2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. TRPA1 agonist-3

TRPA1 agonist-3 是一种具有选择性和口服活性的 TRPA1 激动剂，在 HEK-293T 细胞中对人源和小鼠 TRPA1 的 EC50 分别为 50.05 μM 和 314.04 μM。TRPA1 agonist-3 未能激活 hTRPV1 、 mTRPV2、hTRPV3、hTRPV4、hTRPC6 和 hTRPM8 通道。TRPA1 agonist-3 可通过通道脱敏机制缓解小鼠的炎性疼痛。

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TRPA1 agonist-3

TRPA1 agonist-3 Chemical Structure

CAS No. : 3083086-77-2

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TRPA1 agonist-3 相关抗体

Top Publications Citing Use of Products

查看 TRP Channel 亚型特异性产品:

查看所有亚型
TRPA1 TRPC3 TRPC4 TRPC5 TRPM8 TRPM2 TRPM3 TRPM4 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TRPA1 agonist-3 is a selective and orally active TRPA1 agonist, with EC50 values of 50.05 μM and 314.04 μM for human and mouse TRPA1, respectively. TRPA1 agonist-3 does not activate hTRPV1, mTRPV2, hTRPV3, hTRPV4, hTRPC6, or hTRPM8 channels. TRPA1 agonist-3 alleviates inflammatory pain in mice through a channel desensitization mechanism[1].

IC50 & Target[1]

TRPA1

50.50 μM (EC50, human)

TRPA1

314.04 μM (EC50, mouse)

体外研究
(In Vitro)

TRPA1 agonist-3 (compound NMTA) (50 μM, 24 h) 在 HEK-293T 细胞中以浓度依赖的方式激活 hTRPA1 通道，从而导致钙离子内流[1]。
TRPA1 agonist-3 通过 TRPA1 脱敏机制发挥镇痛作用[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

TRPA1 agonist-3 相关抗体:
体内研究
(In Vivo)

TRPA1 agonist-3 (compound NMTA) (10-40 mg/kg，口服给药，一次) 可缓解雄性 C57BL/6J 小鼠的由足底注射 (p.i.) CFA (20 μL) (Complete Freund’s Adjuvant) (HY-153808B) 诱导的炎症性疼痛[1]。
TRPA1 agonist-3 (10-40 mg/kg，口服给药，一次) 对在雄性 C57BL/6J 小鼠中 TRPA1 具有选择性脱敏作用，而非直接抑制热敏感通道[1]。
TRPA1 agonist-3 (10-40 mg/kg，口服给药，一次) 对雄性 C57BL/6J 小鼠冷诱导疼痛具有抗伤害性作用[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CFA (p.i. 20 μL)-induced male C57BL/6J mice (6-8 weeks old, 18 g-20 g)[1].
Dosage: 10, 20, 40 mg/kg
Administration: p.o. at a volume of 200 μL per 20 g body weight, once
Result: Reduced the paw withdrawal mechanical threshold and paw withdrawal thermal threshold in the CFA model group.
Prolonged the thermal withdrawal latency with peak effect at 0.5 h and lasted for 1 h.
Animal Model: Female C57BL/6J mice (6-8 weeks old, 18 g-20 g)[1]
Dosage: 10, 20, 40 mg/kg
Administration: p.o., once
Result: Prolonged the thermal withdrawal latency.
Reached peak effect at 0.5 h and lasted for 1 h.
Produced weak antinociceptive effects in 40 mg/kg with peak effect evidenced by prolonged withdrawal latency (23.15 ± 1.30 s) at 0.5 h postdosing.
Lasted for 1 h but completely lost at 2 and 4 h.
Animal Model: Male C57BL/6J mice (6-8 weeks old, 18 g-20 g)[1]
Dosage: 10, 20, 40 mg/kg
Administration: p.o., once
Result: Prolonged the thermal withdrawal latency. All treatment groups reached peak effect at 0.5 h and lasted for 1 h in cold plate test.
Increased the tail-flick latency and reached a peak at 17.70 s at 1 h (40 mg/kg) in Cold Tail-Flick Test.
分子量

262.37

Formula

C14H18N2OS
CAS 号
性状

固体

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
纯度 & 产品资料
参考文献

TRPA1 agonist-3 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TRPA1 agonist-33083086-77-2TRP ChannelTransient receptor potential channelsInflammatory painNMTATRPA1analgesicantinociceptionInhibitorinhibitorinhibit

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