TRPV1 antagonist 3
目录号 : GC70067TRPV1 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。
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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].
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].
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].
| 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]
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[1]. Yue Qiao, et al. Discovery of (S)-N-(3-isopropylphenyl)-2-(5-phenylthiazol-2-yl)pyrrolidine-1-carboxamide as potent and brain-penetrant TRPV1 antagonist. Eur J Med Chem. 2022 Apr 5;233:114191.
| Cas No. | SDF | Download SDF | |
| 分子式 | C23H25N3OS | 分子量 | 391.53 |
| 溶解度 | DMSO : ≥ 100 mg/mL (255.41 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 10 mM | 0.2554 mL | 1.277 mL | 2.5541 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。