FRG8701
目录号 : GC32050
FRG-8701是一种新组氨酸H2-receptor拮抗剂，IC50值为0.25至0.43μM。
Cas No.:108498-50-6
Sample solution is provided at 25 µL, 10mM.
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FRG-8701 is a new Histamine H2-receptor antagonist with an IC50 of ranging from 0.25 to 0.43 μM.
Positive chronotropic response to histamine at 10-5 M is dose dependently inhibited by FRG8701 (FRG-8701) famotidine or cimetidine; and the IC50 values of FRG8701, famotidine and cimetidine are 3.3, 3.0 and 108.6 (×10-7M), respectively.The inhibitory potency of FRG8701 is almost the same as that of famotidine and approximately 33 times greater than that of cimetidine[1].
In the pylorus-ligated (4 hr) rats, each drug, given intraduodenally, dose-dependently inhibits the total acid output. FRG8701 at 10 or 30 mg/kg, given orally or intraperitoneally, significantly prevent the formation of the gastric mucosal lesions induced by 0.4 N HCI+50% ethanol (HCI•ethanol). Other necrotizing agents-induced gastric lesions are also inhibited by treatment of FRG8701. The oral ED50 values against the lesions range from 1.1 to 9.4 mg/kg. FRG8701, given orally, dose-dependently prevents the development of gastric lesions induced by stress and indomethacin. Duodenal ulcer induced by mepirizole is also inhibited with FRG8701. The ED50 values of FRG8701 for each ulcer model range from 1.7 to 6.9 mg/kg[1].
[1]. Shibata M,et al. Effects of FRG-8701 on gastric acid secretion, gastric mucosal lesions by necrotizing agents and experimental gastric or duodenal ulcer in rats. Jpn J Pharmacol. 1990 Nov;54(3):277-85.
Cell experiment: | In this study, male guinea pigs weighing 250-350 g are used. The hearts are excised from animals and right atria are dissected carefully. Atria are suspended in Krebs Henseleit (KH) solution, maintained at 32°C and aerated with 95% O2 and 5% CO2. The tissue is attached with an initial load of 1 g to an isometric transducer and allowed to stabilize for 60 min before histamine application. The histamine response is repeated 10 min after the tissue is incubated with various concentrations of FRG8701 or reference H2-antagonist[1]. |
Animal experiment: | Gastric mucosal lesions are produced using various kinds of necrotizing agents. One hour after necrotizing agent treatment, the animals are sacrificed. The stomach is removed and in flated by injecting 10 mL of 2% formalin. Subsequently, the stomach is incised along the curvature and examined for macroscopic hemorrhagic damages under a dissecting microscope (×10). In addition, FRG8701 is given intraperitoneally before HCI-ethanol treatment[1]. |
References: [1]. Shibata M,et al. Effects of FRG-8701 on gastric acid secretion, gastric mucosal lesions by necrotizing agents and experimental gastric or duodenal ulcer in rats. Jpn J Pharmacol. 1990 Nov;54(3):277-85. | |
| Cas No. | 108498-50-6 | SDF | |
| Canonical SMILES | O=C(NCCCOC1=CC=CC(CN2CCCCC2)=C1)CS(CC3=CC=CO3)=O | ||
| 分子式 | C22H30N2O4S | 分子量 | 418.55 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3892 mL | 11.946 mL | 23.892 mL |
| 5 mM | 0.4778 mL | 2.3892 mL | 4.7784 mL |
| 10 mM | 0.2389 mL | 1.1946 mL | 2.3892 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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