SC-19220 - CAS:19395-87-0

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SC-19220

目录号 : KCM12290 CAS No. : 19395-87-0 纯度 : ≥96%

Data Sheet 产品使用指南

The prostaglandin E (PGE) receptor EP is involved in triggering PGE-mediated pain, neuronal survival and growth as well as the suppression of tumor metastasis. SC-19220 is a dibenzoxazepine that acts as a selective antagonist of PGE at the EP receptor. At doses between 0.3-300 µM, SC-19220 acts as a competitive antagonist of PGE-induced smooth muscle contractions of guinea pig ileum and stomach. SC-19220 also acts as a PGE antagonist in the EP receptor-mediated contraction of guinea pig trachea. SC-19220 displaces radiolabeled PGE from the cloned human EP receptor with an IC of 6.7 µM and exhibits no binding at the human EP receptor. It binds with apparent low affinity to the cloned mouse EP receptor expressed in CHO cells. In a model of bone resorption, 3-150 μM SC-19220 inhibited both 1,25 dihydroxy vitamin D- and PGE-stimulated osteoclastogenesis in mouse osteoclast precursors. Antagonism of EP with 1 μM SC-19220 has been shown to promote metastasis in a mouse model of metastatic breast cancer. In a rodent model of Parkinson’s disease, 1.5 μM SC-19220 prevented PGE-mediated loss of dopaminergic neurons from rat substantia nigra.

规格	价格	是否有货	数量
5mg		In-stock
10mg		In-stock
25mg		In-stock
10 mM * 1 mL in DMSO		In-stock

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6,4'-Dihydroxy-7-methoxyflavanone In-stock
Schizandriside In-stock
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EP2 receptor antagonist-2 In-stock

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生物活性

SC-19220 is a prostaglandin E2 receptor EP1 antagonist. SC-19220 blocks functional EP1 receptor activation, and RANK/RANKL signaling pathway. SC-19220 inhibits osteoclast formation and bone resorption by pre-existing osteoclasts. SC-19220 can be used for the research of osteoporotic disorders, inflammatory bone resorption.

体外研究

SC-19220 (3-150 µM; 8 days) dose-dependently inhibits osteoclast formation and bone resorption induced by 1,25(OH)2D3 and PGE2 in mouse bone marrow cell cultures, achieving complete inhibition at a concentration of 75 µM.
SC-19220 (75 µM; 4 days) inhibits 1,25(OH)2D3-induced osteoclast formation and bone resorption in mouse bone marrow cell cultures.
SC-19220 (75 µM; 1 day) directly inhibits the bone resorption activity of isolated Wistar rat osteoclasts without reducing their number after 1 day of incubation.
SC-19220 (30-150 µM; 7 days) does not inhibit granulocyte/macrophage colony formation induced by GM-CSF in mouse bone marrow cell cultures but instead mildly enhances colony formation.
SC-19220 (75 µM; 8 days) can inhibit the formation of osteoclasts and bone resorption induced by IL-11, IL-6, and PTH in a mouse osteoblast-marrow cell co-culture system.
SC-19220 (5-25 μg/mL; 6-7 days) dose-dependently inhibited PGE2- or 11-deoxy-PGE1- or RANKL/M-CSF-induced osteoclast formation in mouse bone marrow cell culture systems, with the 25 μg/mL concentration nearly completely eliminating the formation of TRACP+ cells.
SC-19220 (5-25 μg/mL; 24 hours) does not alter the expression of RANKL mRNA in PGE2-induced primary mouse calvarial osteoblasts.
SC-19220 (5-25 μg/mL; 1-2 days) dose-dependently reduced mRNA and protein expression of RANK and c-Fms in mouse bone marrow macrophages treated with M-CSF and RANKL, with the highest inhibitory effect observed at a concentration of 25 μg/mL.
SC-19220 (5-25 μg/mL; 2 days) dose-dependently reduced the expression of c-Src protein in mouse bone marrow macrophages treated with M-CSF and RANKL.
SC-19220 (5-25 μg/mL; 1 day) dose-dependently reduced NFAT2 mRNA and protein expression in mouse bone marrow macrophages treated with M-CSF and RANKL, with the strongest inhibitory effect observed at 25 μg/mL after 1 day of incubation .

RT-PCR

Cell Line:

primary mouse calvarial osteoblastic cells

Concentration:

5 μg/mL; 10 μg/mL; 25 μg/mL

Incubation Time:

24 hours

Result:

Did not alter PGE₂-induced RANKL mRNA expression.

Western Blot Analysis

Cell Line:	mouse bone marrow macrophages
Concentration:	5 μg/mL; 10 μg/mL; 25 μg/mL
Incubation Time:	2 days
Result:	Dose-dependently reduced RANK, c-Fms and c-Src expression in mouse bone marrow macrophages treated with M-CSF and RANKL.

Western Blot Analysis

Cell Line:	mouse bone marrow macrophages
Concentration:	5 μg/mL; 10 μg/mL; 25 μg/mL
Incubation Time:	1 day
Result:	Dose-dependently reduced NFAT2 and protein expression in mouse bone marrow macrophages treated with M-CSF and RANKL.

分子式

C₁₆H₁₄ClN₃O₃

分子量

331.75

CAS号

19395-87-0

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 (301.43 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0143 mL	15.0716 mL	30.1432 mL
5 mM	0.6029 mL	3.0143 mL	6.0286 mL
10 mM	0.3014 mL	1.5072 mL	3.0143 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: 2.5 mg/mL (7.54 mM); Clear solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.54 mM) 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。
2.

请依序添加每种溶剂：10% DMSO → 90% corn oil

Solubility: 2.5 mg/mL (7.54 mM); Clear solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.54 mM) 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。