SR 17018 is an orally bioavailable and brain-penetrant agonist of μ-opioid receptors. It is functionally selective for G protein-coupled receptor signaling (EC50 = 97 nM for GTPγS binding in CHO cells expressing μ-opioid receptors) over β-arrestin 2 recruitment (EC50 = >10,000 nM) at the μ-opioid receptor. SR 17018 increases latency to withdraw in the hot plate and warm water tail-flick assay (ED50s = 6.9 and 7.7 mg/kg, respectively) without inducing respiratory depression in mice when administered at doses up to 48 mg/kg. SR 17018 was designed for this biased agonism at the μ-opioid receptor to potentially widen the therapeutic window and reduce adverse effects of μ-opioid receptors, such as respiratory depression.
SR 17018
目录号: GC18317纯度: >98.00%
A functionally-selective μ-opioid receptor agonist
Cas No.: 2134602-45-0
| 规格 | 价格 | 库存 | 数量 | 操作 |
|---|---|---|---|---|
| 5mg | ¥720.00 | 现货 | 1 | |
| 10mg | ¥1,170.00 | 现货 | 1 | |
| 50mg | ¥3,780.00 | 现货 | 1 | |
| 10mM 1 mL in DMSO | ¥792.00 | 现货 | 1 |
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文献被引
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Nature641, 529–536 (2025)
Nature628, 630–638 (2024)
Nature632, 686–694 (2024)
Nature618, 1017–1023 (2023)
Nature610, 366–372 (2022)
Cell187(9):2288-2304 (2024)
Cell183(7):1867-1883 (2020)
Science388(6745) (2025)
Science387(6739) (2025)
Science387(6734) (2025)
Cell Research35, 97–116 (2025)
Cell Research34, 683–706 (2024)
Cell Research33, 273–287 (2023)
Cell Research33, 546–561 (2023)
Cell Research33, 904–922 (2023)
Cell Research31, 1291–1307 (2021)
产品描述 Description
产品文档 Product Documents
Purity:>98.00%
化学性质Chemical Properties
CAS 号
2134602-45-0
化学名
5,6-dichloro-1-[1-[(4-chlorophenyl)methyl]-4-piperidinyl]-1,3-dihydro-2H-benzimidazol-2-one
SMILES
ClC(C=C1)=CC=C1CN2CCC(N3C(NC4=C3C=C(Cl)C(Cl)=C4)=O)CC2
分子式
C19H18Cl3N3O
分子量
410.7 g/mol
溶解性
DMF: 1 mg/ml,DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml,Ethanol: slightly soluble
保存条件
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°C，然后在超声波浴中震荡一段时间。
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°C，然后在超声波浴中震荡一段时间。
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。
计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度
g/mol