Cannabinoid Receptor
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S5119 | Olivetol | 100 mg/mL | ||
| S3021 | Rimonabant | <1 mg/mL | 25 mg/mL | 2 mg/mL |
| S2819 | AM251 | <1 mg/mL | 40 mg/mL | <1 mg/mL |
| S8012 | Otenabant (CP-945598) HCl | <1 mg/mL | 5 mg/mL | <1 mg/mL |
| S8694 | CID16020046 (CID 16020046) | <1 mg/mL | 85 mg/mL | <1 mg/mL |
| S1544 | AM1241 | <1 mg/mL | 101 mg/mL | <1 mg/mL |
| S2854 | BML-190 | <1 mg/mL | 22 mg/mL | <1 mg/mL |
| S2778 | GW842166X | <1 mg/mL | 20 mg/mL | <1 mg/mL |
| S1534 | Org 27569 | <1 mg/mL | 82 mg/mL | <1 mg/mL |
特异性亚型抑制剂
- Cannabinoid Receptor抑制剂（9）
- 新Cannabinoid Receptor产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S5119New |
OlivetolOlivetol is a naturally occurring organic compound being a precursor in various syntheses of tetrahydrocannabinol. It acts as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. |
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| S3021 |
RimonabantRimonabant是一个大脑中心大麻素受体（CB1）特异性口服拮抗剂。在hCB1转染HEK293细胞中IC50浓度为13.6 nM，EC50浓度为17.3 nM。 |
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| S2819 |
AM251AM251是大麻素CB1受体拮抗剂，IC50为700 nM，在体内与小鼠脑CB1受体结合。 |
Inhibition of CB1 suppresses the proliferation and migration and induces apoptosis of RCC cells. a Western blot analysis of CB1 protein in RCC cell lines (786-O, CAKI-1, CAKI-2, 769-P, A498, and ACHN) and normal cell line HK-2, and β-actin was used as a loading control for western blot assays. b RCC cell lines were treated at the indicated concentrations for different time points, and the cell viability was analyzed by MTT assay. AM251-induced cell death in 769-P cells in a dose- and time-dependent manner. c AM251-induced cell death in 786-O cells in a dose- and timedependent manner. d AM251 reduced migration in 786-O and 769-P cell lines at 20 and 30 μM concentrations. e The transmembrane cell number of 786-O and 769-P cells after treatment with different concentrations of AM251 significantly decreased compared with untreated control. |
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| S8012 |
Otenabant (CP-945598) HClOtenabant (CP-945598) HCl是一种有效的，选择性cannabinoid receptor CB1拮抗剂，Ki为0.7 nM，比作用于人类CB2受体选择性高10，000倍。Phase 1。 |
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| S8694New |
CID16020046 (CID 16020046)CID16020046 is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor. |
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| S1544 |
AM1241AM1241是一种选择性的cannabinoid CB2 receptor激动剂，Ki为3.4 nM，比作用于CB1受体选择性高82倍。 |
AM1241 increased ki67+ positive cells and decreased cardiac fibrosis after MI. A, Masson's trichrome-stained myocardial sections from a sub- group of animals at POD 28. B, Comparison of fibrosis areas in all groups. *, P<0.05 vs. MI group; #, P<0.05 vs. MI+AM group. C, Immunohistochemistry of Ki67 (green), and DAPI (blue) staining in adjacent infarction areas. D, Comparison of ki67 positive cells in all groups. *, P<0.05 vs. MI group; #, P<0.05 vs. MI+AM group. Scale bar, 20 μm. |
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| S2854 |
BML-190BML-190是一种选择性的cannabinoid CB2 receptor逆向激动剂，Ki为435 nM，比作用于CB1受体选择性高50倍。 |
The effect of BML-190 on DSS-treated Rassf1a +/- mice. DSS-treated Rassf1a+/- mice were given 3% DSS in drinking water for 7 days followed by fresh water for recovery for another 7 days. BML-190 was administrated orally (100µg/g body weight) on days 2, 4, 5and 7. BML-190 did not protect DSS-treated Rassf1a+/- from inflammation induced injury. n=6-10 for all. |
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| S2778 |
GW842166XGW842166X是一种有效的，高选择性cannabinoid receptor CB2受体激动剂，EC50为63 nM，对CB1受体没有显著的活性。Phase 2。 |
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| S1534 |
Org 27569Org 27569是cannabinoid CB1 receptor变构调节剂，通过增强激动剂亲和力而诱导CB1受体状态改变，且降低逆向激动剂的亲和力。 |
