N-acetyl Dapsone
(Synonyms: N-乙酰氨苯砜) 目录号 : GC44294
A metabolite of dapsone
Cas No.:565-20-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
N-acetyl Dapsone is a metabolite of dapsone, an anti-inflammatory and antibacterial compound that is widely used in the treatment of leprosy, malaria, acne, and various immune disorders. Dapsone is acetylated in the liver to monoacetyldapsone, the major metabolite, and other mono and diacetyl derivatives, and subsequently deacetylated back to diaminodiphenylsulfone (dapsone) until a state of equilibrium is achieved.
| Cas No. | 565-20-8 | SDF | |
| 别名 | N-乙酰氨苯砜 | ||
| Canonical SMILES | NC1=CC=C(S(C2=CC=C(NC(C)=O)C=C2)(=O)=O)C=C1 | ||
| 分子式 | C14H14N2O3S | 分子量 | 290.3 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4447 mL | 17.2236 mL | 34.4471 mL |
| 5 mM | 0.6889 mL | 3.4447 mL | 6.8894 mL |
| 10 mM | 0.3445 mL | 1.7224 mL | 3.4447 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Dapsone 5% gel: a review of its efficacy and safety in the treatment of acne vulgaris
Am J Clin Dermatol 2009;10(4):221-7.PMID:19489655DOI:10.2165/00128071-200910040-00002.
Dapsone, a synthetic sulfone that has been available for over 60 years, has been used to treat a myriad of cutaneous disorders. Prior to the general acceptance of isotretinoin, oral dapsone had been reported to be effective in the treatment of nodulocystic acne. However, the potential for systemic toxicity prevented its widespread adoption in the treatment of acne. For many years scientists explored the possibility of developing a topical formulation of dapsone for the treatment of acne in the hope of minimizing the adverse hematologic effects of oral dapsone. Such a formulation had been unavailable until recently. Dapsone 5% gel (Aczone) was recently developed to treat acne vulgaris. This topical formulation was approved in the US based on two randomized, vehicle-controlled studies. A 12-month, open-label study was also conducted to assess the safety and efficacy of topical dapsone over the long term. Finally, two open-label phase I pharmacokinetic studies were conducted to evaluate the systemic absorption of topical dapsone compared with oral dapsone. This article reports the results of these studies, which show a reduction in acne lesion count comparable to those observed in clinical trials of other approved topical acne therapies. With regard to safety, the studies demonstrated that the concentrations of dapsone and N-acetyl Dapsone remain low and do not accumulate over time once steady state is reached. Of the total of 50 patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency in all the studies, only two experienced a drop in hemoglobin levels, and those shifts in values were consistent with fluctuations observed for other study participants. A recent study evaluating the risk of hemolysis in patients with G6PD deficiency found topical dapsone 5% gel to be safe to use in this patient population. Based on the observations noted in the above-mentioned studies, we conclude that topical dapsone 5% gel is safe and effective in the treatment of acne vulgaris.
Pharmacokinetics of dapsone gel, 5% for the treatment of acne vulgaris
Clin Pharmacokinet 2007;46(8):697-712.PMID:17655376DOI:10.2165/00003088-200746080-00006.
Background: Oral dapsone has been available for over 60 years and has been used to treat severe acne vulgaris; however, the oral formulation is known to cause dose-dependent haematological reactions and is currently indicated only for diseases such as dermatitis herpetiformis and Hansen's disease. A gel formulation of dapsone was recently developed to treat acne vulgaris. As dapsone is administered topically, it was expected that systemic absorption would be considerably lower than that observed with oral dapsone therapy, thereby avoiding any adverse haematological effects. Objective: To report the pharmacokinetic profile of topically applied dapsone gel, 5% in the treatment of acne vulgaris. Study participants and methods: Three prospective, open-label studies enrolled a total of 548 subjects with acne vulgaris: two phase I pharmacokinetic studies (crossover and drug interaction) and one phase III long-term safety study. In the crossover study (n = 18), topical dapsone gel applied twice daily for a total of 14 days to 22.5% of the body surface area was compared with a single dose of oral dapsone 100mg (the typical clinical dose). In the drug-interaction study (n = 24), oral trimethoprim/sulfamethoxazole monotherapy, topical dapsone gel monotherapy and the two in combination were used twice daily for 7, 21 and 7 days, respectively. In the long-term safety study (n = 506), topical dapsone gel was applied twice daily to acne-affected areas for up to 12 months. Blood samples were drawn at various timepoints in each study to assess drug and metabolite concentrations. Systemic concentrations of dapsone, N-acetyl Dapsone, dapsone hydroxylamine, trimethoprim and sulfamethoxazole were determined, according to the study design. Results: In the crossover study, the mean area under the plasma concentration-time curve (AUC) from 0 to 24 hours for dapsone was 417.5 ng x h/mL after 2 weeks of dapsone gel therapy (n = 10), compared with an AUC from time zero to infinity of 52,641 ng x h/mL after a single dose of oral dapsone; this represents a 126-fold lower systemic exposure for dapsone gel at typical therapeutic doses. In the drug-interaction study, the AUC from 0 to 12 hours for dapsone was 221.52 ng x h/mL after 3 weeks of dapsone gel monotherapy compared with 320.3 ng x h/mL after 1 week of coadministration with trimethoprim/sulfamethoxazole. In the long-term safety study, the mean plasma dapsone concentrations ranged from 7.5 to 11 ng/mL over 12 months. Overall, total systemic exposures to dapsone and its metabolites were approximately 100-fold less for dapsone gel than for oral dapsone, even in the presence of trimethoprim/sulfamethoxazole. There were no reports of any haematological adverse events. Conclusions: Topical application of dapsone gel in various settings ranging from 2 weeks to 12 months resulted in systemic exposures to dapsone and its metabolites that were approximately 100-fold less than those after oral dapsone at a therapeutic dose level. The concentrations of dapsone and its metabolites reached steady state and did not increase during prolonged treatment.
Safety and Pharmacokinetics of Once-Daily Dapsone Gel, 7.5% in Patients With Moderate Acne Vulgaris
J Drugs Dermatol 2016 Oct 1;15(10):1250-1259.PMID:27741344doi
Background: Reducing the dosing frequency of topical acne treatments to once daily may improve adherence.
Objective: Evaluate pharmacokinetics (PK), safety, and tolerability of 3 formulations of once-daily dapsone gel, 7.5% and of twice-daily dapsone gel, 5% over 28 days in patients with moderate acne vulgaris.
Methods: This phase 1, multicenter, parallel-group study randomized males and females aged 16 to 35 years to 1 of 3 dapsone gel, 7.5% formulations (DAP-11078, DAP-11079, or DAP-11080 double-blind; applied once daily) or to dapsone gel, 5% (investigator-blinded only, applied twice-daily). Blood samples were collected for PK assessments of dapsone and its metabolites, N-acetyl Dapsone (NAD) and dapsone hydroxylamine (DHA), before the morning dose on days 1, 7, 14, 18, 21, 26, 27, and 28, and at several follow-up time points (days 29-32). Safety profile assessments included adverse events (AEs), physical examinations, laboratory tests, and local tolerability assessments.
Results: Steady-state dapsone, NAD, and DHA concentrations were reached within 7 days of the first dose in all treatment groups. Daily systemic exposures of the 3 dapsone gel, 7.5% formulations were approximately 25% to 40% lower than that for dapsone gel, 5%, and these differences were statistically significant. Among the 3 dapsone gel, 7.5% formulations, the highest daily exposure of dapsone (per the AUC) was observed with DAP-11080, with respective Cmax and AUC0-24 being approximately 28.6% and 28.7% lower relative to dapsone gel, 5%. Most AEs were mild to moderate in intensity. The safety profiles for all 3 formulations of once-daily dapsone, 7.5% gel and twice-daily dapsone gel, 5% were similar following 28 days of topical administration. All 4 dapsone formulations were well tolerated.
Conclusions: This study demonstrated lower systemic exposure with all 3 once-daily dapsone gel, 7.5% formulations than with twice-daily dapsone gel, 5%. All 4 formulations were well tolerated and demonstrated similar safety profiles.
J Drugs Dermatol. 2016;15(10):1250-1259.
Hematologic safety of dapsone gel, 5%, for topical treatment of acne vulgaris
Arch Dermatol 2008 Dec;144(12):1564-70.PMID:19075138DOI:10.1001/archdermatol.2008.518.
Objective: To evaluate the risk of hemolysis in subjects with glucose-6-phosphate dehydrogenase (G6PD) deficiency who were treated for acne vulgaris with either dapsone gel, 5% (dapsone gel), or vehicle gel. Design: Double-blind, randomized, vehicle-controlled, crossover study. Setting: Referral centers and private practice. Participants: Sixty-four subjects 12 years or older with G6PD deficiency and acne vulgaris. Intervention Subjects were equally randomized to 1 of 2 sequences of 12-week treatment periods (vehicle followed by dapsone gel or dapsone gel followed by vehicle). The washout period was 2 weeks. Treatments were applied twice daily to the face and to other acne-affected areas of the neck, upper chest, upper back, and shoulders as required. Main outcome measures: Results of clinical chemical analysis and hematology values; plasma dapsone and N-acetyl Dapsone concentrations; spontaneous reports of adverse events. Results: A 0.32-g/dL decrease in hemoglobin concentration occurred from baseline to 2 weeks during dapsone gel treatment. This was not accompanied by changes in other laboratory parameters, including reticulocytes, haptoglobin, bilirubin, and lactate dehydrogenase levels, and was not apparent at 12 weeks as treatment continued. The number of subjects with a 1-g/dL drop in hemoglobin concentration was similar between treatment groups at both week 2 and week 12. The largest drops in hemoglobin concentration were 1.7 g/dL in the vehicle gel treatment group and 1.5 g/dL in the dapsone gel treatment group. No clinical signs or symptoms of hemolytic anemia were noted. Conclusions: After treatment with dapsone gel, 5%, no clinical or laboratory evidence of drug-induced hemolytic anemia was noted in G6PD-deficient subjects with acne vulgaris. Trial Registration clinicaltrials.gov Identifier: NCT00243542.
Influences of Re Du Ning Injection, a traditional Chinese medicine injection, on the CYP450 activities in rats using a cocktail method
J Ethnopharmacol 2015 Nov 4;174:426-36.PMID:26318744DOI:10.1016/j.jep.2015.08.035.
Ethnopharmacological relevance: Re Du Ning Injection (RDN), a traditional Chinese medicine injection, is made from the extracts of Lonicerae japonicae flos (LJF), Artemisiae annuae herba (AAH) and Gardeniae fructus (GF). Since last decade, RDN has been widely used in China for the treatment of fever, inflammation, allergy and viral infection. Aim of the study: To elucidate the potential influences of RDN on the activities of four cytochrome P450 (CYP) isozymes in rats (CYP1A2, CYP2C11, CYP2D1 and CYP3A1/2) by "cocktail method". Materials and methods: A sensitive and specific LC-MS method capable of simultaneous quantification of four substrates and their metabolites in rat plasma was developed and validated. Relative activity estimation of four isozymes was carried out by comparing plasma pharmacokinetics of substrates and their metabolites (phenacetin/ paracetamol for CYP1A2, tolbutamide/4-hydroxytolbutamide for CYP2C11, dextromethorphan/ dextrorphan for CYP2D1 and dapsone/N-acetyl Dapsone for CYP3A1/2) between control and RDN treatment groups. Results: Compared with control group, RDN at different levels could increase the total amount of tolbutamide, dextromethorphan and dapsone absorbed into blood, while decrease the total amount of phenacetin absorbed into blood at low and medium dosage and increase it at high dosage. Conclusions: RDN could inhibit the activities of CYP2C11, CYP2D1 and CYP3A1/2, induce the activity of CYP1A2 at low and medium dosage but inhibit it at high dosage. The results indicated that drug co-administrated with RDN may need dose adjustment.