• CB1
  • CB2

CB1 选择性激动剂 | 拮抗剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S8012 Otenabant (CP-945598) HCl Otenabant (CP-945598) HCl is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. Phase 1. Selective hCB1, Ki: 0.7 nM; rCB1, Ki: 2.8 nM
S6735 JD-5037 JD-5037 is a peripherally restricted (PR) cannabinoid-1 receptor blocker with an IC50 value of 2 nM for CB1 receptor and > 1000 nM for CB2 receptor. Selective CB1 receptor, IC50: 2 nM
S3021 Rimonabant (SR141716) Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3. Selective hCB1, IC50: 13.6 nM
S1534 Org 27569 Org 27569 is an allosteric modulator of cannabinoid CB1 receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity. Selective
S2819 AM251 AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain. Selective
S0412 Bay 59-3074 Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki of 55.4 nM, 48.3 nM and 45.5 nM at rat and human CB1 and human CB2 receptors, respectively. Bay 59-3074 displays analgesic properties. Pan rat CB1 receptor, Ki: 55.4 nM; human CB1 receptor, Ki: 48.3 nM
S1544 AM1241 AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor. Pan CB1, Ki: 280 nM
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