SB-649868 - CAS:380899-24-1

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SB-649868 (Synonyms:GSK649868)

目录号 : KM3389 CAS No. : 380899-24-1

Data Sheet 产品使用指南

SB-649868 是一种口服有效的选择性食欲素 OX1 和 OX 2 受体拮抗剂 (作用于 OX1 和 OX2 受体，pK_i 分别为 9.4 和 9.5)。

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5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

SB-649868 is a potent and selective orally active orexin (OX) 1 and OX₂ receptor antagonist (pK_i =9.4 and 9.5 at the OX₁ and OX₂ receptor, respectively).

体外研究

SB-649868 is identified as one the most in vitro potent dual OX₁ and OX₂ receptor antagonist known at that time (pK_i=9.4 and 9.5 at the OX₁ and OX₂ receptor, respectively) . SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pK_B value (OX₁=9.67; OX₂=9.64). SB-649868 displaces the [H]ACT-078573 receptor binding with the following pKi values: OX₁=9.27; OX₂=8.91. Increasing concentrations of SB-649868 (0.3 nM-30 nM) induces a rightward shift of the orexin-A CRCs with a depression of the agonist efficacy suggesting a clear non-surmountable behavior. The calculated apparent pK_b values are 9.67±0.03 and 9.64±0.07 for OX₁ and OX₂.

体内研究

Pharmacokinetic studies in the male CD rat, performed at 1 mg/kg, iv and 3 mg/kg, po, demonstrate an excellent pharmacokinetic profile for a hypnotic agent featuring moderate clearance in plasma (Cl_p=24 mL/min/kg), short half-life of (<0.6 h) and a low volume of distribution (V_ss=1.1 l/kg), coupled with excellent oral bioavailability (F=85%) and good exposure in plasma (C_max=333 ng/mL). A brain to blood ratio (B/B) of 0.1:1 is observed 1 h after iv administration, a value in line with the expected partition between the two compartments based on the lower tissue binding observed in vitro in brain tissues (fraction unbound/brain=5.28%) with respect to plasma proteins (fraction unbound/plasma=1.34%). SB-649868, administered orally 3 h before OX-A injection at doses of 1, 3 and 10 mg/kg, causes a dose-dependent reduction of OX-A induced grooming as measured by total time spent grooming and number of grooming bouts (p <0.01 at 3 and 10 mg/kg po) . From dissociation kinetic studies using [H]ACT-078573, the calculated long half-life, (t_1/2) supports the non-surmountability profile of SB-649868 (t_1/2=35.91 min) at OX₁ orexin receptor. The long or moderately long t_1/2values for SB-649868 at OX₂ orexin receptor (t_1/2=8.09 min).

分子式

C₂₆H₂₄N₃O₃FS

分子量

477.55

CAS号

380899-24-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (209.40 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0940 mL	10.4701 mL	20.9402 mL
5 mM	0.4188 mL	2.0940 mL	4.1880 mL
10 mM	0.2094 mL	1.0470 mL	2.0940 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.24 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.24 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。