ICI 118,551 hydrochloride

ICI 118,551 hydrochloride 是一種高度選擇性的 β2 adrenergic receptor 拮抗劑，結(jié)合 β2，β1 和 β3 腎上腺素能受體的Ki 值分別為 0.7，49.5 和 611 nM。貨號：HY-13951，CAS：72795-01-8

參數(shù)品牌：HY-13951

產(chǎn)品參數(shù)

品牌：HY-13951

型號：HY-13951

起訂量：1

規(guī)格:：10mg

價格:：￥744

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產(chǎn)品詳情

ICI 118,551 hydrochloride (Synonyms: ICI 118551 hydrochloride)

ICI 118,551 hydrochloride 是一種高度選擇性的 β2 adrenergic receptor 拮抗劑，結(jié)合 β2，β1 和 β3 腎上腺素能受體的K_i 值分別為 0.7，49.5 和 611 nM。

生物活性

ICI 118,551 (hydrochloride) is a highly selective β2 adrenergic receptor antagonist, with K_is of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.

IC₅₀ & Target

Ki: 0.7nM (β2 receptor), 49.5 nM (β1 receptor), 611 nM (β3 receptor)^[4]

體外研究(In Vitro)

ICI 118551 inhibits cAMP accumulation with IC₅₀ of 1.7 μM in IMCD cells^[1]. ICI 118551 (10 μM) induces a prominent vasorelaxation of norepinephrine (NE)-precontracted PA but not AO^[2]. In failing human heart, ICI 118551 has significant effects on beat duration, with time-to-peak contraction and time-to-90% relaxation reduced compared with basal contraction. Negative Inotropic Effect of ICI 118551 Is Not cAMP-Related. Overexpression of β2AR in rabbit myocytes enhances negative inotropic effects of ICI 118551^[3].

體內(nèi)研究(In Vivo)

ICI 118551 (0.2 mg/kg) injected into the jugular vein of the mice, reduces systolic pressure in the pulmonary circuit but not systemic arterial pressure^[2].

分子量:313.86

Formula:C₁₇H₂₈ClNO₂

CAS 號:72795-01-8

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)

In Vitro:

DMSO : 33.33 mg/mL (106.19 mM; Need ultrasonic)

H₂O : 12.5 mg/mL (39.83 mM; Need ultrasonic)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	3.1861 mL	15.9307 mL	31.8613 mL
5 mM	0.6372 mL	3.1861 mL	6.3723 mL
10 mM	0.3186 mL	1.5931 mL	3.1861 mL

*

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。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；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

1.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.97 mM); Clear solution
2.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.97 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.97 mM); Clear solution
4.

請依序添加每種溶劑： PBS
Solubility: 2 mg/mL (6.37 mM); Clear solution; Need ultrasonic

參考文獻(xiàn)

[1]. Yasuda G, et al. The beta 1- and beta 2-adrenoceptor subtypes in cultured rat inner medullary collecting duct cells. Am J Physiol. 1996 Sep;271(3 Pt 2):F762-9.

[2]. Wenzel D, et al. beta(2)-adrenoceptor antagonist ICI 118,551 decreases pulmonary vascular tone in mice via a G(i/o) protein/nitric oxide-coupled pathway. Hypertension. 2009 Jul;54(1):157-63.

[3]. Gong H, et al. Specific beta(2)AR blocker ICI 118,551 actively decreases contraction through a G(i)-coupled form of the beta(2)AR in myocytes from failing human heart. Circulation. 2002 May 28;105(21):2497-503.

[4]. Hoffmann C, et al. Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch Pharmacol. 2004 Feb;369(2):151-9.

ICI 118,551 hydrochloride

ICI 118,551 hydrochloride 是一種高度選擇性的 β2 adrenergic receptor 拮抗劑，結(jié)合 β2，β1 和 β3 腎上腺素能受體的Ki 值分別為 0.7，49.5 和 611 nM。貨號：HY-13951，CAS：72795-01-8

品牌：HY-13951

型號：HY-13951

起訂量：1

規(guī)格:：10mg

價格:：￥744

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產(chǎn)品詳情

ICI 118,551 hydrochloride (Synonyms: ICI 118551 hydrochloride)

ICI 118,551 hydrochloride 是一種高度選擇性的 β2 adrenergic receptor 拮抗劑，結(jié)合 β2，β1 和 β3 腎上腺素能受體的K_i 值分別為 0.7，49.5 和 611 nM。

生物活性

ICI 118,551 (hydrochloride) is a highly selective β2 adrenergic receptor antagonist, with K_is of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.

IC₅₀ & Target

Ki: 0.7nM (β2 receptor), 49.5 nM (β1 receptor), 611 nM (β3 receptor)^[4]

體外研究(In Vitro)

ICI 118551 inhibits cAMP accumulation with IC₅₀ of 1.7 μM in IMCD cells^[1]. ICI 118551 (10 μM) induces a prominent vasorelaxation of norepinephrine (NE)-precontracted PA but not AO^[2]. In failing human heart, ICI 118551 has significant effects on beat duration, with time-to-peak contraction and time-to-90% relaxation reduced compared with basal contraction. Negative Inotropic Effect of ICI 118551 Is Not cAMP-Related. Overexpression of β2AR in rabbit myocytes enhances negative inotropic effects of ICI 118551^[3].

體內(nèi)研究(In Vivo)

ICI 118551 (0.2 mg/kg) injected into the jugular vein of the mice, reduces systolic pressure in the pulmonary circuit but not systemic arterial pressure^[2].

分子量:313.86

Formula:C₁₇H₂₈ClNO₂

CAS 號:72795-01-8

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)

In Vitro:

DMSO : 33.33 mg/mL (106.19 mM; Need ultrasonic)

H₂O : 12.5 mg/mL (39.83 mM; Need ultrasonic)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	3.1861 mL	15.9307 mL	31.8613 mL
5 mM	0.6372 mL	3.1861 mL	6.3723 mL
10 mM	0.3186 mL	1.5931 mL	3.1861 mL

*

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。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；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

1.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.97 mM); Clear solution
2.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.97 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.97 mM); Clear solution
4.

請依序添加每種溶劑： PBS
Solubility: 2 mg/mL (6.37 mM); Clear solution; Need ultrasonic

參考文獻(xiàn)

[1]. Yasuda G, et al. The beta 1- and beta 2-adrenoceptor subtypes in cultured rat inner medullary collecting duct cells. Am J Physiol. 1996 Sep;271(3 Pt 2):F762-9.

[2]. Wenzel D, et al. beta(2)-adrenoceptor antagonist ICI 118,551 decreases pulmonary vascular tone in mice via a G(i/o) protein/nitric oxide-coupled pathway. Hypertension. 2009 Jul;54(1):157-63.

[3]. Gong H, et al. Specific beta(2)AR blocker ICI 118,551 actively decreases contraction through a G(i)-coupled form of the beta(2)AR in myocytes from failing human heart. Circulation. 2002 May 28;105(21):2497-503.

[4]. Hoffmann C, et al. Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch Pharmacol. 2004 Feb;369(2):151-9.

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ICI 118,551 hydrochloride (Synonyms: ICI 118551 hydrochloride)

ICI 118,551 hydrochloride

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ICI 118,551 hydrochloride (Synonyms: ICI 118551 hydrochloride)