Cannabinoid Receptor
信号通路图
研究领域
抑制剂选择性比较
特异性亚型抑制剂
Cannabinoid Receptor产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S5119 |
OlivetolOlivetol (5-Pentylresorcinol, 5-n-Amylresorcinol) 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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| S9413 |
YangoninYangonin (Y100550) is a dienolide kavalactone originally found in Piper methysticum (kava plant) and exhibits neuroprotective, neuromodulatory, and antifungal activities. It activates cannabinoid (CB1) receptors and potentiates the effects of GABA-A receptors. |
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| S3021 |
RimonabantRimonabant (SR141716)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。Rimonabant也是一种acyl CoA:cholesterol acyltransferases(ACAT) 1和2的双重抑制剂并且可抑制分支杆菌的MmpL3。 |
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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. |
|
| 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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| S8694 |
CID16020046CID16020046 (C390-0219)是选择性的GPR55拮抗剂，能够抑制GPR55的固有活性，在酵母中IC50为0.15 μM。CID16020046对其他GPCRs、离子通道、激酶和核受体仅具有微弱活性。 |
||
| S6735 |
JD-5037JD-5037是cannabinoid-1 receptor阻滞剂，对CB1受体的IC50值为2 nM，而对CB2受体的IC50值大于1000 nM。 |
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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 (IMMA)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. |
|
| S8017New |
WIN 55, 212-2 mesylateWIN 55,212-2 Mesylate ((R)-(+)-WIN 55212)是一种有效的 cannabinoid (CB) receptor 的激动剂，对人重组CB2和CB1的Ki值分别为3.3 nM和62.3 nM。 WIN 55,212-2 Mesylate 可调节谷氨酸的传递。 |
||
| S0412New |
Bay 59-3074Bay 59-3074 是一种选择性的 cannabinoid CB1/CB2 receptor 的部分激动剂，在大鼠CB1、人类CB1和人类CB2受体上的Ki值分别为55.4 nM、48.3 nM和45.5 nM。Bay 59-3074 具有镇痛作用。 |
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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。 |
||
| S9048 |
(+)-Gallocatechin(+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant. |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S5119 |
OlivetolOlivetol (5-Pentylresorcinol, 5-n-Amylresorcinol) 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. |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S9413 |
YangoninYangonin (Y100550) is a dienolide kavalactone originally found in Piper methysticum (kava plant) and exhibits neuroprotective, neuromodulatory, and antifungal activities. It activates cannabinoid (CB1) receptors and potentiates the effects of GABA-A receptors. |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S3021 |
RimonabantRimonabant (SR141716)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。Rimonabant也是一种acyl CoA:cholesterol acyltransferases(ACAT) 1和2的双重抑制剂并且可抑制分支杆菌的MmpL3。 |
||
| 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. |
|
| 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。 |
||
| S8694 |
CID16020046CID16020046 (C390-0219)是选择性的GPR55拮抗剂，能够抑制GPR55的固有活性，在酵母中IC50为0.15 μM。CID16020046对其他GPCRs、离子通道、激酶和核受体仅具有微弱活性。 |
||
| S6735 |
JD-5037JD-5037是cannabinoid-1 receptor阻滞剂，对CB1受体的IC50值为2 nM，而对CB2受体的IC50值大于1000 nM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| 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. |
|
| S2854 |
BML-190BML-190 (IMMA)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. |
|
| S8017New |
WIN 55, 212-2 mesylateWIN 55,212-2 Mesylate ((R)-(+)-WIN 55212)是一种有效的 cannabinoid (CB) receptor 的激动剂，对人重组CB2和CB1的Ki值分别为3.3 nM和62.3 nM。 WIN 55,212-2 Mesylate 可调节谷氨酸的传递。 |
||
| S0412New |
Bay 59-3074Bay 59-3074 是一种选择性的 cannabinoid CB1/CB2 receptor 的部分激动剂，在大鼠CB1、人类CB1和人类CB2受体上的Ki值分别为55.4 nM、48.3 nM和45.5 nM。Bay 59-3074 具有镇痛作用。 |
||
| 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。 |
||
| 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。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S9048 |
(+)-Gallocatechin(+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant. |
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