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嗎替麥考酚酯

NMR下載 COA and HPLC MSDS下載
names：
Mycophenolate Mofetil
CAS號：
128794-94-5
MDL Number： MFCD00867568
MF(分子式)： C23H31NO7 MW(分子量)： 433.49
EINECS:680-628-5 Reaxys Number:
Pubchem ID:5281078 Brand:BIOFOUNT

嗎替麥考酚酯(128794-94-5,Mycophenolate Mofetil)是非競爭性，選擇性和可逆的肌苷一磷酸脫氫酶(IMPDH)抑制劑，免疫抑制劑，IC₅₀分別為39 nM 和27 nM。

貨品編碼	規(guī)格	純度	價格 (￥)	現(xiàn)價(￥)	特價(￥)	庫存描述	數(shù)量	總計 (￥)
YZM001238-100mg	100mg	99.7%	￥ 1002.00	￥ 1002.00		2-3天	- +	￥ 0.00
YZM001238-50mg	50mg	99.7%	￥ 585.00	￥ 585.00		2-3天	- +	￥ 0.00

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中文別名	嗎替麥考酚酯(128794-94-5,Mycophenolate Mofetil);麥考酚酸酯;霉酚酸酯;霉酚酸嗎啉乙酯
英文別名	Mycophenolate Mofetil(128794-94-5);Mycophenolatemofetil;TM-MMF
CAS號	128794-94-5
Inchi	InChI=1S/C23H31NO7/c1-15(5-7-19(25)30-13-10-24-8-11-29-12-9-24)4-6-17-21(26)20-18(14-31-23(20)27)16(2)22(17)28-3/h4,26H,5-14H2,1-3H3/b15-4+
InchiKey	RTGDFNSFWBGLEC-SYZQJQIISA-N
分子式 Formula	C23H31NO7
分子量 Molecular Weight	433.49
溶解度Solubility	生物體外In Vitro:DMSO溶解度≥ 100 mg/mL(230.69 mM)*"≥" means soluble可溶, but saturation unknown溶解度未知.
性狀	白色至灰白色固體粉末
儲藏條件 Storage conditions	-20°C 3 years年 4°C 2 years年 / 溶液中:-80°C 6 months月 -20°C 1 month月

嗎替麥考酚酯(128794-94-5,Mycophenolate Mofetil)實驗注意事項：
1.實驗前需戴好防護眼鏡，穿戴防護服和口罩，佩戴手套，避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生，必要時實驗操作需要手套箱內(nèi)完成以免對實驗人員造成傷害
3.實驗后產(chǎn)生的廢棄物需分類存儲，并交于專業(yè)生物廢氣物處理公司處理，以免造成環(huán)境污染

Mycophenolate Mofetil(128794-94-5) Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

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產(chǎn)品說明	嗎替麥考酚酯(128794-94-5,Mycophenolate Mofetil)是麥考酚酸（MPA）的嗎啉代乙酯，具有有效的免疫抑制特性。
Introduction	Mycophenolate Mofetil(128794-94-5,嗎替麥考酚酯) is the morpholinoethyl ester of mycophenolic acid (MPA) with potent immunosuppressive properties.
Application1	嗎替麥考酚酯通過選擇性抑制嘌呤生物合成的從頭途徑來停止T細胞和B細胞增殖。
Application2	Mycophenolate Mofetil is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively.
Application3	Mycophenolate mofetil is a carboxylic ester resulting from the formal condensation between the carboxylic acid group of mycophenolic acid and the hydroxy group of 2-(morpholin-4-yl)ethanol.

Mycophenolate Mofetil(128794-94-5), also known as cellcept or RS 61443, belongs to the class of organic compounds known as phthalides. Phthalides are compounds containing a 3-hydrocarbylidene-2-benzofuran-1(3H)-one moiety, . Mycophenolate mofetil is a drug which is used for the prophylaxis of organ rejection in patients receiving allogeneic renal, cardiac or hepatic transplants. mycophenolate mofetil should be used concomitantly with cyclosporine and corticosteroids. . Mycophenolate mofetil exists as a solid and is considered to be practically insoluble (in water) and relatively neutral. Mycophenolate mofetil has been detected in multiple biofluids, such as urine and blood. Within the cell, mycophenolate mofetil is primarily located in the membrane (predicted from logP). Mycophenolate mofetil participates in a number of enzymatic reactions. In particular, Mycophenolate mofetil can be converted into N-(2-carboxymethyl)-morpholine, N-(2-hydroxyethyl)-morpholine, and N-(2-hydroxyethyl)-morpholine N-oxide; which is mediated by the enzyme cocaine esterase. In addition, Mycophenolate mofetil can be converted into N-(2-carboxymethyl)-morpholine, N-(2-hydroxyethyl)-morpholine, and N-(2-hydroxyethyl)-morpholine N-oxide; which is mediated by the enzymes liver carboxylesterase 1 and cocaine esterase. In humans, mycophenolate mofetil is involved in the mycophenolic Acid metabolism pathway.

警示圖
危險性	warning
危險性警示	Not available
安全聲明	H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對身體有害
安全防護	P264處理后徹底清洗+P280戴防護手套/穿防護服/戴防護眼罩/戴防護面具+P305如果進入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P2393獲得醫(yī)療建議/護理
備注	實驗過程中防止吸入、食入，做好安全防護

象形圖
信號警告	Danger
GHS危險說明	Aggregated GHS information provided by 52 companies from 8 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies. H302 (98.08%): Harmful if swallowed [Warning Acute toxicity, oral] H341 (11.54%): Suspected of causing genetic defects [Warning Germ cell mutagenicity] H360 (19.23%): May damage fertility or the unborn child [Danger Reproductive toxicity] H400 (90.38%): Very toxic to aquatic life [Warning Hazardous to the aquatic environment, acute hazard] H410 (13.46%): Very toxic to aquatic life with long lasting effects [Warning Hazardous to the aquatic environment, long-term hazard] Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.
防范說明代碼	P201, P202, P264, P270, P273, P281, P301+P312, P308+P313, P330, P391, P405, and P501 (The corresponding statement to each P-code can be found at the GHS Classification page.)

Effizienz von Mycophenolat-Mofetil bei der Therapie der intermedi?ren und posterioren Uveitis(Der Ophthalmologe,2002)

Stellungnahme zum Einsatz von Mycophenolat-Mofetil beim systemischen Lupus erythematodes(Zeitschrift für Rheumatologie,2013)

Effect of RS61443 in combination with leflunomide or FK506 on rat heart allograft survival(Transplant International,1996)

RS-61443 reverses acute renal allograft rejection in dogs(Transplant International Official Journal of the European Society for Organ Transplantation,1992)

Mycophenolat scheint Azathioprin in der Erhaltungstherapie bei Lupusnephritis überlegen(Zeitschrift für Rheumatologie,2012)

1.Nocturnal Arousal in a 68-Year-Old Woman.
Hoque R, DelRosso LM. J Clin Sleep Med. 2016 Mar 21. pii: jc-00024-16. [Epub ahead of print]
ABSTRACT: The patient is a 68-year-old white woman, with past medical history of autoimmune hepatitis, hypertension, coronary artery disease, depression, and mild cognitive impairment. Medications include: mycophenolate mofetil, lisinopril, aspirin, sertraline, trazadone, and galantamine. She presents for evaluation of witnessed snoring and sleep maintenance insomnia, with frequent tossing and turning during the night. She goes to bed at 9:30 PM and falls asleep within minutes. She has two nocturnal awakenings, usually to urinate. She falls asleep quickly upon returning from the bathroom. She rises at 6 AM, and feels refreshed upon awakening. She denies lower extremity restlessness, or leg kicking during sleep. She has been told she snores, but denies witnessed apnea. She denies use of tobacco, alcohol, or illicit drugs.

2.Pharmacokinetic Variability of Mycophenolic Acid in Pediatric and Adult Patients with Hematopoietic Stem Cell Transplantation.
Zhang D1, Renbarger JL2, Chow DS1. J Clin Pharmacol. 2016 Apr 6. doi: 10.1002/jcph.745. [Epub ahead of print]
The aim of this study was to evaluate the pharmacokinetic variations of mycophenolic acid (MPA), the active metabolite of mycophenolate mofetil (MMF), in both pediatric and adult patients following hematopoietic stem cell transplantation (HSCT). Twenty pediatric patients with a median age of 3 years (range, 0.2-12 years) and thirteen adult patients with a median age of 54 years (range, 18-63 years) were enrolled. Blood samples were collected on days 0, 7, 14, 21 and 30 after allogeneic HSCT. Total and free (unbound) MPA, as well as MPAG were quantified using a validated LC-MS/MS assay. The plasma protein binding of MPA and MPAG did not change significantly in pediatric patients over the one month sampling period post HSCT. However, it increased in adult patients from day 7 to day 30 post HSCT, from 97.3±0.8% to 98.3±0.6% for MPA (P <0.05), and 74.6±9.4% to 82.9±8.1% for MPAG (P <0.05). The plasma protein binding of MPA was significantly higher in males compared to females in both pediatric (98.

3.Everolimus versus mycophenolate mofetil de novo after lung transplantation - a prospective, randomized, open-label trial.
Strueber M1, Warnecke G2,3, Fuge J4, Simon AR5, Zhang R2, Welte T3,4, Haverich A2,3, Gottlieb J3,4. Am J Transplant. 2016 Apr 22. doi: 10.1111/ajt.13835. [Epub ahead of print]
The role of mTOR inhibitors in de novo immunosuppression after lung transplantation is not well-defined. We compared Everolimus versus mycophenolate mofetil in an investigator-initiated single center trial in Hannover, Germany. A total of 190 patients were randomly assigned 1:1 on day 28 post-transplantation to MMF or Everolimus combined with CsA and Steroids. Patients were followed up for two years. Primary endpoint was freedom from BOS. Secondary endpoints were incidence of acute rejections, infections, treatment failure and kidney function. BOS-free survival in ITT analysis was similar in both groups (p=0.174). The study protocol was completed by 51% of enrolled patients. The per-protocol analysis shows incidence of BOS- 1/43 in the everolimus and 8/54 in the MMF group (p=0.041). Less biopsy-proven AR (p=0.005), CMV antigenemia (p=0.005), lower respiratory tract infection (p=0.003) and no leucopenia were seen in the everolimus group. GFR decreased in both groups about 50% within 6 months.

4.Enhancement of Mycophenolate Mofetil Permeation for Topical Use by Eucalyptol and N-Methyl-2-pyrrolidone.
Amnuaikit T1, Songkram C2, Pinsuwan S1. Scientifica (Cairo). 2016;2016:9672718. doi: 10.1155/2016/9672718. Epub 2016 Mar 16.
Mycophenolate mofetil (MMF) is a prodrug of mycophenolic acid (MPA) which can be metabolized by esterase. MMF has been approved by the United States Food and Drug Administration (USFDA) for treatment of psoriasis patient with skin symptoms. However, it remains unclear whether MMF is efficiently effective to treat skin symptoms developed from psoriasis. The insufficient amount of MMF penetrating through the skin results in the treatment failure due to the difficulty in MMF penetration through the stratum corneum. Skin permeation enhancers such as eucalyptol (EUL) and N-methyl-2-pyrrolidone (NMP) potentially aid in increasing skin penetration. This study aimed to investigate the effects of a concentration ratio (% w/v) between two enhancers (EUL and NMP). The results showed that EUL enhanced MMF permeation with an enhancement ratio (ER) of 3.44 while NMP was not able to promote the penetration of MMF. Interestingly, the synergistic effect of the two enhancers was observed with a suitable ratio given that the ER was 8.

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