ReN-1869 hydrochloride (NNC-05-1869 hydrochloride)
(Synonyms: NNC-05-1869 hydrochloride) 目录号 : GC31812
ReN 1869 hydrochloride 是一种新型选择性组胺 H1 受体拮抗剂，对组胺 H1 受体（豚鼠脑）具有亲和力，Ki 为 0.19±；0.04 μ；M 和非选择性 σ；位点（豚鼠脑），Ki 为 0.45 μ；M.
Cas No.:170149-76-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | ReN 1869 is labelled with 3H in the tricyclic ring system resulting in a specific activity of 40 Ci/mmol. Thawed membranes (1 mg protein/tube), test compounds and [3H]ReN 1869 are added to test tubes in a final volume of 0.5 mL. Unless otherwise indicated, the concentration of the radioligand is 5 nM and non-specific binding is defined as the binding in the presence of 10 μM ReN 1869. Samples are incubated for 120 min at 37 °C in a shaking water bath. Free and bound radioactivity is separated by filtration over Whatman GF/F filters that are washed with 25 mL of ice-cold buffer (20 mM Tris-HCl, pH 7.4). Radioligand bound to filters accounted for 5-700 dpm that is subtracted before calculating specific binding[1]. |
References: [1]. Olsen UB, et al. ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation. Eur J Pharmacol. 2002 Jan 18;435(1):43-57. | |
ReN 1869 hydrochloride is a novel, selective histamine H1 receptor antagonist, which demonstrates affinity to the histamine H1 receptor (guinea pig brain) with Ki of 0.19±0.04 μM and the non-selective σ site (guinea pig brain) with Ki of 0.45 μM.
ReN 1869 is a highly selective tricyclic antihistamine that shows functional histamine H1 receptor antagonism. Binding studies with radioactively labelled ReN 1869 reveals high affinity only for the histamine H1 receptor in addition to some affinity for a sigma site. ReN 1869 is profiled for activity at 10 μM at various receptors, transporters, enzymes and ion channels. ReN 1869 only demonstrates affinity to the histamine H1 receptor (guinea pig brain, [3H]pyrilamine) with a Ki of 0.19±0.04 μM and the non-selective σ site [guinea pig brain, [3H]1,3-di-tolylguanidine (DTG)] with a Ki of 0.45 μM. ReN 1869 dose-dependently reduces the responses with IC50 of 1.70±0.002 μM[1].
The in vivo binding of [3H]Mepyramine to mouse spinal cord and cerebellar histamine H1 receptors is dose-dependently inhibited by ReN 1869. ReN 1869 (in doses as low as 10 μg/kg i.p.) significantly inhibits the histamine-evoked paw edema. The ED50 is approximately 300 μg/kg. Interestingly, even a high dose of Mepyramine (10 mg/kg) is unable to inhibit significantly this type of edema (0.29±0.06 versus 0.34±0.05 in controls, n=7).ReN 1869 (1 mg/kg s.c.) is administered 30 min before paw injection with carrageenan and has no effect on the development of the paw edema. Dexamethasone (1 mg/kg s.c.) is given 1 h before carrageenan and expectedly diminished the edema. This effect is not affected by the simultaneous administration of 1 mg/kg ReN 1869[1].
[1]. Olsen UB, et al. ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation. Eur J Pharmacol. 2002 Jan 18;435(1):43-57.
| Cas No. | 170149-76-5 | SDF | |
| 别名 | NNC-05-1869 hydrochloride | ||
| Canonical SMILES | O=C([C@H]1CN(CC/C=C2C3=CC=CC=C3CCC4=CC=CC=C\24)CCC1)O.[H]Cl | ||
| 分子式 | C24H28ClNO2 | 分子量 | 397.94 |
| 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 | 2.5129 mL | 12.5647 mL | 25.1294 mL |
| 5 mM | 0.5026 mL | 2.5129 mL | 5.0259 mL |
| 10 mM | 0.2513 mL | 1.2565 mL | 2.5129 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。