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塞来昔布

选择性环氧合酶2(COX-2)抑制剂。非甾体抗炎药。
规格或纯度: ≥99%
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货号 (SKU) 包装规格 是否现货 价格 数量
C129279-100mg
100mg 现货 Stock Image
C129279-5g
5g 现货 Stock Image
C129279-10g
10g 现货 Stock Image
C129279-25g
25g 现货 Stock Image
C129279-100g
100g 现货 Stock Image
C129279-500g
500g 现货 Stock Image

基本描述

规格或纯度 ≥99%
英文名称 Celecoxib
别名 塞内昔布|4-[5-(4-甲苯基)-3-(三氟甲基)-1H-吡唑-1-基]甲磺酰胺|5-(4-甲苯基)-1-(4-磺酰基苯基)-3-(三氟甲基)吡唑
英文别名 celecoxib|169590-42-5|Celebrex|Celebra|Onsenal|Celecox|Celocoxib|Xilebao|184007-95-2|SC 58635|SC-58635|YM177|4-[5-(4-METHYLPHENYL)-3-(TRIFLUOROMETHYL)-1H-PYRAZOL-1-YL]BENZENESULFONAMIDE|4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonam
生化机理 Celecoxib is a selective cyclooxygenase-2 (Cox-2) inhibitor (IC50 = 40 nM) with low sensitivity against Cox-1. Celecoxib shows an anti-proliferative effect on nasopharyngeal carcinoma (NPC) cell lines including HNE1 (IC50 = 32.86 μM) and CNE1-LMP1 (IC50 = 61.31 μM).Selective COX-2 inhibitor (IC 50 values are 15 and 0.04 μM for COX-1 and COX-2 respectively). Non-steroidal anti-inflammatory drug. Enhances tumor cell apoptosis in vivo . Orally active.
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 100mg卖完停产,不再备货;如果有可能,您尽量在使用的当天配置溶液,并在当天使用完它。但是,如果您需要预先配制储备溶液,我们建议您将溶液等份保存在-20°C的密封小瓶中。通常,它们最多可以使用一个月。在使用前和打开样品瓶之前,我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。
产品介绍

Celecoxib是环氧合酶-2(COX-2)选择性抑制剂,IC50为40 nM。A selective Cox-2 inhibitor

Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM.
A selective Cox-2 inhibitor

名称和标识符

EC号 685-962-5
IUPAC Name 4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide
INCHI InChI=1S/C17H14F3N3O2S/c1-11-2-4-12(5-3-11)15-10-16(17(18,19)20)22-23(15)13-6-8-14(9-7-13)26(21,24)25/h2-10H,1H3,(H2,21,24,25)
InChi Key RZEKVGVHFLEQIL-UHFFFAOYSA-N
Canonical SMILES CC1=CC=C(C=C1)C2=CC(=NN2C3=CC=C(C=C3)S(=O)(=O)N)C(F)(F)F
WGK Germany 3
RTECS DB2944937
关联CAS 169590-42-5
PubChem CID 2662
NSC Number 719627
MeSH Entry Terms 4-(5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide;Celebrex;celecoxib;SC 58635;SC-58635;SC58635
分子量 381.37

化学和物理性质

溶解性 Soluble in DMSO (76 mg/ml at 25 °C), methanol, ethanol (33 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and dichloromethane., Soluble in DMSO (76 mg/ml at 25 °C), methanol, ethanol (33 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and dichloromethane
敏感性 对热、光线敏感
熔点 163 °C

安全和危险性(GHS)

象形图
ghs08

Health Hazard

信号词 Danger
危险声明 H360: May damage fertility or the unborn child
预防措施声明 P280,P405,P501,P203,P318
WGK Germany 3
RTECS DB2944937
Merck Index 1956

关联配体

Ligand ID 2892
名称 celecoxib
别名 Celecox®
类别 Synthetic organic
学名 4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) .
配体家族 Non-steroidal anti-inflammatory ligands
临床描述 Efficacy, Tolerability, and Safety of DFN-15 in episodic migraine with or without aura, being conducted at multiple centers in the United States.
Efficacy, Tolerability, and Safety of DFN-15 in episodic migraine with or without aura, being conducted at multiple centers in the United States
This is a randomized, placebo-controlled Phase I/II multi-center trial, of the safety and efficacy of Celecoxib in a cohort of 81 HNPCC subjects and gene carriers. The three proposed intervention arms are: Celecoxib (to be provided by Searle) will be administered at 200mg p.o. BID x 12 months or 400mg p.o. BID x 12 months vs. Placebo p.o. BID x 12 months. Assessment of endoscopic and tissue-based biomarker endpoints will be conducted at baseline and 12 months on study drug or placebo. Patients that present with polyps at baseline will undergo a month 4 endoscopy. Plasma drug trough samples for pharmacokinetic analyses will be collected at baseline and month 12. NCI-Chemoprevention Branch will coordinate the efforts and activities of all sites. Safety monitoring will occur via in-patient interviews with exams at month twelve; symptom questionnaires completed at baseline, months one, four, eight and twelve; blood and urinalysis at baseline and at months one, four, eight and twelve. A post-administration telephone call to evaluate side effect resolution will occur at months 13-14 for patients who have unresolved adverse events at the end of month 12.
来源公司 Dr. Reddy's Laboratories Limited
Dr. Reddy's Laboratories Limited
National Institutes of Health Clinical Center (CC)

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参考文献

1. Penning TD, Talley JJ, Bertenshaw SR, Carter JS, Collins PW, Docter S, Graneto MJ, Lee LF, Malecha JW, Miyashiro JM et al..  (1997)  Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib)..  J Med Chem,  40  (9):  (1347-65).  [PMID:9135032]
2. Naji S et al..  (2019)  Cadmium Induces Migration of Colon Cancer Cells: Roles of Reactive Oxygen Species, P38 and Cyclooxygenase-2..  Cell Physiol Biochem,  52  (6):  (1517-1534).  [PMID:31120230]
3. Chen L et al..  (2017)  L161982 alleviates collagen-induced arthritis in mice by increasing Treg cells and down-regulating Interleukin-17 and monocyte-chemoattractant protein-1 levels..  BMC Musculoskelet Disord,  18  ():  (462).  [PMID:29145862]
4. Harati R et al..  (2020)  Loss of miR-101-3p Promotes Transmigration of Metastatic Breast Cancer Cells through the Brain Endothelium by Inducing COX-2/MMP1 Signaling..  Pharmaceuticals (Basel),  13  (7):  ().  [PMID:32645833]
5. Dey R & Bishayi B.  (2020)  TLR-2 neutralization potentiates microglial M1 to M2 switching by the combinatorial treatment of ciprofloxacin and dexamethasone during S. aureus infection..  J Neuroimmunol,  344  ():  (577262).  [PMID:32450430]

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