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  1. GPCR/G Protein Apoptosis NF-κB
  2. Angiotensin Receptor Apoptosis NF-κB
  3. Fimasartan

Fimasartan  (Synonyms: 非馬沙坦; BR-A-657)

目錄號(hào): HY-B0780 純度: 98.55%
COA 產(chǎn)品使用指南

Fimasartan (BR-A-657) 是口服有效的血管緊張素受體 AT1 非肽類拮抗劑。Fimasartan 具有抗高血壓的作用。Fimasartan 可改善腦出血后 NLRP3 炎癥小體介導(dǎo)的神經(jīng)炎癥和腦損傷,具有神經(jīng)保護(hù)的作用。Fimasartan 通過(guò) NF-κB 和激活蛋白-1 失活抑制誘導(dǎo)型一氧化氮合酶的表達(dá)。

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Fimasartan Chemical Structure

Fimasartan Chemical Structure

CAS No. : 247257-48-3

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥331
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5 mg ¥300
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10 mg ¥500
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25 mg ¥823
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50 mg ¥1100
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100 mg ¥1700
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Customer Review

Other Forms of Fimasartan:

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Fimasartan (BRA-657) is an orally effective angiotensin receptor AT1 non-peptide antagonist. Fimasartan has antihypertensive effects. Fimasartan improves neuroinflammation and brain injury mediated by NLRP3 inflammatome after intracerebral hemorrhage, and has neuroprotective effect. Fimasartan inhibits the expression of inducible nitric oxide synthase through the inactivation of NF-κB and activator protein-1[1][2][3].

IC50 & Target

AT1 Receptor

 

體外研究
(In Vitro)

Fimasartan (62.5, 125 和 250 μM; 1 小時(shí)) 在 LPS (HY-D1056) 誘導(dǎo)的 RAW264.7 巨噬細(xì)胞中抑制 NO 產(chǎn)生和誘導(dǎo)型一氧化氮合酶表達(dá)[1]。
Fimasartan (250 μM; 1 小時(shí)) 在 LPS (HY-D1056) 誘導(dǎo)的 RAW264.7 巨噬細(xì)胞中降低 NF-κB 和激活蛋白 1 的活性[1]
Fimasartan (30 ng/mL; 6 小時(shí)) 在溶血液誘導(dǎo)的模擬腦出血的小膠質(zhì)細(xì)胞模型中抑制 NLRP3 炎癥體的激活[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: LPS treated RAW264.7 macrophages
Concentration: 62.5, 125 and 250μM
Incubation Time: 1 h
Result: Reduced the levels of inducible nitric oxide synthase in a concentration‐dependent manner.

Western Blot Analysis[2]

Cell Line: BV2 microglia cell
Concentration: 30 ng/mL
Incubation Time: 6 h
Result: Reduced the levels of NLRPS, ASC and cleaved caspase-1.
體內(nèi)研究
(In Vivo)

Fimasartan (0.5 mg/kg; 口服; 33 天) 可在大鼠腦出血模型中改善 NLRP3 炎癥小體介導(dǎo)的神經(jīng)炎癥和腦損傷[2]。
Fimasartan (0.03-3 mg/kg; 口服/靜脈注射; 3-24 小時(shí)) 在高血壓大鼠中具有降血壓作用[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Intracerebral hemorrhage treated male Sprague-Dawley rats aged four weeks old (65-75 g)[2]
Dosage: Low-dose (0.5 mg/kg); regular-doses (1.0 and 3.0 mg/kg)
Administration: Oral administration (p.o.); 33 days
Result: Reduced blood pressure in a dose-dependent manner in the regular-dose groups, the blood pressure in the low-dose groups was not significantly different from that of control groups.
Attenuated intracerebral hemorrhage-induced edema and improved neurological functions in the regular-dose groups.
Significantly decreased the activation of NLRP3/ASC/caspase-1 and NF-κB pathways after intracerebral hemorrhage in the regular-dose groups.
Animal Model: Male Sprague-Dawley rats (280-320g)[3]
Dosage: 0.03, 0.1, 0.3mg/kg;
1, 3 mg/kg
Administration: Intravenous injection (i.v.); 3 h;
Oral administration (p.o.); 24 h
Result: Significantly decreased in mean arterial blood pressure with rapid onset a dose-dependent manner by i.v. and p.o.
Clinical Trial
分子量

501.65

Formula

C27H31N7OS

CAS 號(hào)
性狀

固體

顏色

Light yellow to yellow

中文名稱

非馬沙坦

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : ≥ 49 mg/mL (97.68 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.9934 mL 9.9671 mL 19.9342 mL
5 mM 0.3987 mL 1.9934 mL 3.9868 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9934 mL 9.9671 mL 19.9342 mL 49.8355 mL
5 mM 0.3987 mL 1.9934 mL 3.9868 mL 9.9671 mL
10 mM 0.1993 mL 0.9967 mL 1.9934 mL 4.9836 mL
15 mM 0.1329 mL 0.6645 mL 1.3289 mL 3.3224 mL
20 mM 0.0997 mL 0.4984 mL 0.9967 mL 2.4918 mL
25 mM 0.0797 mL 0.3987 mL 0.7974 mL 1.9934 mL
30 mM 0.0664 mL 0.3322 mL 0.6645 mL 1.6612 mL
40 mM 0.0498 mL 0.2492 mL 0.4984 mL 1.2459 mL
50 mM 0.0399 mL 0.1993 mL 0.3987 mL 0.9967 mL
60 mM 0.0332 mL 0.1661 mL 0.3322 mL 0.8306 mL
80 mM 0.0249 mL 0.1246 mL 0.2492 mL 0.6229 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱:
Fimasartan
目錄號(hào):
HY-B0780
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