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6-アミノ-N-メチル-5-(2,3,5-トリクロロフェニル)ピコリンアミド

6-アミノ-N-メチル-5-(2,3,5-トリクロロフェニル)ピコリンアミド 化学構造式
875051-72-2
CAS番号.
875051-72-2
化学名:
6-アミノ-N-メチル-5-(2,3,5-トリクロロフェニル)ピコリンアミド
别名:
6-アミノ-N-メチル-5-(2,3,5-トリクロロフェニル)ピコリンアミド
英語名:
PF-01247324
英語别名:
133786;CS-2577;PF-1247324;PF-01247324;PF01247324;PF 01247324;6-amino-N-methyl-5-(2,3,5-trichlorophenyl)picolinamide;6-AMINO-N-METHYL-5-(2,3,5-TRICHLOROPHENYL)PYRIDINE-2-CARBOXAMIDE;2-PyridinecarboxaMide, 6-aMino-N-Methyl-5-(2,3,5-trichlorophenyl)-;6-AMINO-5-(2,3,5-TRICHLORO-PHENYL)-PYRIDINE-2-CARBOXYLIC ACID METHYLAMIDE;Sodium Channel,PF 01247324,PF-01247324,Na+ channels,Na channels,PF01247324,Inhibitor,inhibit
CBNumber:
CB42682530
化学式:
C13H10Cl3N3O
分子量:
330.6
MOL File:
875051-72-2.mol
MSDS File:
SDS

6-アミノ-N-メチル-5-(2,3,5-トリクロロフェニル)ピコリンアミド 物理性質

沸点 :
477.7±45.0 °C(Predicted)
比重(密度) :
1.460±0.06 g/cm3(Predicted)
貯蔵温度 :
room temp
溶解性:
DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS (pH 7.2) (1:4): 0.2 mg/ml
酸解離定数(Pka):
6.56±0.46(Predicted)
外見 :
粉
色:
白からベージュ
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)
RIDADR  UN 2811 6.1 / PGIII
絵表示（GHS） GHS 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
H301 飲み込むと有毒 急性毒性、経口 3 危険 GHS hazard pictograms P264, P270, P301+P310, P321, P330,P405, P501
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
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。

6-アミノ-N-メチル-5-(2,3,5-トリクロロフェニル)ピコリンアミド 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 PZ0274 ≥98% (HPLC)
PF-01247324 ≥98% (HPLC)		 875051-72-2 5mg ￥23900 2024-03-01 購入
Sigma-Aldrich Japan PZ0274 ≥98% (HPLC)
PF-01247324 ≥98% (HPLC)		 875051-72-2 25mg ￥76400 2024-03-01 購入

6-アミノ-N-メチル-5-(2,3,5-トリクロロフェニル)ピコリンアミド 化学特性,用途語,生産方法

説明

PF-01247324 is a blocker of the tetrodotoxin-resistant (TTX-R) sodium channel Nav1.8 (IC50 = 0.19 μM for human Nav1.8). It is selective for Nav1.8 over Nav1.1, Nav1.2, Nav1.5, and Nav1.7 channels (IC50s = 13, 12.8, 9, and 19 μM, respectively) as well as ether-a-go-go (ERG) potassium channels (IC50 = 30 μM). PF-01247324 blocks Nav1.8 channels in a VSP-FRET assay using HEK293 cells (IC50 = 2.6 μM). In vivo, PF-01247324 (100 mg/kg) reduces phase 2 flinching in a rat model of formalin-induced persistent pain. It increases latency to lift the inflamed paw and latency to paw withdrawal in rat models of carrageenan-induced thermal hyperalgesia and mechanical hyperalgesia induced by complete Freund''s adjuvant (CFA), respectively.

Biochem/physiol Actions

In humans, PF-01247324 [6-amino-5-(2, 3, 5-trichloro-phenyl)-pyridine-2-carboxylic acid methylamide] prevents native tetrodotoxin-resistant (TTX-R) currents in dorsal root ganglion (DRG) neurons.

酵素阻害剤

This novel oral NaV1.8 blocker (FW = 330.59 g/mol) attenuates nociception and neuronal excitability by selectively targeting voltage-gated sodium transporter NaV1.8, with much weaker action against NaV1.1, NaV1.2, NaV1.4, NaV1.5, NaV1.6, and NaV1.7 transporters. PF-01247324 inhibited native tetrodotoxin-resistant (TTX-R) currents in human dorsal root ganglion (DRG) neurons (IC50 = 331 nM) and in recombinantly expressed hNav 1.8 (IC50 = 196 nM), with 50-fold selectivity over recombinantly expressed TTX-R hNav 1.5 channels (IC50 ～ 10 μM) and 65-100 greater selectivity over TTX-sensitive (TTX-S) channels (IC50 ～ 10-18 μM). Native TTX-R currents in small diameter rodent DRG neurons were inhibited with an IC50 of 448 nM, and the block of both human recombinant Nav1.8 and TTX-R from rat DRG neurons was both frequency and statedependent. Unlike previously published NaV1.8 blockers, PF-01247324 demonstrates frequency-dependence, and off-target frequency-dependence at other sodium channel subtypes may reduce its selectivity window. The majority of small molecule sodium channel blockers interact at the local anesthetic binding site, which due to a high level of sequence homology across voltage-gated sodium channel subtypes seems an unlikely site for interaction of selective agents such as PF-01247324. The majority of small molecule sodium channel blockers interact at the local anesthetic binding site, which due to a high level of sequence homology across voltage-gated sodium channel subtypes seems an unlikely site for interaction of selective agents such as PF-01247324

6-アミノ-N-メチル-5-(2,3,5-トリクロロフェニル)ピコリンアミド 上流と下流の製品情報

原材料

準備製品

6-アミノ-N-メチル-5-(2,3,5-トリクロロフェニル)ピコリンアミド 生産企業

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875051-72-2(6-アミノ-N-メチル-5-(2,3,5-トリクロロフェニル)ピコリンアミド)キーワード:

ホルムアニリド ブレポシチニブ 2-チオキソ-4-オキソ-6-(2-メトキシ-5-クロロフェニル)-1,2,3,4-テトラヒドロピリミジン-1-アセトアミド ステゾリド 1-イソプロピル-1′-(2-メチル-1H-ベンゾイミダゾール-6-イルカルボニル)スピロ[1H-インダゾール-5(4H),4′-ピペリジン]-7(6H)-オン 2-メチル-3-クロロ-5-(トリフルオロメチル)-7-[(S)-2-(ヒドロキシメチル)モルホリノ]-1H-ピロロ[3,2-b]ピリジン-6-カルボニトリル
  • 875051-72-2
  • 2-PyridinecarboxaMide, 6-aMino-N-Methyl-5-(2,3,5-trichlorophenyl)-
  • 6-amino-N-methyl-5-(2,3,5-trichlorophenyl)picolinamide
  • 6-AMINO-5-(2,3,5-TRICHLORO-PHENYL)-PYRIDINE-2-CARBOXYLIC ACID METHYLAMIDE
  • PF-1247324
  • PF-01247324
  • 6-AMINO-N-METHYL-5-(2,3,5-TRICHLOROPHENYL)PYRIDINE-2-CARBOXAMIDE
  • PF01247324;PF 01247324
  • 133786
  • CS-2577
  • Sodium Channel,PF 01247324,PF-01247324,Na+ channels,Na channels,PF01247324,Inhibitor,inhibit
  • 6-アミノ-N-メチル-5-(2,3,5-トリクロロフェニル)ピコリンアミド
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