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嗎伐考昔

嗎伐考昔

中文名稱嗎伐考昔
中文同義詞嗎伐考昔;4-(5-(4-氟苯基)-3-(三氟甲基)-1H-吡唑-1-基)苯磺酰胺;優(yōu)選]MAVACOXIB;嗎伐考昔,10 MM DMSO 溶液;嗎伐考昔 Mavacoxib
英文名稱4-[5-(4-FLUOROPHENYL)-3-(TRIFLUOROMETHYL)PYRAZOL-1-YL]BENZENE-1-SULFONAMIDE
英文同義詞4-[5-(4-FLUOROPHENYL)-3-(TRIFLUOROMETHYL)PYRAZOL-1-YL]BENZENE-1-SULFONAMIDE;Mavacoxib;BenzenesulfonaMide, 4-[5-(4-fluorophenyl)-3-(trifluoroMethyl)-1H-pyrazol-1-yl]-;4-[5-(4-Fluorophenyl)-3-trifluoroMethyl-1H-pyrazol-1-yl] benzenesulfonaMide;Trocoxil;PHA 739521;Mavacoxib D4Q: What is Mavacoxib D4 Q: What is the CAS Number of Mavacoxib D4 Q: What is the storage condition of Mavacoxib D4 Q: What are the applications of Mavacoxib D4;MavacoxibQ: What is Mavacoxib Q: What is the CAS Number of Mavacoxib Q: What is the storage condition of Mavacoxib Q: What are the applications of Mavacoxib
CAS號(hào)170569-88-7
分子式C16H11F4N3O2S
分子量385.34
EINECS號(hào)
相關(guān)類別定制;Aromatics, Heterocycles, Inhibitors, Pharmaceuticals, Intermediates & Fine Chemicals
Mol文件170569-88-7.mol
結(jié)構(gòu)式嗎伐考昔 結(jié)構(gòu)式

嗎伐考昔 性質(zhì)

熔點(diǎn)167-169°C
沸點(diǎn)519.8±60.0 °C(Predicted)
密度1.51±0.1 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
溶解度可溶于DMSO(少許)、甲醇(少許)
酸度系數(shù)(pKa)9.67±0.10(Predicted)
形態(tài)固體
顏色灰白色至淺米色

嗎伐考昔 用途與合成方法

嗎伐考昔又叫馬氟考昔,是一種新一代的化合物,具有獨(dú)特的作用機(jī)制即特異性地抑制環(huán)氧化酶?2(COX?2)。炎癥刺激可誘導(dǎo)COX?2生成,因而導(dǎo)致炎性前列腺素類物質(zhì)的合成和聚積,尤其是前列腺素E2,引起炎癥、水腫和疼痛。嗎伐考昔可通過抑制COX?2阻止炎性前列腺素類物質(zhì)的產(chǎn)生,達(dá)到抗炎、鎮(zhèn)痛及退熱作用。

向一個(gè)250ml三頸瓶中依次投入三氟乙酸乙酯(13.60g,0.0958mol),乙醇(20ml),28.4%甲醇鈉的甲醇溶液(16.50g,0.0868mol),然后邊攪拌邊滴加4?氟苯乙酮(10.00g,0.0725mol)。滴畢,將反應(yīng)液升溫至10?15℃反應(yīng)2.5小時(shí)。然后滴加乙酸(6.54g,0.109mol),滴畢,慢慢加入4?氨基磺?;诫蔓}酸鹽。然后將反應(yīng)液在15℃反應(yīng)2小時(shí)。將反應(yīng)液冷至5℃,然后用50%氫氧化鈉調(diào)PH至7。加入乙醇(37ml)和水(31ml),升溫至30℃。緩慢加水(32ml)至反應(yīng)液。將反應(yīng)液冷至5℃,過濾,濾餅用50%乙醇?水溶液(v/v,50克)洗滌倆次。濾餅真空干燥得終產(chǎn)品20.109克,產(chǎn)率72.0%。

170569-88-7的合成

Mavacoxib (Trocoxil)是一種選擇性的、長(zhǎng)效的 cyclooxygenase-2 (COX-2) 抑制劑。Mavacoxib是一種新型的非甾體抗炎藥(NSAID)。
TargetValue
COX-2
()

Mavacoxib (0-200 μM; 72 hours; CSKOS, U2OS, REM, K9TCC and T24 cells) treatment reduces cell viability in a dose-dependent manner. However, sensitivity to Mavacoxib varied between the cell lines, with IC 50 values ranging from 34.5 μM to 157.7 μM. The IC 50 values of U2OS, KTOSA5, CSKOS, REM, LILY, K9TCC, K9TCC-AXA, K9TCC-In, K9TCC-Sh, T24, 5637 and HT-1376 cells are 52.6 μM, 89.8 μM, 106.3 μM, 66.6 μM, 97.5 μM, 54.9 μM, 34.5 μM, 78.7 μM, 50.7 μM, 63.4 μM, 72.5 μM and 157.7 μM, respectively.
Mavacoxib (0-200 μM; 48 hours; KTOSA5, REM, LILY, K9TCC, U2OS, and T24 cells) treatment can induce caspase-dependent apoptosis in a number of cell lines.
Mavacoxib (0-75 μM; 24 hours; CSKOS, U2OS, REM, K9TCC and T24 cells) treatment down-regulates the expression of p-Akt in CSKOS cells in in a dose-dependent manner, as is total Akt in U2OS cells. In REM cells, both p-ERK and p-Akt are increased in expression with increasing doses of Mavacoxib, and in K9TCC cells p-ERK expression is also increased with Mavacoxib treatment.

Cell Viability Assay

Cell Line: CSKOS, U2OS, REM, K9TCC and T24 cells
Concentration: 0 μM, 0.04 μM, 25 μM, 50 μM, 75 μM, 100 μM, 125 μM, 150 μM, 175 μM, 200 μM
Incubation Time: 72 hours
Result: Cell viability was reduced in a dose-dependent manner.

Apoptosis Analysis

Cell Line: KTOSA5, REM, LILY, K9TCC, U2OS, and T24 cells
Concentration: 0 μM, 50 μM, 100 μM, 200 μM
Incubation Time: 48 hours
Result: Induced apoptosis in canine and human cancer cell lines.

Cell Viability Assay

Cell Line: CSKOS, U2OS, REM, K9TCC and T24 cells
Concentration: 0 μM, 25 μM, 50 μM or 75 μM
Incubation Time: 24 hours
Result: In CSKOS cells, p-Akt was downregulated, as was total Akt in U2OS cells. In REM cells, both p-ERK and p-Akt were increased in expression, and in K9TCC cells p-ERK expression was also increased.

Osteoarthritic dogs enrolled in the studies are randomized to receive treatment with Mavacoxib and daily placebo for carprofen or placebo for Mavacoxib and daily carprofen at a nominal dose of 4 mg/kg BW. Mavacoxib is administered in both studies with a 2-week interval between the first and second doses but with monthly dosing thereafter. The nominal Mavacoxib doses in Studies 1 and 2 are 4 and 2 mg/kg BW, respectively. Seven Mavacoxib doses are administered in Study 1, but only five doses in Study 2. In Study 1, Mavacoxib is administered without regard to the timing of meals, but in Study 2, all of the Mavacoxib doses are administered with food.

安全信息

MSDS信息

更新日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2025/05/22HY-119447嗎伐考昔
Mavacoxib
1 mg280元
2025/05/22HY-119447嗎伐考昔
Mavacoxib
170569-88-710mM * 1mLin DMSO509元

嗎伐考昔 上下游產(chǎn)品信息

"嗎伐考昔"相關(guān)產(chǎn)品信息
羅貝考昔 維生素B12 泛昔洛韋 代他考昔
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