GDC-0276|cas:1494581-70-2|西域试剂

GDC-0276,99.51%

产品编号：Bellancom-114237| CAS NO：1494581-70-2| 分子式：C₂₄H₃₁FN₂O₄S| 分子量：462.58

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-114237	￥4500.00	杭州北京（现货）
Bellancom-114237	￥7800.00	杭州北京（现货）
Bellancom-114237	￥24000.00	杭州北京（现货）

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GDC-0276

产品介绍

GDC-0276 是一种有效的、选择性的、可逆的具有口服活性 NaV1.7 抑制剂，其 IC₅₀ 值为 0.4 nM。GDC-0276 耐受性良好，显现良好的药代动力学特征。GDC-0276 可用于疼痛以及解决现有止痛活性分子缺陷，如成瘾和脱靶副作用的相关研究。

生物活性

GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC₅₀ value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects.

体外研究

体内研究

GDC-0276 (oral adminstration; 0.5-5 mg/kg) shows enrichment of 14^C with observed specific activities of 22.6 µCi/mg. GDC-0276 is not detected in urine; however, metabolites in urine were enriched in 14^C with observed specific activities of 19.6 µCi/mg.

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

Animal Model:	Six drug-naïve beagle dogs Group 1 four dogs (n=2 per sex) and Group 2 2 BDC dogs (n=2 male)
Dosage:	0.5, 1, 2, 3, 4, 5 mg/kg
Administration:	Oral adminstration
Result:	Showed mean specific activities of 12.2 µCi/mg (a 24% enrichment) (n=4 animals) and 23.5 µCi/mg (a 139% enrichment) (n=2 animals) for Groups 1 and 2, respectively.

体内研究

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

Animal Model:	Six drug-naïve beagle dogs Group 1 four dogs (n=2 per sex) and Group 2 2 BDC dogs (n=2 male)
Dosage:	0.5, 1, 2, 3, 4, 5 mg/kg
Administration:	Oral adminstration
Result:	Showed mean specific activities of 12.2 µCi/mg (a 24% enrichment) (n=4 animals) and 23.5 µCi/mg (a 139% enrichment) (n=2 animals) for Groups 1 and 2, respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (270.22 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1618 mL	10.8089 mL	21.6179 mL
5 mM	0.4324 mL	2.1618 mL	4.3236 mL
10 mM	0.2162 mL	1.0809 mL	2.1618 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 90% corn oil
Solubility: ≥ 6.25 mg/mL (13.51 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (13.51 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 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。