2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel Calcium Channel
  4. A-425619

A-425619  (Synonyms: 化合物A 425619)

目录号: HY-110292 纯度: 99.96%
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A-425619 是一种具有口服活性和选择性的瞬时受体电位 V1 型 (TRPV1) 拮抗剂。A-425619 阻断 Capsaicin (HY-10448) 和 N-花生四烯酰多巴胺 (NADA) 诱导的背根神经节和三叉神经节中的 Ca2+ 流入。A-425619 缓解大鼠中与炎症和组织损伤相关的病理性疼痛。A-425619 可用于研究与炎症和组织损伤相关的疼痛。

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A-425619

A-425619 Chemical Structure

CAS No. : 581809-67-8

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A-425619 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

A-425619 is an orally active and selective transient receptor potential type V1 (TRPV1) antagonist. A-425619 blocks Capsaicin (HY-10448)- and N-arachidonoyl-dopamine (NADA)-induced Ca2+ influx in dorsal root ganglia and trigeminal ganglia. A-425619 relieves pathophysiological pain associated with inflammation and tissue injury in rats. A-425619 can be used for the study of pain related to inflammation and tissue injury[1][2][3].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
2 nM
Compound: 7
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay
[PMID: 17489570]
HEK293 IC50
5 nM
Compound: 7
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
[PMID: 17489570]
HEK293 IC50
9 nM
Compound: 7
Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
[PMID: 17489570]
体外研究
(In Vitro)

A-425619 (10 μM) 阻断 500 nM Capsaicin (HY-10448) 诱导的背根神经节 (IC50 = 78 nM) 和三叉神经节 (IC50 = 115 nM) 中的 Ca2+ 流入，并抑制 3 μM N-花生四烯酰多巴胺 (NADA) 诱导的背根神经节 (IC50 = 36 nM) 和三叉神经节 (IC50 = 37 nM) 中的 Ca2+ 流入[1]。
A-425619 (100 nM) 可完全抑制背根神经节和三叉神经节神经元中 TRPV1 介导的酸激活电流[1]。
A-425619 (0.01-1 μM) 可显著阻断 300 nM Capsaicin 和 3 μM NADA 诱导的背根神经节中降钙素基因相关肽 (CGRP) 释放[1]。
A-425619 (3-100 nM) 强效阻断大鼠背根神经节神经元中天然 TRPV1 通道的激活 (IC50 = 9 nM)[2]。

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

A-425619 相关抗体:
体内研究
(In Vivo)

A-425619 (10.3-103 μg/只 (30-300 nmol/只)，足底注射，Capsaicin 前 15 分钟，单次剂量或 10.3-35 mg/kg (30-100 μmol/kg)，口服，Capsaicin 前 60 分钟，单次剂量) 以剂量依赖方式阻断大鼠中 Capsaicin 诱导的机械性痛觉过敏[3]。
A-425619 (3.5-35 mg/kg (10-100 μmol/kg)，腹腔注射，测试前 30 分钟，单次剂量或 3.5-103 mg/kg (10-300 μmol/kg)，口服，测试前 60 分钟，单次剂量) 以剂量依赖方式缓解大鼠中 CFA 诱导的慢性炎症性热痛觉过敏[3]。
A-425619 (103 μg/只 (300 nmol/只)，足底注射至炎症足，测试前 30 分钟，单次剂量) 减轻大鼠中 CFA 诱导的热痛觉过敏[3]。
A-425619 (3.5-35 mg/kg (10-100 μmol/kg)，腹腔注射，Carrageenan (HY-125474) 后 90 分钟，单次剂量) 以剂量依赖方式缓解大鼠中 Carrageenan 诱导的急性炎症性热痛觉过敏[3]。
A-425619 (35 mg/kg (100 μmol/kg)，口服，每日两次，持续 5 天) 在大鼠中保持缓解皮肤切口诱导的机械性痛觉异常的效能[3]。
A-425619 (35-103 mg/kg (100-300 μmol/kg)，腹腔注射，测试前 30 分钟，单次) 减轻大鼠中 MIA 诱导的骨关节炎疼痛[3]。
A-425619 (35 mg/kg (100 μmol/kg)，腹腔注射，测试前 30 分钟，单次剂量) 减轻大鼠 L5/L6 脊神经结扎模型和坐骨神经结扎模型中神经病理性疼痛的机械性痛觉异常[3]。

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

Animal Model: Capsaicin-induced mechanical hyperalgesia model in rats: 2 μg/10 μL of capsaicin solution was subcutaneously injected into the plantar aspect of the right hind paw of rats[3]
Dosage: 10.3-103 μg/rats (30-300 nmol/rats)
Administration: intraplantar 15 min before Capsaicin for a single dose
Result: Showed dose-dependent blocking effects on capsaicin-induced mechanical hyperalgesia.
Showed no effect on the paw withdrawal threshold of the capsaicin-injected paw when 300 nmol/rat was injected into the contralateral paw.
Animal Model: Capsaicin-induced mechanical hyperalgesia model in rats: 2 μg/10 μL of capsaicin solution was subcutaneously injected into the plantar aspect of the right hind paw of rats[3]
Dosage: 10.3-35 mg/kg (30-100 μmol/kg)
Administration: p.o. 60 min before Capsaicin for a single dose
Result: Showed dose-dependent preventive effects on capsaicin-induced mechanical hyperalgesia.
Achieved full efficacy at 35 mg/kg (100 μmol/kg), with an ED50 of 45 μmol/kg.
Significantly increased the paw withdrawal threshold compared with vehicle-treated rats that received Capsaicin.
Animal Model: Complete Freund’s adjuvant (CFA)-induced chronic inflammatory pain model in rats: 150 μL of 50% CFA solution was injected into the plantar surface of the right hind paw of rats[3]
Dosage: 3.5-35 mg/kg (10-100 μmol/kg) or 3.5-103 mg/kg (10-300 μmol/kg)
Administration: i.p. 30 min before testing for a single dose or p.o. 60 min before testing for a single dose
Result: Relieved CFA-induced thermal hyperalgesia, with an ED50 of 51 μmol/kg administered intraperitoneally.
Relieved CFA-induced thermal hyperalgesia, with an ED50 of 40 μmol/kg administered orally.
Animal Model: Complete Freund’s adjuvant (CFA)-induced chronic inflammatory pain model in rats: 150 μL of 50% CFA solution was injected into the plantar surface of the right hind paw of rats[3]
Dosage: 103 mg/rats (300 nmol/rats)
Administration: intraplantar into inflamed paw 30 min before testing for a single dose
Result: Produced a 56.2% reduction in CFA-induced thermal hyperalgesia.
Animal Model: Carrageenan-induced acute inflammatory pain model in rats: 100 μL of 1% λ-carrageenan solution was injected into the plantar surface of the right hind paw of rats[3]
Dosage: 3.5-35 mg/kg (10-100 μmol/kg)
Administration: i.p. 90 min after Carrageenan (HY-125474) for a single dose
Result: Relieved carrageenan-induced thermal hyperalgesia, with an ED50 of 50 μmol/kg.
Animal Model: Skin incision postoperative pain model in rats: a 1-cm longitudinal incision was made on the plantar surface (starting 0.5 cm from the proximal edge of the heel and extending toward the toes), the plantaris muscle was elevated and incised longitudinally (with origin and insertion intact), the skin was closed with two 5-0 nylon sutures[3]
Dosage: 35 mg/kg (100 μmol/kg)
Administration: p.o. twice daily for 5 days
Result: Produced a 42.6% reduction in mechanical allodynia when tested at 24 hours after surgery (day 2), and still exerted a 37.6% analgesic effect on day 5 after surgery.
Animal Model: Monoiodoacetate (MIA)-induced osteoarthritic pain model in rats: under light halothane anesthesia, a single intra-articular injection of 3 mg MIA (dissolved in 0.05 ml sterile isotonic saline) was administered into the knee joint cavity of rats[3]
Dosage: 35-103 mg/kg (100-300 μmol/kg)
Administration: i.p. 30 min before testing for a single dose
Result: Reduced MIA-induced increase in weight-bearing difference between the injured and non-injured hind limbs.
Animal Model: Spinal nerve (L5/L6) ligation neuropathic pain model in rats: a 1.5-cm incision was made dorsal to the lumbosacral plexus, the left L5 and L6 spinal nerves were isolated and tightly ligated with 3-0 silk threads[3]
Dosage: 35 mg/kg (100 μmol/kg)
Administration: i.p. 30 min before testing for a single dose
Result: Reduced mechanical allodynia induced by spinal nerve injury.
分子量

345.32

Formula

C18H14F3N3O
CAS 号
性状

固体

颜色

White to off-white

中文名称

化合物A 425619
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
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (289.59 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8959 mL 14.4793 mL 28.9586 mL
5 mM 0.5792 mL 2.8959 mL 5.7917 mL
查看完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

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动物数量

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由于实验过程有损耗，建议您多配一只动物的量
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工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

A-425619 相关分类

完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8959 mL 14.4793 mL 28.9586 mL 72.3966 mL
5 mM 0.5792 mL 2.8959 mL 5.7917 mL 14.4793 mL
10 mM 0.2896 mL 1.4479 mL 2.8959 mL 7.2397 mL
15 mM 0.1931 mL 0.9653 mL 1.9306 mL 4.8264 mL
20 mM 0.1448 mL 0.7240 mL 1.4479 mL 3.6198 mL
25 mM 0.1158 mL 0.5792 mL 1.1583 mL 2.8959 mL
30 mM 0.0965 mL 0.4826 mL 0.9653 mL 2.4132 mL
40 mM 0.0724 mL 0.3620 mL 0.7240 mL 1.8099 mL
50 mM 0.0579 mL 0.2896 mL 0.5792 mL 1.4479 mL
60 mM 0.0483 mL 0.2413 mL 0.4826 mL 1.2066 mL
80 mM 0.0362 mL 0.1810 mL 0.3620 mL 0.9050 mL
100 mM 0.0290 mL 0.1448 mL 0.2896 mL 0.7240 mL
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:

A-425619581809-67-8化合物A 425619A425619A 425619TRP ChannelCalcium ChannelTransient receptor potential channelsCa2+ channelsCa channelsinflammationtissue injuryTRPV1Inhibitorinhibitorinhibit

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