XL01126|西域试剂

XL01126,99.81%

产品编号：Bellancom-148030| 分子式：C₅₀H₆₄ClFN₁₀O₆S₂| 分子量：1019.69

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-148030		￥8500.00	杭州北京（现货）

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XL01126

产品介绍

XL01126 是一种强效的 LRRK2 降解剂，DC₅₀ 分别为 14 nM (G2019S LRRK2) 和 32 nM (WT LRRK2)。XL01126 可透过血脑屏障，并作为降解探针，用于帕金森疾病的研究。XL01126 能在 LRRK2 的非催化和框架功能的研究中发挥作用。

生物活性

XL01126 is a potent degrader of LRRK2 with DC₅₀s of 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2), respectively. XL01126 can cross blood-brain barrier and be used as a degrader probe in Parkinson’s disease research. XL01126 exerts function of study of non-catalytic and scaffolding functions of LRRK2.

体外研究

XL01126 (300 nM; 4 h) exhibits strong degradation performance by forming a positively cooperative ternary complex with E3 ubiquitin ligase ligand VHL and target protein LRRK2.
XL01126 (10, 30, 100 nM; 24 h) increases mitophagy in immortalized mouse embryonic fibroblasts cells.
XL01126 (10 μM; 90 min) displays high permeability in Caco-2 cells.
XL01126 (10 μM; 0-60 min; every 15 min interval gradient) exhibits high stability in mouse plasma, liver microsome and hepatocyte.
Pharmacokinetic of XL01126 in vitro

Parameter	Properties
T_1/2 in mouse plasma	108.29 min
T_1/2 in mouse liver microsome	3.65 min
Cl_int in mouse liver microsome	1494.62 mL/min/kg
T_1/2 in mose hepatocytes	314.33 min
Cl_int in mose hepatocytes	26.04 mL/min/kg

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

Western Blot Analysis

Cell Line:	G2019S LRRK2 MEFs (mouse embryonic fibroblasts)
Concentration:	300 nM
Incubation Time:	4 hours
Result:	Resulted LRRK2 pSer935, Rab10 pThr73 decrease.

体内研究
(In Vivo)

XL01126 (30 mg/kg; p.o.; single dose) shows oral activity with bioavailable value (F) of 15% and can penetrate the blood brain barrier after either oral or parenteral dosing in mice.
Pharmacokinetic property of XL01126 in mice

Route	Dose (mg/kg)	CL (L/h/kg)	V_ss (L/kg)	T_max (h)	C_max (ng/mL)	T_1/2 (h)	AUC_last (h·ng/mL)	AUC_inf (h·ng/mL)	MRT (h)	F (%)
p.o.	30			2	3620	21.9	21337	109271		15
i.v.	5	0.208	0.511			1.52	23663	23981	2.45
i.p.	30			0.25	7700	5.2	41434	64068		29.2

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

体内研究

Route	Dose (mg/kg)	CL (L/h/kg)	V_ss (L/kg)	T_max (h)	C_max (ng/mL)	T_1/2 (h)	AUC_last (h·ng/mL)	AUC_inf (h·ng/mL)	MRT (h)	F (%)
p.o.	30			2	3620	21.9	21337	109271		15
i.v.	5	0.208	0.511			1.52	23663	23981	2.45
i.p.	30			0.25	7700	5.2	41434	64068		29.2

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

体内研究

Route	Dose (mg/kg)	CL (L/h/kg)	V_ss (L/kg)	T_max (h)	C_max (ng/mL)	T_1/2 (h)	AUC_last (h·ng/mL)	AUC_inf (h·ng/mL)	MRT (h)	F (%)
p.o.	30			2	3620	21.9	21337	109271		15
i.v.	5	0.208	0.511			1.52	23663	23981	2.45
i.p.	30			0.25	7700	5.2	41434	64068		29.2

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

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (98.07 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.9807 mL	4.9035 mL	9.8069 mL
5 mM	0.1961 mL	0.9807 mL	1.9614 mL
10 mM	0.0981 mL	0.4903 mL	0.9807 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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式