JYL 1421 (SC 0030)
(Synonyms: SC 0030) 目录号 : GC31236
A TRPV1 antagonist
Cas No.:401907-26-4
Sample solution is provided at 25 µL, 10mM.
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JYL1421 is an antagonist of transient receptor potential vanilloid 1 (TRPV1).1 It inhibits calcium uptake induced by capsaicin in CHO cells expressing rat TRPV1 (EC50 = 9.2 nM). JYL1421 inhibits capsaicin-induced release of the neuropeptides somatostatin, substance P , and calcitonin gene-related peptide (CGRP) from isolated rat trachea (IC50s = 227-491 nM).2 It inhibits capsaicin-induced hypothermia and hypotension in rats when administered at doses of 2 and 0.4 mg/kg, respectively. JYL1421 (2 mg/kg) also reduces the number of wiping movements induced by ocular administration of capsaicin in rats. Unlike several other TRPV1 antagonists, JYL1421 does not induce hyperthermia in rats when administered at doses ranging from 1.02 to 32.77 μmol/kg.3
1.Wang, Y., Szabo, T., Welter, J.D., et al.High affinity antagonists of the vanilloid receptorMol. Pharmacol.62(4)947-956(2002) 2.Jakab, B., Helyes, Z., Varga, A., et al.Pharmacological characterization of the TRPV1 receptor antagonist JYL1421 (SC0030) in vitro and in vivo in the ratEur. J. Pharmacol.517(1-2)35-44(2005) 3.Garami, A., Shimansky, Y.P., Pakai, E., et al.Contributions of different modes of TRPV1 activation to TRPV1 antagonist-induced hyperthermiaJ. Neurosci.30(4)1435-1440(2010)
Animal experiment: | Rats[1]Pretreatment with JYL 1421 (0.4, 1, 2, or 5 mg/kg) is performed i.p. 20 min before capsaicin administration. In control rats the solvent is injected in the same volume, in the reference group capsazepine (2 or 5 mg/kg) is administered i.p. The number of wiping movements in response to 50 μL capsaicin solution (10 μg/mL) drops into the left eye of male Wistar rats (180-220 g) is determined during 60 s after instillation. The body temperature is maintained at 37°C by a heating lamp. Drugs are administered through a cannula inserted into the right jugular vein. The pulmonary chemoreflex is evoked by rapid injections of capsaicin (1 and 2 μg/kg i.v.) separated by a 5 min interval. Thereafter JYL 1421 (0.4 and 1.6 mg/kg i.v.) is administered and 5 min later capsaicin injections are repeated at increasing doses until the magnitude of the control responses could be achieved. For quantitative analysis the area under the curve (AUC) of the capsaicin-induced hypotension is determined[1]. |
References: [1]. Jakab B, et al. Pharmacological characterization of the TRPV1 receptor antagonist JYL1421 (SC0030) in vitro and in vivo in the rat. Eur J Pharmacol. 2005 Jul 4;517(1-2):35-44. | |
| Cas No. | 401907-26-4 | SDF | |
| 别名 | SC 0030 | ||
| Canonical SMILES | CS(=O)(NC1=CC=C(CNC(NCC2=CC=C(C(C)(C)C)C=C2)=S)C=C1F)=O | ||
| 分子式 | C20H26FN3O2S2 | 分子量 | 423.57 |
| 溶解度 | Soluble in DMSO | 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 | 2.3609 mL | 11.8044 mL | 23.6088 mL |
| 5 mM | 0.4722 mL | 2.3609 mL | 4.7218 mL |
| 10 mM | 0.2361 mL | 1.1804 mL | 2.3609 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 | ||||||||||
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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.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet