2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. TRPV1 antagonist 3

TRPV1 antagonist 3 

目录号: HY-144372 纯度: 99.30%
COA 产品使用指南

摩尔计算器

TRPV1 antagonist 3 (Compound 7q) 是一种有效的 TRPV1 拮抗剂，对 capsaicin 的 IC50 值为 2.66 nM。 TRPV1 antagonist 3 具有模式选择性和良好的口服生物利用度 (F = 60%)，可透过血脑屏障。

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TRPV1 antagonist 3 Chemical Structure

TRPV1 antagonist 3 Chemical Structure

CAS No. : 2765294-54-8

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1 mg ￥1454
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5 mg ￥3200
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10 mg ￥5200
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Customer Review

TRPV1 antagonist 3 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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TRPC TRPM TRPV TRPA TRPML

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant[1].

IC50 & Target

hTRPV1

2.66 nM (IC50)

TRPM8

7.45 μM (IC50)

体外研究
(In Vitro)

TRPV1 antagonist 3 (Compound 7q) is highly selective for the TRPV1 receptor relative to other TRP channels[1].
TRPV1 antagonist 3 shows acceptable aqueous solubility (solubility at pH 7.4 = 26 μg/mL) [1].

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

TRPV1 antagonist 3 相关抗体:
体内研究
(In Vivo)

TRPV1 antagonist 3 (Compound 7q) (0-30 mg/kg; i.p.; 30 min) shows anti-nociceptive effect mainly mediated by blocking CAP-activated channel[1].
TRPV1 antagonist 3 (0-100 mg/kg; i.g.) had no obvious thermal effect in rats[1].
TRPV1 antagonist 3 (10 mg/kg; i.v.) shows a good concentration in the brain at 0.5 h, with value of 2311 ng/g, and has good CNS penetration, with a brain/plasma ratio of 1.66[1].

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

Animal Model: KM male mice (18-22 g), capsaicin, acetic acid, and thermal induced pain model[1]
Dosage: 3, 10, and 30 mg/kg. 20 μL of solution of capsaicin (16 mg/20 mL) was injected s.c. under the skin of the dorsal surface of the right hind paw, or injected with 0.6% acetic acid (0.1 mL/10 g/mouse i.p.).
Administration: Intraperitoneally administration; 30 min
Result: In capsaicin-induced nociception, licking time decreased significantly in a dose-dependent manner. In acid-induced nociception, no significant anti-nociceptive activities were found compared with the control (SB-705498 and BCTC) at all dosage. In thermal-induced nociception, the latency time of nociceptive responses was increased at the doses of 10 and 30 mg/kg.
Animal Model: Spragur-Dawley male rats (220-250 g)[1]
Dosage: 10 mg/kg or 20 mg/kg
Administration: Intravenous injection of 10 mg/kg or oral dose of 20 mg/kg (Pharmacokinetic Analysis)
Result: In vivo pharmacokinetic parameters of TRPV1 antagonist 3 in rats (n=3)[1]
Parameters IV PO
t1/2 (h) 0.106 ± 0.076
t1/2, ka (h) 0.462 ± 0.096
t1/2, k10 (h) 0.527 ± 0.106
ka (1/h) 1.65 ± 0.364
k10 (1/h) 12.076 ± 2.337 1.133 ± 0.358
V (L/kg) 0.003 ± 0.001 0.016 ± 0.006
CL (L/h/kg) 0.024 ± 0.013 0.022 ± 0.01
Tmax (h) 0.711 ± 0.144
Cmax (ng/mL) 311.377 ± 108.017
AUC 0-inf (ng/mL*h) 495.955 ± 214.634 598.873 ± 212.319
分子量

391.53

Formula

C23H25N3OS
CAS 号
性状

固体

颜色

Off-white to pale purple

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
In Vitro: 

DMSO 中的溶解度 : ≥ 100 mg/mL (255.41 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5541 mL 12.7704 mL 25.5408 mL
5 mM 0.5108 mL 2.5541 mL 5.1082 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

μL

动物数量

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

TRPV1 antagonist 3 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 2.5541 mL 12.7704 mL 25.5408 mL 63.8521 mL
5 mM 0.5108 mL 2.5541 mL 5.1082 mL 12.7704 mL
10 mM 0.2554 mL 1.2770 mL 2.5541 mL 6.3852 mL
15 mM 0.1703 mL 0.8514 mL 1.7027 mL 4.2568 mL
20 mM 0.1277 mL 0.6385 mL 1.2770 mL 3.1926 mL
25 mM 0.1022 mL 0.5108 mL 1.0216 mL 2.5541 mL
30 mM 0.0851 mL 0.4257 mL 0.8514 mL 2.1284 mL
40 mM 0.0639 mL 0.3193 mL 0.6385 mL 1.5963 mL
50 mM 0.0511 mL 0.2554 mL 0.5108 mL 1.2770 mL
60 mM 0.0426 mL 0.2128 mL 0.4257 mL 1.0642 mL
80 mM 0.0319 mL 0.1596 mL 0.3193 mL 0.7982 mL
100 mM 0.0255 mL 0.1277 mL 0.2554 mL 0.6385 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:

TRPV1 antagonist 32765294-54-8TRP ChannelTransient receptor potential channelsCNS penetrationKM male micecapsaicinTRPM8Inhibitorinhibitorinhibit

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