Chembridge-5861528 (TCS 5861528) 是一种有效的TRPA1通道拮抗剂,可拮抗异硫氰酸烯丙基和 4-HNE 诱发的 TRPA1 反应,IC50值分别为 14.3 μM 和 18.7 μM。Chembridge-5861528 具有抗过敏效果。
生物活性 | Chembridge-5861528 (TCS 5861528) is a potentTRPA1channel antagonist that antagonizes similarly allyl isothiocyanate- and 4-HNE-evoked TRPA1 responses, withIC50values of 14.3 μM and 18.7 μM, respectively. Chembridge-5861528 shows antihypersensitivity activities[1]. |
IC50& Target | TRPA1 14.3 μM (IC50, allyl isothiocyanate-evoked TRPA1 response) | TRPA1 18.7 μM (IC50, 4-HNE-evoked TRPA1 response) |
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体外研究 (In Vitro) | Chembridge-5861528 (TCS 5861528) shows no TRPA1 or TRPV1 channel agonism and no TRPV1 channel antagonism up to a dose of 100 μM[1].
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体内研究 (In Vivo) | Chembridge-5861528 (TCS 5861528) (30 mg/kg; i.p.; twice daily for a week) significantly attenuates development of mechanical hypersensitivity inStreptozocin(HY-13753)-induced diabetes mellitus rat model[1]. Chembridge-5861528 (3 and 10 μg/rat; i.t.; once) attenuatesCapsaicin(HY-10448)-induced blood flow increase in a dose-related fashion[2].
Animal Model: | Male Hannover-Wistar rats, Streptozocin-induced diabetes mellitus model[1] | Dosage: | 30 mg/kg | Administration: | Intraperitoneal injection, twice daily for a week | Result: | Significantly attenuated development of mechanical hypersensitivity as revealed by the paw pressure test (F1,80= 31.4, P< 0.0001). |
Animal Model: | Male Hannover–Wistar rats (220-260 g), Capsaicin-induced neurogenic inflammation model[2] | Dosage: | 0, 3, and 10 μg/rat | Administration: | Intrathecal injection, 20 min before Capsaicin injection | Result: | Significantly decreased the blood flow at 10 μg. |
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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 | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 120 mg/mL(324.83 mM;Need ultrasonic) 配制储备液 1 mM | 2.7069 mL | 13.5347 mL | 27.0695 mL | 5 mM | 0.5414 mL | 2.7069 mL | 5.4139 mL | 10 mM | 0.2707 mL | 1.3535 mL | 2.7069 mL |
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此方案可获得 ≥ 3 mg/mL (8.12 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 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。
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