CJ-42794

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CJ-42794

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:

847728-01-2

CJ-042794

CJ-42794 (CJ-042794) 是一种口服有效的选择性前列腺素E受体 4 (EP4) 拮抗剂，其IC₅₀值为 10 nM，其选择性是EP1、EP2和EP3的 200 倍。CJ-42794 可用于胃溃疡的研究。

生物活性

CJ-42794 (CJ-042794) is a potent, orally active, selectiveprostaglandin E receptor 4 (EP4)antagonist with anIC₅₀value of 10 nM, which is 200-fold more selective thanEP1,EP2andEP3. CJ-42794 can be used in research of gastric ulcers^[1]^[2].

IC₅₀& Target

10 nM (EC₅₀)

体外研究
(In Vitro)

CJ-042794 (CJ-042794, 0.3-5000 nM; 10 min; hEP4/HEK293 cells) inhibits the PGE₂-induced elevation of cAMP in a concentration-dependent manner with a pIC₅₀value of 7.5^[1].
CJ-042794 (3-3000 nM; 24 h) reverses the inhibitory effects of PGE₂(10 nM) on the LPS-induced TNFα production in human whole blood (HWB) in a concentration-dependent manner with a pIC50 value of 6.4^[1].

体内研究
(In Vivo)

CJ-042794 (CJ-042794; 0.3-3 mg/kg; i.d.; once) antagonizes the HCO3 stimulatory action of AE1-329 in the duodenum^[1].
CJ-042794 (30 and 50 mg/kg; p.o.; once) does not cause any damage to the gastric mucosa of normal rats and has no gastric ulcerogenic response to cold-restraint stress^[1].
CJ-042794 (30 and 50 mg/kg; p.o.; once) does not damage the stomach and small intestine of helper arthritis rats^[1].
CJ-042794 (3-45 mg/kg; p.o.; twice daily for 14 d; Sprague-Dawley rats) promotes spontaneous healing of gastric ulcers^[1].
CJ-042794 (10 mg/kg; p.o.; daily, for 7 d) repeats administration impairs the healing of chronic gastric ulcers with a down-regulation of vascular endothelial growth factor expression in the ulcerated mucosa^[1].

Animal Model:	Male Sprague-Dawley rats (200-230 g)^[1]
Dosage:	0.3, 1, and 3 mg/kg
Administration:	intradermal injection; once
Result:	Attenuated the PGE₂-stimulated HCO₃secretion in a dose-dependent manner and had the inhibition being 68.9% at 1 mg/kg.

Animal Model:	Male Sprague-Dawley rats (200-230 g)^[1]
Dosage:	30 and 50 mg/kg
Administration:	Oral administration; once
Result:	Did not produce any damage in the gastrointestinal mucosa. Did not produce gastric ulcerogenic response induced by cold-restraint stress.

Animal Model:	Dark Agouti (DA) rats (140-160 g)^[1]
Dosage:	30 and 50 mg/kg
Administration:	Oral administration; once
Result:	Caused any visible damage in the gastric mucosa of normal rats. Had little injurious effect on the small intestine of arthritic rats.

Animal Model:	Male Sprague-Dawley rats (200-230 g)^[1]
Dosage:	3, 10, and 45 mg/kg
Administration:	Oral administration; twice daily for 14 days
Result:	Healed ulcers gradually within 14 days, and the ulcer score on day 17 was 1.6 mm².

Animal Model:	Male Sprague-Dawley rats (200-230 g)^[1]
Dosage:	10 mg/kg
Administration:	Oral administration; daily for 7 days
Result:	Down-regulates the expression of VEGF and decreased the angiogenic response.

分子量

413.83

性状

Solid

Formula

C₂₂H₁₇ClFNO₄

CAS 号

847728-01-2

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 : ≥ 28 mg/mL(67.66 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	2.4165 mL	12.0823 mL	24.1645 mL
5 mM	0.4833 mL	2.4165 mL	4.8329 mL
10 mM	0.2416 mL	1.2082 mL	2.4165 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 (6.04 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.04 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-CDin saline)
Solubility: 2.5 mg/mL (6.04 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.04 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 (6.04 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.04 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。