2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. AG1529

AG1529 是一种 TRPV1 抑制剂，同时也是基于辣椒素类的软剂，对人源 TRPV1 的 IC50 为 0.9-0.93 μM。AG1529 可可逆性阻断辣椒素诱导的 TRPV1 激活，结合于 TRPV1 的辣椒素结合位点，对 pH 诱导的 TRPV1 门控有中度影响，且不会改变电压或热介导的 TRPV1 反应。AG1529 可抑制 TRPV1 介导的神经元兴奋性，减少辣椒素和 pH 诱导的神经元放电，消除组胺能及炎症介导的 TRPV1 敏化作用。AG1529 具有抗伤害感受和止痒作用，可减轻体内痛觉过敏和瘙痒症状，呈剂量依赖性降低啮齿类动物的急性组胺能瘙痒，还可轻度阻断 hTRPA1 和 hTRPM8 通道活性。AG1529 可发生水解和皮肤失活，最大限度减少 TRPV1 相关的不良反应，不会引发类似辣椒素的灼烧感，也不会干扰生理性体温调节。AG1529 可用于炎症性皮肤伤害感受及急性组胺能瘙痒的相关研究。

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AG1529

AG1529 Chemical Structure

CAS No. : 2225980-49-2

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AG1529 相关抗体

Top Publications Citing Use of Products

查看 TRP Channel 亚型特异性产品:

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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

AG1529 is a TRPV1 inhibitor and capsaicinoid-based soft agent with a human TRPV1 IC50 of 0.9-0.93 μM. AG1529 reversibly blocks capsaicin-evoked TRPV1 activation, binds to the TRPV1 capsaicin binding site, moderately affects pH-induced TRPV1 gating, and does not alter voltage- or heat-mediated TRPV1 responses. AG1529 suppresses TRPV1-mediated neuronal excitability, reduces capsaicin- and pH-evoked neuronal firing, abolishes histaminergic and inflammation-mediated TRPV1 sensitization. AG1529 exhibits anti-nociceptive and antipruritic effects, attenuates in vivo hyperalgesia and pruritus, dose-dependently reduces acute histaminergic itch in rodents, and mildly blocks hTRPA1 and hTRPM8 channel activity. AG1529 undergoes hydrolysis and dermal deactivation, minimizes TRPV1-associated side reactions, does not evoke capsaicin-like burning sensation, and does not disrupt physiological thermal regulation. AG1529 can be used for the research of inflammatory cutaneous nociception and acute histaminergic pruritus[1][2].

IC50 & Target[1]

TRPV1

0.93 μM (IC50)

体外研究
(In Vitro)

AG1529 (1-100 μM) 在稳定表达 TRPV1 的 SH-SY5Y 细胞中可强效拮抗 TRPV1，其 IC50 为 0.93 μM[1]。
AG1529 在 HaCaT 匀浆中稳定性极高 (25 μM; 240 min)，在人血浆中稳定性中等 (100 μM; 20 min)，而在受试条件下，其在人肝 S9 组分中会完全水解 (50 μM; 60 min)[1]。
AG1529 (50 μM; 120 min) 在原代成人表皮角质形成细胞和真皮成纤维细胞匀浆中发生显著水解，120 min 后分别仅剩余 22.6%和 13.3%的底物[1]。
AG1529 (0.2 mg/mL) 可被 hCE1 和 hCE2 水解，hCE2 对其代谢具有偏好性，这一点可通过该同工酶对应的更高内在清除率和更短半衰期得到证实[1]。
AG1529 (1 μM) 可在 HEK293 细胞中以可逆且竞争性的方式阻断辣椒素激活的 hTRPV1，其 IC50 为 0.9 μM[2]。
AG1529 (1-10 μM; 30 s) 在 10 μM 浓度下可中度阻断 HEK293 细胞中 pH 诱导的 hTRPV1 激活，但在测试浓度下对电压或热介导的 hTRPV1 门控无显著影响[2]。
AG1529 (10 μM; 30 s) 可在 HEK293 细胞中以 10 μM 浓度中度抑制薄荷醇激活的 hTRPM8 和 AITC 激活的 hTRPA1，其效力显著低于对 hTRPV1 的抑制作用[2]。
AG1529 以与辣椒素相似的构象结合 TRPV1 的辣椒素结合位点，这支持其作为竞争性 TRPV1 拮抗剂的作用机制，而 TRPA1 中的空间位阻会降低其对该通道的结合亲和力[2]。

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

AG1529 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUClast AUCinf
Mice[2] 5 mg/kg i.v. 3.6 min 5.0 min 738.1 ng/mL 14709.3 min·ng/mL 14728.5 min·ng/mL
体内研究
(In Vivo)

AG1529 (10-100 μg；足底注射；单次给药) 可短暂、呈剂量依赖性地逆转 CFA 诱导的热痛觉过敏，且不影响对侧热伤害感受[1]。
AG1529 (1-10 mg/kg；静脉注射；单次给药) 可短暂、呈剂量依赖性地逆转 CFA 诱导的热痛觉过敏，且不影响对侧热伤害感受[1]。
AG1529 (100 μg；皮内注射；单次给药；组胺注射前 30 分钟) 可显著减轻小鼠的组胺能瘙痒，组胺注射后 10-20 分钟可观察到峰值效应[1]。
AG1529 (100 μg；皮内注射；单次给药；氯喹给药前 30 分钟) 可显著减轻小鼠的非组胺依赖性瘙痒，在氯喹注射后 5-15 分钟观察到峰值效应[1]。
AG1529 (10 mg/kg；静脉注射；单次给药) 不影响小鼠的体温，可避免其他 TRPV1 拮抗剂相关的体温过高副作用[1]。
AG1529 (0.1-1% w/v; 局部擦拭；单次给药) 可剂量依赖性地减轻组胺诱导的大鼠瘙痒，其中 1% AG1529 对搔抓行为的抑制作用最强[2]。
AG1529 (0.1-1% w/w；局部给药；每日 2 次；连续 3 天) 可显著减轻组胺诱导的大鼠瘙痒症状，其中 1% AG1529 可完全消除搔抓行为[2]。

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

Animal Model: unspecified[1]
Dosage: 10 μg; 30 μg; 100 μg
Administration: i.pl.; single dose
Result: Ablated CFA-induced thermal hyperalgesia in the ipsilateral paw in a dose-dependent and transient manner.
Showed anti-hyperalgesic activity at 30 minutes, peaked at 60 minutes, and lasted for 90 minutes at the 100 μg dose.
Did not affect thermal nociception in the contralateral paw.
Animal Model: unspecified[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.v.; single dose
Result: Attenuated CFA-induced thermal hyperalgesia in the ipsilateral paw in a dose-dependent and transient manner.
Showed anti-hyperalgesic effects at 30 minutes, lasting 60 minutes at the 1 mg/kg dose.
Showed effects at 60 minutes, lasting 90 minutes at the 3 mg/kg dose.
Showed significant effects only at 60 minutes at the 10 mg/kg dose.
Did not affect thermal nociception in the contralateral paw.
Animal Model: unspecified[1]
Dosage: 100 μg
Administration: i.pl.; single dose; 30 minutes prior to histamine
Result: Attenuated histamine-induced paw licking time, with statistically significant reductions in the 10-15 minute and 15-20 minute intervals after histamine instillation.
Animal Model: unspecified[1]
Dosage: 100 μg
Administration: i.pl.; single dose; 30 minutes prior to chloroquine
Result: Reduced chloroquine-induced paw licking time, with statistically significant reductions in the 5-10 minute and 10-15 minute intervals after chloroquine instillation.
Animal Model: unspecified[1]
Dosage: 10 mg/kg
Administration: i.v.; single dose
Result: Did not alter mouse body temperature over the 120-minute observation period, unlike the positive control TRPV1 antagonist BCTC which induced significant hyperthermia.
Animal Model: Wistar (adult, 100-125 g, pruritus model via subcutaneous histamine injection)[2]
Dosage: 0.1% w/v; 1% w/v
Administration: topical wipe; single application
Result: Significantly reduced histamine-induced licking time across all 10-minute intervals from 0-60 minutes post-histamine injection.
Produced a dose-dependent reduction in total scratching counts over 60 minutes: 0.1% AG1529 reduced scratching compared to vehicle (p = 0.0003), and 1% AG1529 produced an even greater reduction (p < 0.0001 vs vehicle; p = 0.0395 vs 0.1% AG1529).
Animal Model: Wistar (adult, 100-125 g, pruritus model via subcutaneous histamine injection)[2]
Dosage: 0.1% w/w; 1% w/w
Administration: topical application; twice daily; 3 days
Result: Significantly reduced histamine-induced licking time across all 10-minute intervals from 0-60 minutes post-histamine injection, with the 1% dose nearly eliminating licking activity in most intervals.
Reduced total scratching counts over 60 minutes: 0.1% AG1529 reduced scratching compared to vehicle (p = 0.0122), and 1% AG1529 fully abrogated scratching behavior (p = 0.0003 vs vehicle).
分子量

519.41

Formula

C22H34INO5
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

AG1529 相关分类

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  • 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:

AG15292225980-49-2AG 1529AG-1529TRP ChannelTransient receptor potential channelshuman liver S9 fractiondermal fibroblastTRPV1hCE2human epidermal keratinocytecapsaicinSH-SY5Y cellshCE1human plasmaHaCaTInhibitorinhibitorinhibit

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