GNE-3511|cas:1496581-76-0|西域试剂

GNE-3511,99.85%

产品编号：Bellancom-12947| CAS NO：1496581-76-0| 分子式：C₂₃H₂₆F₂N₆O| 分子量：440.49

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货号	价格	库存与货期
Bellancom-12947	￥900.00	杭州北京（现货）
Bellancom-12947	￥1500.00	杭州北京（现货）
Bellancom-12947	￥2200.00	杭州北京（现货）
Bellancom-12947	￥3520.00	杭州北京（现货）

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GNE-3511

产品介绍

GNE-3511 是一种生物可利用性和脑渗透 dual leucine zipper kinase (DLK) 抑制剂，具有口服活性，其 K_i 值为 0.5 nM。GNE-3511 可穿过血脑屏障，被用于神经退行性疾病的研究。

生物活性

GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a K_i of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases.

体外研究

GNE-3511 has inhibitory activity for p-JNK and DRG with IC₅₀ values of 30 nM and 107 nM, respectively.
GNE-3511 has kinase selectivity for MKK4, MKK7, JNK1, JNK2, JNK3, MLK1, MLK2 and MLK3 with IC₅₀ values of ＞5000 nM, ＞5000 nM, 129 nM, 514 nM, 364 nM, 67.8 nM, 767 nM and 602 nM, respectively.
GNE-3511 displays concentration-dependent protection of neurons from degeneration in vitro.

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

体内研究

GNE-3511 (oral gavage; 75 mg/kg; single) suppresses CYP-induced nociceptive behavior by inhibiting DLK in mice.
GNE-3511 (oral gavage; 75 mg/kg; single) suppresses CYP-induced edema and hemorrhage in mouse bladder.
GNE-3511 (iv.; 1 mg/kg or po.; 5 mg/kg) exhibits moderate in vivo plasma clearances, moderate volumes of distribution, short half-lives, and brain penetration.
Pharmacokinetic Parameters of GNE-3511 (iv.; 1 mg/kg or po.; 5 mg/kg).

species	CL_p (mL/min/kg	Vd_ss (L/kg	t_1/2 (h)	F (%)	B_u/P_u	CSF/P_u
mouse	56	2.5	0.6	45	0.24 at 6 h
rat	30	3.7	1.8	63	0.7	0.4
dog	41	6.5	4	32		0.4
cynomolgous	16	3.1	2.4	19		0.6

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

Animal Model:	Cystitis mouse model
Dosage:	75 mg/kg
Administration:	oral gavage;75 mg/kg; single
Result:	Significantly reduced the number of nociceptive behavior as well as nociceptive score. Had no impact on bladder weight, did not induce bladder edema or hemorrhage and significantly suppressed CYP-induced increase in bladder weight, bladder edema, and hemorrhage.

Animal Model:	mouse, rat, cynomolgus and dog
Dosage:	1 mg/k, 5 mg/kg
Administration:	iv.; 1 mg/kg or po.; 5 mg/kg
Result:	Exhibited moderate in vivo plasma clearances, moderate volumes of distribution, short half-lives and brain penetration.

体内研究

species	CL_p (mL/min/kg	Vd_ss (L/kg	t_1/2 (h)	F (%)	B_u/P_u	CSF/P_u
mouse	56	2.5	0.6	45	0.24 at 6 h
rat	30	3.7	1.8	63	0.7	0.4
dog	41	6.5	4	32		0.4
cynomolgous	16	3.1	2.4	19		0.6

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

Animal Model:	Cystitis mouse model
Dosage:	75 mg/kg
Administration:	oral gavage;75 mg/kg; single
Result:	Significantly reduced the number of nociceptive behavior as well as nociceptive score. Had no impact on bladder weight, did not induce bladder edema or hemorrhage and significantly suppressed CYP-induced increase in bladder weight, bladder edema, and hemorrhage.

Animal Model:	mouse, rat, cynomolgus and dog
Dosage:	1 mg/k, 5 mg/kg
Administration:	iv.; 1 mg/kg or po.; 5 mg/kg
Result:	Exhibited moderate in vivo plasma clearances, moderate volumes of distribution, short half-lives and brain penetration.

性状

Solid

溶解性数据

In Vitro:

DMSO : 31.25 mg/mL (70.94 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2702 mL	11.3510 mL	22.7020 mL
5 mM	0.4540 mL	2.2702 mL	4.5404 mL
10 mM	0.2270 mL	1.1351 mL	2.2702 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: ≥ 2.08 mg/mL (4.72 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.72 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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