SB 452533|cas:459429-39-1|西域试剂

SB 452533,98.92%

产品编号：Bellancom-108458| CAS NO：459429-39-1| 分子式：C₁₈H₂₂BrN₃O| 分子量：376.29

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-108458	￥960.00	杭州北京（现货）
Bellancom-108458	￥1600.00	杭州北京（现货）
Bellancom-108458	￥3120.00	杭州北京（现货）
Bellancom-108458	￥4800.00	杭州北京（现货）
Bellancom-108458	￥7200.00	杭州北京（现货）

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SB 452533

产品介绍

SB 452533 是一种有效的选择性 TRPV1 拮抗剂，pK_b 为 7.8。

生物活性

SB 452533 is a potent and selective TRPV1 antagonist with the pK_b of 7.8.

体外研究

SB 452533 is potent as an antagonist at the cloned recombinant rat TRPV1 receptor in HEK293 cells with a pK_b of 7.7 and a pIC₅₀ of 7.0.
SB-452533 reduces phosphorylation of CAMKK2 and AMPK.

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

Western Blot Analysis

Cell Line:	Skeletal muscle (C2C12) cells
Concentration:	0, 50, 100, 200, and 400 μM
Incubation Time:	30 minutes; followed by 200 μM Capsaicin treatment for another 30 min.
Result:	Significantly reduced Capsaicin-induced phosphorylation of AMPK and CAMKK2.

体内研究
(In Vivo)

Capsaicin (Cap; small dose 2 mg/kg) significantly reduces Bleomycin-induced pulmonary fibrosis in mice. SB-452533 abolishes the effects of small dose Cap.

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

Animal Model:	BALB/c mice bearing pulmonary fibrosis model
Dosage:	2.5 mg/kg
Administration:	Treatment received daily drug via subcutaneous injection for 21 days
Result:	The effect (reduced Bleomycin-induced pulmonary fibrosis) of Cap were abolished in the presence of SB-452533.

体内研究

Capsaicin (Cap; small dose 2 mg/kg) significantly reduces Bleomycin-induced pulmonary fibrosis in mice. SB-452533 abolishes the effects of small dose Cap.

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

Animal Model:	BALB/c mice bearing pulmonary fibrosis model
Dosage:	2.5 mg/kg
Administration:	Treatment received daily drug via subcutaneous injection for 21 days
Result:	The effect (reduced Bleomycin-induced pulmonary fibrosis) of Cap were abolished in the presence of SB-452533.

体内研究

Capsaicin (Cap; small dose 2 mg/kg) significantly reduces Bleomycin-induced pulmonary fibrosis in mice. SB-452533 abolishes the effects of small dose Cap.

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

Animal Model:	BALB/c mice bearing pulmonary fibrosis model
Dosage:	2.5 mg/kg
Administration:	Treatment received daily drug via subcutaneous injection for 21 days
Result:	The effect (reduced Bleomycin-induced pulmonary fibrosis) of Cap were abolished in the presence of SB-452533.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (265.75 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6575 mL	13.2876 mL	26.5752 mL
5 mM	0.5315 mL	2.6575 mL	5.3150 mL
10 mM	0.2658 mL	1.3288 mL	2.6575 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 (protect from light)。-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 (6.64 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.64 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。
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: 2.5 mg/mL (6.64 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.64 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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 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: ≥ 2.5 mg/mL (6.64 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.64 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。