL	33.0775 mL	66.1551 mL
5 mM	1.3231 mL	6.6155 mL	13.2310 mL
10 mM	0.6616 mL	3.3078 mL	6.6155 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (66.16 mM); Suspended solution; Need ultrasonic
2.

請依序添加每種溶劑： saline 0.5% Tween-80
Solubility: 10 mg/mL (66.16 mM); Clear solution; Need ultrasonic
3.

請依序添加每種溶劑： PBS
Solubility: 6.67 mg/mL (44.13 mM); Clear solution; Need ultrasonic
4.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (13.76 mM); Clear solution
5.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (13.76 mM); Clear solution
6.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (13.76 mM); Clear solution

參考文獻

[1]. Hinz, B, et al. Acetaminophen (paracetamol) is a selective cyclooxygenase-2 inhibitor in man. FASEB J, 2008. 22(2): p. 383-90.

[2]. Miroslav Dini?, et al. Lactobacillus fermentum Postbiotic-induced Autophagy as Potential Approach for Treatment ofAcetaminophen Hepatotoxicity. Front Microbiol. 2017 Apr 6;8:594.

[3]. Uchida NS, et al. Hepatoprotective Effect of Citral on Acetaminophen-Induced Liver Toxicity in Mice. Evid Based Complement Alternat Med. 2017;2017:1796209.

[4]. Rothen JP, et al. Acetaminophen is an inhibitor of hepatic N-acetyltransferase 2 in vitro and in vivo. Pharmacogenetics. 1998 Dec;8(6):553-9.

Acetaminophen (對乙酰氨基酚)

Acetaminophen (Paracetamol) 是選擇性環(huán)氧合酶-2 (COX-2) 的抑制劑，IC50 值為 25.8 μM。Acetaminophen 是一種有效的肝 N-乙酰轉(zhuǎn)移酶 2 (NAT2) 抑制劑。Acetaminophen 在解熱和止痛劑方面應(yīng)用是比較廣的。

貨號：HY-66005

品牌：MCE

型號：HY-66005

起訂量：1

規(guī)格:：10g

價格:：￥600

15906629305

在線客服

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產(chǎn)品詳情

Acetaminophen (Synonyms: 對乙酰氨基酚）

Acetaminophen (Paracetamol) 是選擇性環(huán)氧合酶-2 (COX-2) 的抑制劑，IC50 值為 25.8 μM。Acetaminophen 是一種有效的肝 N-乙酰轉(zhuǎn)移酶 2 (NAT2) 抑制劑。Acetaminophen 在解熱和止痛劑方面應(yīng)用是比較廣的。

生物活性

Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC₅₀ of 25.8 μM; is a widely used antipyretic and analgesic agent^[1]^[2]^[3]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor^[4]

體外研究(In Vitro)

In vitro, acetaminophen elicites a 4.4-fold selectivity toward COX-2 inhibition (IC₅₀ 113.7 μM for COX-1; IC₅₀ 25.8 μM for COX-2). Following oral administration of the drug, maximal ex vivo inhibitions are 56% (COX-1) and 83% (COX-2). Acetaminophen plasma concentrations remaine above the in vitro IC₅₀ for COX-2 for at least 5 h postadministration. Ex vivo IC₅₀ values (COX-1: 105.2 μM; COX-2: 26.3 μM) of acetaminophen compared favorably with its in vitro IC₅₀ values. In contrast to previous concepts, acetaminophen inhibited COX-2 by more than 80%, i.e., to a degree comparable to nonsteroidal antiinflammatory drugs (NSAIDs) and selective COX-2 inhibitors. However, a >95% COX-1 blockade relevant for suppression of platelet function is not achieved^[1]. MTT assay shows that Acetaminophen (APaP) in a dose of 50 mM significantly (p<0.001) reduces cell viability to 61.5±6.65%. Interestingly, the significant (p<0.01) increase in cell viability to 79.7±2.47% is observed in the Acetaminophen/HV110 co-treated cells, compared to Acetaminophen treated cells^[2].

體內(nèi)研究(In Vivo)

Administering Acetaminophen (250?mg/kg, orally) to the mice causes significant (p<0.001) liver damage and necrosis of cells as evidenced by the elevated serum hepatic enzymes alanine aminotransferase (ALT), aminotransferase (AST), alkaline phosphatase (ALP), and gamma-glutamyl transferase (γGT) compared with normal group. Conversely, effects of pretreatment with different doses of citral (125, 250, and 500?mg/kg) exhibited a significant (p<0.05) decrease in serum activities of ALT (91.79%, 93.07%, and 95.61%, resp.), AST (93.40%, 91.89%, and 96.52%, resp.), ALP (39.29%, 37.07%, and 59.80%, resp.), and γGT (92.83%, 91.59%, and 93.0%, resp.), when compared to the Acetaminophen group. Similar results were found in pretreatment with SLM on the activity of ALT (95.90%), AST (95.03%), ALP (70.52%), and γGT (92.69%)^[3].

分子量：151.16

Formula：C₈H₉NO₂

CAS 號：103-90-2

中文名稱：對乙酰氨基酚；乙酰氨基酚；撲熱息痛；退熱凈；醋氨酚；對醋氨酚；索密痛；乙酰氨基苯酚；二醋洛爾

運輸條件：Room temperature in continental US; may vary elsewhere.

儲存方式

Powder	-20°C	3 years
	4°C	2 years

*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

溶解性數(shù)據(jù)

DMSO : 250 mg/mL (1653.88 mM; Need ultrasonic)

H₂O : 10 mg/mL (66.16 mM; Need ultrasonic)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	6.6155 mL	33.0775 mL	66.1551 mL
5 mM	1.3231 mL	6.6155 mL	13.2310 mL
10 mM	0.6616 mL	3.3078 mL	6.6155 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (66.16 mM); Suspended solution; Need ultrasonic
2.

請依序添加每種溶劑： saline 0.5% Tween-80
Solubility: 10 mg/mL (66.16 mM); Clear solution; Need ultrasonic
3.

請依序添加每種溶劑： PBS
Solubility: 6.67 mg/mL (44.13 mM); Clear solution; Need ultrasonic
4.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (13.76 mM); Clear solution
5.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (13.76 mM); Clear solution
6.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (13.76 mM); Clear solution

參考文獻

[1]. Hinz, B, et al. Acetaminophen (paracetamol) is a selective cyclooxygenase-2 inhibitor in man. FASEB J, 2008. 22(2): p. 383-90.

[2]. Miroslav Dini?, et al. Lactobacillus fermentum Postbiotic-induced Autophagy as Potential Approach for Treatment ofAcetaminophen Hepatotoxicity. Front Microbiol. 2017 Apr 6;8:594.

[3]. Uchida NS, et al. Hepatoprotective Effect of Citral on Acetaminophen-Induced Liver Toxicity in Mice. Evid Based Complement Alternat Med. 2017;2017:1796209.

[4]. Rothen JP, et al. Acetaminophen is an inhibitor of hepatic N-acetyltransferase 2 in vitro and in vivo. Pharmacogenetics. 1998 Dec;8(6):553-9.

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Acetaminophen (Synonyms: 對乙酰氨基酚）

Acetaminophen (對乙酰氨基酚)

分享到微信

Acetaminophen (Synonyms: 對乙酰氨基酚）