(R,S)-AM1241

 化学構造式
444912-48-5
CAS番号.
444912-48-5
化学名:
别名:
英語名:
(R,S)-AM1241
英語别名:
Methanone, (2-iodo-5-nitrophenyl)[1-[(1-methyl-2-piperidinyl)methyl]-1H-indol-3-yl]-;(R,S)-AM1241;AM1241 (AM-1241;(R,S)-AM1241 USP/EP/BP;(R,S)-3-(2-Iodo-5-nitrobenzoyl)-1-(1-methyl-2-piperidinylmethyl)-1H-indole;(3-iodo-5-nitrophenyl)-[1-[(1-methylpiperidin-2-yl)methyl]indol-3-yl]methanone;(2-iodo-5-nitrophenyl)-[1-[(1-methylpiperidin-2-yl)methyl]indol-3-yl]methanone;(2-Iodo-5-nitrophenyl)[1-[(1-methyl-2-piperidinyl)methyl]-1H-indol-3-yl]methanone;(2-Iodo-5-nitrophenyl)(1-((1-methylpiperidin-2-yl)methyl)-1H-Indol-3-yl)methanone
CBNumber:
CB4972473
化学式:
C22H22IN3O3
分子量:
503.33
MOL File:
444912-48-5.mol

(R,S)-AM1241 物理性質

沸点 :
630.7±55.0 °C(Predicted)
比重(密度) :
1.60±0.1 g/cm3(Predicted)
貯蔵温度 :
Store at -20°C
溶解性:
DMSO: 60°Cで~18mg/mL
酸解離定数(Pka):
9.73±0.10(Predicted)
外見 :
個体
色:
黄色
安全性情報
  • リスクと安全性に関する声明
  • 危険有害性情報のコード(GHS)
主な危険性  Xn
Rフレーズ  36/37/38-42/43
Sフレーズ  22-26-36/37-45
WGK Germany  3
絵表示(GHS) GHS hazard pictogramsGHS hazard pictograms
注意喚起語 危険
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H315 皮膚刺激 皮膚腐食性/刺激性 2 警告 GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 強い眼刺激 眼に対する重篤な損傷性/眼刺激 性 2A 警告 GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H334 吸入するとアレルギー、喘息または、呼吸困難 を起こすおそれ 感作性、呼吸器 1 危険 GHS hazard pictograms P261, P285, P304+P341, P342+P311,P501
H335 呼吸器への刺激のおそれ 特定標的臓器毒性、単回暴露; 気道刺激性 3 警告 GHS hazard pictograms
注意書き
P302+P352 皮膚に付着した場合:多量の水と石鹸で洗うこと。
P305+P351+P338 眼に入った場合:水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

(R,S)-AM1241 価格 もっと(2)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
Sigma-Aldrich Japan A6478 ≥98% (HPLC), solid
(R,S)-AM1241 ≥98% (HPLC), solid
444912-48-5 5mg ¥57500 2018-12-25 購入
Sigma-Aldrich Japan A6478 ≥98% (HPLC), solid
(R,S)-AM1241 ≥98% (HPLC), solid
444912-48-5 25mg ¥195900 2018-12-25 購入

(R,S)-AM1241 化学特性,用途語,生産方法

説明

AM1241 is a cannabinoid (CB) receptor agonist that is selective for CB2 over CB1 with Ki values of 7.1 and 580 nM for human recombinant receptors transfected into HEK and CHO cells, respectively, in a radioligand binding assay. It is considered a protean agonist as it has neutral antagonist and partial agonist activity, depending on the assay utilized. It is also acts in a species-dependent manner in vitro, acting as an agonist at human CB2 receptors (EC50 = 190 nM) but an inverse agonist at rat and mouse CB2 receptors (EC50s = 216 and 463 nM, respectively). AM1241 produces antinociception to thermal stimuli in rat hindpaw. The antinociceptive actions of AM1241 were blocked by the CB2 receptor-selective antagonist AM630 but not by the CB1 receptor-selective antagonist AM251 . AM1241 is neuroprotective, preventing HIV-1 glycoprotein Gp120-induced apoptosis in primary human and murine neural progenitor cells and increasing cell survival and differentiation. It increases hippocampal neurogenesis and decreases astro- and gliogenesis in GFAP/Gp120 transgenic mice when administered at a dose of 10 mg/kg daily for ten days. AM1241 also delays motor impairment in a murine model of amytrophic lateral sclerosis (ALS).

使用

(2-Iodo-5-nitrophenyl)[1-[(1-methyl-2-piperidinyl)methyl]-1H-indol-3-yl]methanone is a compound from the aminkalkylindole family which exerts potent and selective agonist activity for the cannabinoid receptor CB2.

Biochem/physiol Actions

AM1241 acts as an antinociceptive agent in several animal pain models. It has a potential to delay disease progression in amyotrophic lateral sclerosis (ALS) mouse model. Intrathecal, intravenous or intraperitoneal administration of AM1241 reduces hyperalgesia and allodynia in neuropathic rats.

(R,S)-AM1241 上流と下流の製品情報

原材料

準備製品


(R,S)-AM1241 生産企業

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444912-48-5()キーワード:


  • 444912-48-5
  • (R,S)-AM1241
  • (R,S)-3-(2-Iodo-5-nitrobenzoyl)-1-(1-methyl-2-piperidinylmethyl)-1H-indole
  • (3-iodo-5-nitrophenyl)-[1-[(1-methylpiperidin-2-yl)methyl]indol-3-yl]methanone
  • (2-Iodo-5-nitrophenyl)(1-((1-methylpiperidin-2-yl)methyl)-1H-Indol-3-yl)methanone
  • (2-iodo-5-nitrophenyl)-[1-[(1-methylpiperidin-2-yl)methyl]indol-3-yl]methanone
  • (2-Iodo-5-nitrophenyl)[1-[(1-methyl-2-piperidinyl)methyl]-1H-indol-3-yl]methanone
  • AM1241 (AM-1241
  • (R,S)-AM1241 USP/EP/BP
  • Methanone, (2-iodo-5-nitrophenyl)[1-[(1-methyl-2-piperidinyl)methyl]-1H-indol-3-yl]-
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