SB-674042|cas:483313-22-0|西域试剂

SB-674042,99.84%

产品编号：Bellancom-10898| CAS NO：483313-22-0| 分子式：C₂₄H₂₁FN₄O₂S| 分子量：448.51

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-10898		￥921.00	杭州北京（现货）
Bellancom-10898		￥1534.00	杭州北京（现货）

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SB-674042

产品介绍

SB-674042 是非肽类食欲肽 OX₁ 受体拮抗剂 (K_d=5.03 nM)，对 OX₁ 受体的结合能力约是对 OX₂ 受体 100 倍，IC₅₀ 分别为 3.76 nM 和 531 nM。

生物活性

SB-674042 is a potent and selective non-peptide orexin OX₁ receptor antagonist (K_d=5.03 nM), exhibits 100-fold selectivity for OX₁ over OX₂ receptors with IC₅₀ values of 3.76 nM and 531 nM, respectively^[4].

体外研究

SB-674042 ([³H]) (0.2-24 nM; 2 h) shows high-affinity and serves as a radio ligand suitable for labelling human OX1 receptors stably expressed in CHO cells.
SB-674042 (5 μM; 4 ℃ for 30 min, and 37 ℃ for 3 h) reduces the potency of CB1 receptor agonist (HY-14137) to phosphorylate ERK1/2 in HEK293 cells co-expressing the orexin-1 and CB1 receptors.
SB-674042 (1 μM; 24 h) eradicates the increase in mTOR phosphorylation in response to Orexin-A (HY-106224) (1 nM-1 μM; 24 h) in INS-1 cells, indicating activation of the mTOR pathway induced by orexin-A was dependent on the activated OX1 receptor.

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

Western Blot Analysis

Cell Line:	INS-1 cells
Concentration:	1 μM
Incubation Time:	24 hours; accompanied with 1 μM Orexin-A for 24 hour
Result:	Decreased the phosphorylation level of mTOR induced by Orexin-A.

体内研究
(In Vivo)

SB-674042 (0.3 nM/0.3 μL; icv; single dose) reduces contextual and cues fear freezing responses in Stay animals in Stress Alternatives Model (SMA) in mice^[4].

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

Animal Model:	Stress-induced mice model (male C57BL/6NHsd mice, 22-26 g)^[4]
Dosage:	0.3 nM/0.3 μL
Administration:	Intracerebroventricular injection; subjected mice to 4 days of social aggression (days 1-4)
Result:	Resulted 39.4% Escape and 60.6% Stay phenotypes among mice.

体内研究

SB-674042 (0.3 nM/0.3 μL; icv; single dose) reduces contextual and cues fear freezing responses in Stay animals in Stress Alternatives Model (SMA) in mice^[4].

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

Animal Model:	Stress-induced mice model (male C57BL/6NHsd mice, 22-26 g)^[4]
Dosage:	0.3 nM/0.3 μL
Administration:	Intracerebroventricular injection; subjected mice to 4 days of social aggression (days 1-4)
Result:	Resulted 39.4% Escape and 60.6% Stay phenotypes among mice.

体内研究

SB-674042 (0.3 nM/0.3 μL; icv; single dose) reduces contextual and cues fear freezing responses in Stay animals in Stress Alternatives Model (SMA) in mice^[4].

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

Animal Model:	Stress-induced mice model (male C57BL/6NHsd mice, 22-26 g)^[4]
Dosage:	0.3 nM/0.3 μL
Administration:	Intracerebroventricular injection; subjected mice to 4 days of social aggression (days 1-4)
Result:	Resulted 39.4% Escape and 60.6% Stay phenotypes among mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (55.74 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2296 mL	11.1480 mL	22.2960 mL
5 mM	0.4459 mL	2.2296 mL	4.4592 mL
10 mM	0.2230 mL	1.1148 mL	2.2296 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: ≥ 1.43 mg/mL (3.19 mM); Clear solution

此方案可获得 ≥ 1.43 mg/mL (3.19 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 14.3 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.43 mg/mL (3.19 mM); Clear solution

此方案可获得 ≥ 1.43 mg/mL (3.19 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.43 mg/mL (3.19 mM); Clear solution

此方案可获得 ≥ 1.43 mg/mL (3.19 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 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。