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)
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

产品目录 产品描述 文献引用 实验数据
S5119New

Olivetol

Olivetol 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.

S3021

Rimonabant

Rimonabant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。

S2819

AM251

AM251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。

S8012

Otenabant (CP-945598) HCl

Otenabant (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。

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.

S1544

AM1241

AM1241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。

S2854

BML-190

BML-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。

S2778

GW842166X

GW842166X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 27569

Org 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。

Tags: Cannabinoid Receptor signaling | CB1 receptor signaling | CB2 signaling | Cannabinoid Receptor inhibitor review