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  1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. Roxatidine Acetate Hydrochloride

Roxatidine Acetate Hydrochloride  (Synonyms: 鹽酸羅沙替丁醋酸酯; HOE 760)

目錄號: HY-B0305A 純度: 99.26%
COA 產(chǎn)品使用指南

Roxatidine Acetate Hydrochloride 是一種有效的、選擇性的、競爭性的、具有口服活性的組胺 H2 受體(histamine H2-receptor)拮抗劑。Roxatidine Acetate Hydrochloride 對胃酸分泌有抗分泌作用。Roxatidine Acetate Hydrochloride 還能抑制炎癥反應(yīng),可用于胃潰瘍和十二指腸潰瘍的研究。Roxatidine Acetate Hydrochloride 具有抗腫瘤活性。

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Roxatidine Acetate Hydrochloride Chemical Structure

Roxatidine Acetate Hydrochloride Chemical Structure

CAS No. : 93793-83-0

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10 mM * 1 mL in DMSO ¥660
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500 mg ¥600
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1 g ¥980
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5 g ¥2800
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Other Forms of Roxatidine Acetate Hydrochloride:

查看 Histamine Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Roxatidine Acetate Hydrochloride is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine Acetate Hydrochloride has antisecretory potency against gastric acid secretion. Roxatidine Acetate Hydrochloride can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine Acetate Hydrochloride has antitumor activity[1][2][3].

IC50 & Target[1]

H2 Receptor

 

體外研究
(In Vitro)

Roxatidine Acetate Hydrochloride (0-120 μM, 1 h) suppresses inflammatory responses via inhibition of NF-κB and p38 MAPK activation in LPS-induced RAW 264.7 macrophages[2].
Roxatidine Acetate Hydrochloride (6.25 ?μM, 12.5?μM, and 25?μM; pre-treatment for 30?min) suppresses the PMACI-induced activation of p38 MAPK, but does not affect the phosphorylation of ERK or JNK. The total ERK 1/2, JNK, and p38 MAPK levels are unaffected by roxatidine in human mast-cells-1 (HMC-1) cells[4].

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

Western Blot Analysis[2]

Cell Line: RAW 264.7
Concentration: 40, 80, and 120 μM
Incubation Time: 1 h
Result: Suppressed LPS-induced PGE2, NO, and histamine production and COX-2, iNOS, and HDC expressions. Inhibited expressions of TNF-α, IL-1β, IL-6, and VEGF-1. Concentration-dependently attenuated the nuclear translocations of p65 and p50. Inhibited LPS-induced phosphorylation of p38 MAP kinase. Significantly down-regulated the LPS-induced productions of NO and PGE2 (prostaglandin E2).
體內(nèi)研究
(In Vivo)

Roxatidine Acetate Hydrochloride (0-300 mg/kg; p.o.; 26 days) suppressed growth of Colon 38 tumor implants in mice[3].
Roxatidine Acetate Hydrochloride (oral gavage; 20?mg/kg; single dose) inhibits Compound 48/80-increased TNF-α, IL-6, and IL-1β production and mRNA expression. Additionally, Roxatidine Acetate Hydrochloride decreases the compound 48/80-induced degradation of procaspase-1 and appearance of the corresponding cleaved bands in mice[4].

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

Animal Model: Male C57BL/6 Colon 38-bearing mice (8-week-old, 20 – 22 g)[3]
Dosage: 30, 100, and 300 mg/kg per day, 1 ml/100 g body weight
Administration: Oral administration, 29 days beginning 3 days before Colon 38 implantation or 26 days beginning concomitantly with Colon 38 implantation
Result: Suppressed growth of Colon 38 tumor implants in a dose-related manner after day 26. Suppressed VEGF levels in tumor tissue and significantly decreased serum VEGF levels.
Animal Model: ICR male mice (6 weeks old)[1]
Dosage: 20?mg/kg
Administration: Oral gavage; 20?mg/kg; single dose
Result: Suppressed compound 48/80-induced allergic inflammation in anaphylactic animal model.
分子量

384.90

Formula

C19H29ClN2O4

CAS 號
性狀

固體

顏色

White to off-white

中文名稱

鹽酸羅沙替丁醋酸酯;鹽酸醋酸羅沙替丁

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細(xì)胞實驗: 

DMSO 中的溶解度 : 50 mg/mL (129.90 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

H2O 中的溶解度 : ≥ 50 mg/mL (129.90 mM)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5981 mL 12.9904 mL 25.9808 mL
5 mM 0.5196 mL 2.5981 mL 5.1962 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

* 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗:

以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請依序添加每種溶劑: PBS

    Solubility: 140 mg/mL (363.73 mM); 澄清溶液; 超聲助溶

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
該產(chǎn)品水溶性佳,請具體參考實測 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(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 / H2O 1 mM 2.5981 mL 12.9904 mL 25.9808 mL 64.9519 mL
5 mM 0.5196 mL 2.5981 mL 5.1962 mL 12.9904 mL
10 mM 0.2598 mL 1.2990 mL 2.5981 mL 6.4952 mL
15 mM 0.1732 mL 0.8660 mL 1.7321 mL 4.3301 mL
20 mM 0.1299 mL 0.6495 mL 1.2990 mL 3.2476 mL
25 mM 0.1039 mL 0.5196 mL 1.0392 mL 2.5981 mL
30 mM 0.0866 mL 0.4330 mL 0.8660 mL 2.1651 mL
40 mM 0.0650 mL 0.3248 mL 0.6495 mL 1.6238 mL
50 mM 0.0520 mL 0.2598 mL 0.5196 mL 1.2990 mL
60 mM 0.0433 mL 0.2165 mL 0.4330 mL 1.0825 mL
80 mM 0.0325 mL 0.1624 mL 0.3248 mL 0.8119 mL
100 mM 0.0260 mL 0.1299 mL 0.2598 mL 0.6495 mL

* 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

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:
Roxatidine Acetate Hydrochloride
目錄號:
HY-B0305A
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