(2R/S)-6-PNG (6-Prenylnaringenin) 是一种有效且可逆的Cav3.2T 型 Ca2+通道 (T 通道)阻滞剂。(2R/S)-6-PNG 可以透过血脑屏障 (BBB)。(2R/S)-6-PNG 抑制小鼠的神经性和内脏疼痛。
生物活性 | (2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversibleCav3.2 T-type Ca2+channels (T-channels)blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice[1]. |
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体外研究 (In Vitro) | (2R/S)-6-PNG (6-Prenylnaringenin) potently blocks Cav3.2, but exhibits minor effect on high-voltage-activated Ca2+channels and voltage-gated Na+channels in differentiated NG108-15 cells[1]. On the basis of IC50 values, the proportion (Cav3.2/HVA) of the inhibition potency of (2R/S)-6-PNG on Cav3.2 and HVA-currents is 5.20, and that (Cav3.2/Nav) on Cav3.2 and Nav-currents is 3.54[1].
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体内研究 (In Vivo) | (2R/S)-6-PNG (6-Prenylnaringenin; 10-30 mg/kg; i.p.; single dose; 15 min before Na2S) significantly reduced the Na2S-induced nociceptive behavior and/or referred hyperalgesia in onscious mice with intracolonic (i.col.) administration of Na2S, an H2S donor[1]. (2R/S)-6-PNG (30 mg/kg; i.p.) prevents the increased number of phosphorylated ERK-positive cells following i.col. Na2S in laminae I-II, V-VI and X to which the primary afferent neurons project, and the Na2S-induced increase in the phosphorylated ERK-positive cell number[1]. (2R/S)-6-PNG (0.01-1 and 0.1-10 nmol/paw; intraplantar administration) restores the mechanical allodynia induced by partial sciatic nerve ligation (PSNL) and by i.p. administration of Oxaliplatin (OHP) a, respectively, in a dose-dependent manner[1]. (2R/S)-6-PNG (20-30 mg/kg; i.p.) significantly reverses the PSNL-induced allodynia. (2R/S)-6-PNG (10-20 mg/kg; i.p.) significantly reverses the OHP-induced allodynia (5 mg/kg; i.p.; single dose)[1].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 125 mg/mL(367.25 mM;Need ultrasonic) 配制储备液 1 mM | 2.9380 mL | 14.6899 mL | 29.3798 mL | 5 mM | 0.5876 mL | 2.9380 mL | 5.8760 mL | 10 mM | 0.2938 mL | 1.4690 mL | 2.9380 mL |
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此方案可获得 ≥ 2.08 mg/mL (6.11 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (6.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.11 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (6.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.11 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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