AM-1241|5mg|K1380-上海高创化学科技有限公司

AM-1241

参考价：¥1056

供货周期：

一周

品牌：

规格：

5mg

货号：

K1380

CAS号：

444912-48-5

SKU:K1380		M. Wt:503.33
Formula:C22H22IN3O3		Solubility:No
Purity:>99%		Storage:2 years at -20 degrees centigrade
CAS No.:444912-48-5		Synonyms:N/A
Chemical NameN/A

Description	AM-1241
Targets	CB2 receptor
IC50	7 nM
In vitro	AM1241 is a CB(2) receptor-selective agonist. AM1241 displays high affinity at the human CB2 receptor with a Ki value of about 7nM, whereas its affinity at the human CB1 receptor is more than 80-fold weaker. In FLIPR assays, AM1241 exhibits antagonist activity, blocking the agonist CP 55,940-evoked Ca2+ response in a concentration dependent manner with a Kb value of 63nM. The antinociceptive actions of AM1241 are blocked by the CB(2) receptor-selective antagonist AM630, but not by the CB(1) receptor-selective antagonist AM251. AM1241 also produces antinociception when injected systemically (intraperitoneally). [1] AM1241 dose-dependently blocks the agonist activity of CP55,940 (4nM) and the inverse agonist activity of SR144528 (100nM) at the human CB2 receptor with Kb values at 27 and 11nM, respectively.[2]
In vivo	AM1241 dose-dependently reverses tactile and thermal hypersensitivity produces by ligation of the L5 and L6 spinal nerves in rats.AM1241 is also active in blocking spinal nerve ligation-induced tactile and thermal hypersensitivity in mice lacking CB1 receptors (CB1-/- mice).[3] In animal models, AM1241 fully reverses carrageenan-induced inflammatory thermal hyperalgesia when injected into the inflamed paw. AM1241 can also inhibits flinching and thermal hyperalgesia produces by hind paw capsaicin injection.[4] AM1241(33, 330 mg/kg i.p.) can suppresses the development of capsaicin-evoked thermal and mechanical hyperalgesia and allodynia. AM1241 also produces a dose-dependent suppression of capsaicin-evoked nocifensive behavior. AM1241 suppresses capsaicin-evoked hyperalgesia and allodynia through a local site of action.[4]
Clinical Trials	N/A
Features	N/A

Description

AM-1241

Targets

CB2 receptor

IC50

7 nM

In vitro

AM1241 is a CB(2) receptor-selective agonist. AM1241 displays high affinity at the human CB2 receptor with a Ki value of about 7nM, whereas its affinity at the human CB1 receptor is more than 80-fold weaker. In FLIPR assays, AM1241 exhibits antagonist activity, blocking the agonist CP 55,940-evoked Ca2+ response in a concentration dependent manner with a Kb value of 63nM. The antinociceptive actions of AM1241 are blocked by the CB(2) receptor-selective antagonist AM630, but not by the CB(1) receptor-selective antagonist AM251. AM1241 also produces antinociception when injected systemically (intraperitoneally). [1] AM1241 dose-dependently blocks the agonist activity of CP55,940 (4nM) and the inverse agonist activity of SR144528 (100nM) at the human CB2 receptor with Kb values at 27 and 11nM, respectively.[2]

In vivo

AM1241 dose-dependently reverses tactile and thermal hypersensitivity produces by ligation of the L5 and L6 spinal nerves in rats.AM1241 is also active in blocking spinal nerve ligation-induced tactile and thermal hypersensitivity in mice lacking CB1 receptors (CB1-/- mice).[3] In animal models, AM1241 fully reverses carrageenan-induced inflammatory thermal hyperalgesia when injected into the inflamed paw. AM1241 can also inhibits flinching and thermal hyperalgesia produces by hind paw capsaicin injection.[4] AM1241(33, 330 mg/kg i.p.) can suppresses the development of capsaicin-evoked thermal and mechanical hyperalgesia and allodynia. AM1241 also produces a dose-dependent suppression of capsaicin-evoked nocifensive behavior. AM1241 suppresses capsaicin-evoked hyperalgesia and allodynia through a local site of action.[4]

Clinical Trials

N/A

Features

N/A