EDP-305

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EDP-305

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1933507-63-1

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议

产品介绍

EDP-305 是一种口服有效且选择性的 farnesoid X 受体 (FXR) 激动剂，其EC₅₀值为 34 nM (CHO 细胞嵌合性 FXR) 和 8 nM (HEK 细胞全长 FXR)。EDP-305 显示出强大而持久的抗纤维化作用。EDP-305 可用于原发性胆道胆管炎 (PBC) 和非酒精性脂肪性肝炎 (NASH) 研究。

生物活性

EDP-305 is an orally active, potent and selectivefarnesoid X receptor (FXR)agonist, withEC₅₀values of 34 nM (chimericFXRin CHO cells) and 8 nM (full-lengthFXRin HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research^[1]^[2].

IC₅₀& Target

IC50: 8 ± 3 nM (Full-length FXR in HEK cells), 34 ± 8 nM (Chimeric FXR in CHO cells), >15000 nM (TGR5 in CHO cells)^[2]

体外研究
(In Vitro)

EDP‐305 (10 μM, 72 h) directly activates FXR in liver hepatoctyes but not stellate cells^[1].
EDP-305 (0-5 μM, 16 h) increases the expression of the FXR target gene, SHP, and downregulates CYP7A1 expression in HepaRG hepatocytes^[2].

Western Blot Analysis^[1]

Cell Line:	Hepatic stellate cell (HSC) lines, primary HSCs and hepatocytes
Concentration:	10 μM
Incubation Time:	72 h
Result:	Induced mRNA expression of SHP and FGF19 in human hepatocytes, and elicited no induction of downstream targets SHP or FGF15/19 in stellate lines.

RT-PCR^[2]

Cell Line:	HepaRG hepatocytes
Concentration:	0.05, 0.1, 0.5, 1, 5, 10, 50, 100, 500, 1000, 5000 nM
Incubation Time:	16 h
Result:	Dose-dependently increased the expression of the FXR target gene, SHP, and downregulated CYP7A1 expression in HepaRG hepatocytes.

体内研究
(In Vivo)

EDP‐305 (0-30 mg/kg, Oral gavage, daily for 2 weeks) reduces serum markers of liver injury, and reduces liver fibrosis in a dose-dependent manner in BDL rats^[1].
EDP‐305 (0-30 mg/kg, Oral gavage, daily for 6 weeks) reduces liver fibrosis in a dose-dependent manner in CDAHFD mice^[1].

Animal Model:	Male CD rats (underwent BDL, n=24, n=8 for each group)^[1]
Dosage:	0, 10 and 30 mg/kg
Administration:	Oral gavage, daily, started on day 4 after BDL and continued until days 17-18
Result:	Significantly reduced alanine aminotransferase and aspartate aminotransferase. Showed a dose-dependent reduction in CPA. Reduced hydroxyproline levels in whole liver tissue samples. Reduced messenger RNA (mRNA) relative quantification (RQ) for both Col1a1 and actin, alpha 2, smooth muscle, aorta (Acta2).

Animal Model:	Male C57BL/6 mice (n = 24, fed a CDAHFD consisting of 60% kcal fat and 0.1% methionine)^[1]
Dosage:	0, 10 and 30 mg/kg
Administration:	Oral gavage, daily, started at the beginning of week 6 on the diet and were continued until week 12
Result:	Reduced serum triglycerides, and significantly reduced hydroxyproline and MR liver signal intensity in a dose-dependent manner. Showed a dose‐dependent reduction in mRNA expression of lysyl oxidase genes Lox and Loxl1-4.

Clinical Trial

分子量

630.92

性状

Solid

Formula

C₃₆H₅₈N₂O₅S

CAS 号

1933507-63-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL(158.50 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	1.5850 mL	7.9249 mL	15.8499 mL
5 mM	0.3170 mL	1.5850 mL	3.1700 mL
10 mM	0.1585 mL	0.7925 mL	1.5850 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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 (3.96 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (3.96 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 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-CDin saline)
Solubility: 2.5 mg/mL (3.96 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (3.96 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 μL20% 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 (3.96 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.96 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。

*以上所有助溶剂都可在本网站选购。