Hydroxy-α-sanshool 是TRPA1和TRPV1激动剂,EC50分别为 69 和 1.1 μM,可用于疼痛的研究。
生物活性 | Hydroxy-α-sanshool is atransient receptor potential ankyrin 1(TRPA1) andTRP vanilloid 1(TRPV1) agonist withEC50s of 69 and 1.1 μM, respectively. Hydroxy-α-sanshool can be used for pain research[1][2]. |
IC50& Target | Human Endogenous Metabolite |
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体外研究 (In Vitro) | Hydroxy-α-sanshool (0-10 mM; 20 s) induces inward currents in cultured DRG neuron[2]. Hydroxy-α-sanshool (1 mM; 0-1 min) increases intracellular Ca2+in cultured DRG neuron[2].
Cell Viability Assay[2] Cell Line: | Dorsal root ganglion (DRG) neurons | Concentration: | 0-10 mM | Incubation Time: | 20 s | Result: | Induced small but robust inward currents for DRG neuron with an EC50of 66.2 μM. |
Cell Viability Assay[2] Cell Line: | Dorsal root ganglion (DRG) neurons | Concentration: | 1 mM | Incubation Time: | 0-1 min | Result: | Led to an intracellular Ca2+increase in the majority of DRG neurons tested (98 of 100). |
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体内研究 (In Vivo) | Hydroxy-α-sanshool (intradermal injection; 4 mg per mouse; once) shows paw-licking response in wild-type and TRPV1-deficient mice[2]. Hydroxy-α-sanshool (1 mM) is markedly aversive to WT mice, but in TRPV1 KO mice, the aversion is almost entirely eliminated (P<0.001)[1].
Animal Model: | Wild-type and TRPV1-deficient mice[2] | Dosage: | 4 mg per mouse | Administration: | Intradermal injection; 4 mg per mouse; once | Result: | Reduced paw-licking response in TRPV1-deficient mice (160 times, P< 0.05). Showed paw-licking response in wild-type mice (mean 284.8 times) in 20 min. |
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来源 | - Plants
- Rutaceae
- Zanthoxylum bungeanumMaxim.
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -20°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(379.68 mM;Need ultrasonic) 配制储备液 1 mM | 3.7968 mL | 18.9840 mL | 37.9680 mL | 5 mM | 0.7594 mL | 3.7968 mL | 7.5936 mL | 10 mM | 0.3797 mL | 1.8984 mL | 3.7968 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.5 mg/mL (9.49 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (9.49 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 25.0 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: 2.5 mg/mL (9.49 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (9.49 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 25.0 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 (7.90 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.90 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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