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  2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. S 38093

S 38093 是一種可透過大腦的，具有口服活性的 H3 receptor 拮抗劑，對大鼠，小鼠和人的 H3 受體具有不同的親和力，Ki 值分別為 8.8，1.44 和 1.2 μM。

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S 38093 Chemical Structure

S 38093 Chemical Structure

CAS No. : 862896-30-8

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查看 Histamine Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

S 38093 is a brain-penetrant, orally active antagonist of H3 receptor, with Kis of 8.8, 1.44 and 1.2 μM for rat, mouse and human H3 receptors, respectively.

IC50 & Target

Ki: 8.8 μM (Rat H3 receptor), 1.44 μM (Mouse H3 receptor), 1.2 μM (Human H3 receptor)[2]
體外研究
(In Vitro)

In cellular models, S 38093 is able to antagonize mice H3 receptors (KB=0.65 μM) and to suppress cAMP decrease induced by an H3 agonist via human H3 receptors (KB=0.11 μM). In cells expressing a high H3 density, S 38093 behaves as a moderate inverse agonist at rat and human H3 receptors (EC50=9 and 1.7 μM, respectively)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

S 38093 (0.3 and 3?mg/kg/d p.o., 28 days) significantly increases proliferation of progenitors in the DG of hippocampus in young adult mice. S 38093 (0.3?mg/kg/d) treatment significantly increases the number of DCX+ cells with tertiary dendrites. S 38093 (0.3, 1 and/or 3?mg/kg) significantly increases cell proliferation, survival, and maturation in the DG of hippocampus in aged mice relative to vehicle. S 38093 (3?mg/kg/d p.o., 28 days) increases cell proliferation and has a strong effect on cell survival, also increases the dendritic intersections in both genotypes (one-way ANOVA with repeated measure, p?TG mice only. In aged mice, chronic administration of S 38093 (1 and/or 3?mg/kg/day p.o., 28 days) reverses this age-dependent decrease in BDNF-IX, BDNF-IV and BDNF-I transcripts. In addition, S 38093 at three tested doses (0.3, 1 and 3?mg/kg/d) increases VEGF transcripts compared to vehicle-aged group[1]. In mice, S 38093 significantly increases ex vivo N-tele-Methylhistamine cerebral levels from 3 mg/kg p.o. and antagonized R-α-Methylhistamine-induced dipsogenia from 10 mg/kg i.p[2].

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

288.38

Formula

C17H24N2O2
CAS 號
性狀

固體

顏色

White to off-white

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 : 2 mg/mL (6.94 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)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.4676 mL 17.3382 mL 34.6765 mL
5 mM 0.6935 mL 3.4676 mL 6.9353 mL
查看完整儲(chǔ)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(chǔ)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(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?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?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

只
由于實(shí)驗(yàn)過程有損耗，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)
Animal Administration
[1]

The context discrimination task consists of an 8-day contextual fear discrimination paradigm in which the mice have to learn to distinguish between a fearful shock context and a similar non-shock context. On day 1 the mice are only exposed to the training shock context, and on days 2-8 the mice are exposed to the shock and then non-shock context in that order each day. The mice are run through the context discrimination task starting at 10 am and ending at 2 pm and are then gavaged with vehicle or S 38093 at 4 pm each day. The drug and vehicle are always administered after behavioral testing to avoid possible acute effects of the drug on behavior. Learning is measured by the percent time the mice spent freezing and testing is terminated when percent freezing is consistently significantly different between the two contexts. The mice are tested after 29 days of drug treatment. Conditioning is conducted on one side of a Med-Associates shuttle box (ENV-010MC; 20.3?cm?×?15.9?cm?×?21.3?cm high) with a clear plexiglass wall, 3 aluminum walls and a stainless steel grid as a floor. Mouse behavior is recorded by digital video cameras mounted above the conditioning chamber. Freezeframe and Freezeview softwar are used for recording and analyzing freezing behavior, respectively. In training context A, mice are allowed to habituate in new cages outside the room and are then brought into the room in the new cages. The house fan and house light are turned on, the stainless steel grid is exposed, the plexiglass wall is up and a mild anise scent is used as an olfactory cue. The door to the sound dampening enclosure is shut for the duration of the trial. 180?s after the mice are placed in the training context, they are delivered a single footshock of 0.75?mA lasting 2?s. 15?s after the end of the footshock, the mice are placed back into their home cages. Non-alcoholic antiseptic wipes are used to clean the grids and catch trays in between trials. An hour later the mice are brought into the room in paper buckets and put into similar context B. The house fan and house light are turned off, the door of the enclosure is left ajar, plastic placemat sheets are put into the shuttle box to make a high-walled circular enclosure, the plexiglass wall is left down and a mild lemon scent is used as the olfactory cue. The stainless steel grid, a salient feature of both contexts, remained exposed. The mice stayed in the chambers for 180?s without receiving a footshock and are placed back into their home cages. 70% ethanol is used to clean the grids and catch trays between trials. The discrimination ratio allowed for evaluation of discrimination between the two contexts and is computed as follows: A?=?freezing in context A, B?=?freezing in context B, and the discrimination ratio?=?A/(A?+?B). Larger values indicate better discrimination.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

完整儲(chǔ)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(chǔ)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(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?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?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 3.4676 mL 17.3382 mL 34.6765 mL 86.6912 mL
5 mM 0.6935 mL 3.4676 mL 6.9353 mL 17.3382 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：
S 38093
目錄號：
HY-104003
需求量：