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  1. GPCR/G Protein Neuronal Signaling
  2. Orexin Receptor (OX Receptor)
  3. SB-408124 Hydrochloride

SB-408124 Hydrochloride 是一種選擇性的非肽類 OX1 受體拮抗劑,在全細(xì)胞和細(xì)胞膜分析中 Ki 為 57 nM 和 27 nM,比對 OX2 受體的抑制性高 50 倍。

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SB-408124 Hydrochloride Chemical Structure

SB-408124 Hydrochloride Chemical Structure

CAS No. : 1431697-90-3

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5 mg ¥550
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10 mg ¥900
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50 mg ¥2880
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100 mg ¥4600
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Other Forms of SB-408124 Hydrochloride:

查看 Orexin Receptor (OX 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

SB-408124 Hydrochloride is a selective non-peptide orexin receptor 1 (OX1) receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor[1].

IC50 & Target

OX1 Receptor

57 nM (Ki, in whole cell )

OX1 Receptor

27 nM (Ki, in cell membrane)

體外研究
(In Vitro)

Primary neuronal cultures from the hypothalamus of newborn SD rats are incubated with orexin A (1 μM), orexin A (1 μM) together with SB-408124 (100 μM) for 6 h. Orexin A-induced increases in arginine vasopressin (AVP) mRNA levels (2.7-fold) are attenuated by SB-408124 (1.2-fold)[3].

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

體內(nèi)研究
(In Vivo)

SB-408124 reduces anxiety after psychotraumatic exposure. Predator induces acute psychotraumatic exposure decrease corticoliberin level in the rat's amygdala. Intranasal administration of SB-408124 restores it closely to normal and has an anxiolytic effect on animal behaviour[2].
Bilateral paraventricular nucleus microinjection of SB-408124 (30 pmol/50 nL per side) results in a greater reduction in mean arterial pressure (MAP) in high-salt intake (-16?mmHg) compared with NS-fed (-4?mmHg) anesthetized Dahl salt-sensitive rats[3].

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

分子量

392.83

Formula

C19H19ClF2N4O

CAS 號
性狀

固體

顏色

White to gray

運(yùn)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(shí)驗(yàn): 

H2O 中的溶解度 : 1 mg/mL (2.55 mM; 超聲助溶 (<60°C))

DMSO 中的溶解度 : < 1 mg/mL (insoluble or slightly soluble)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5456 mL 12.7282 mL 25.4563 mL
5 mM --- --- ---
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

動物溶解方案計算器
請輸入動物實(shí)驗(yàn)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(shí)驗(yàn)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
您所需的儲備液濃度超過該產(chǎn)品的實(shí)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
H2O 1 mM 2.5456 mL 12.7282 mL 25.4563 mL 63.6408 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:
SB-408124 Hydrochloride
目錄號:
HY-76612
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