YL-365是一种强效的GPR34拮抗剂，IC50值为17nM。
Sample solution is provided at 25 µL, 10mM.
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YL-365 is a potent GPR34 antagonist with an IC50 value of 17nM [1]. YL-365 competitively binds to the region of the GPR34 orthosteric binding pocket and induces receptor conformational changes to exert an inhibitory effect [2]. YL-365 is widely used for targeting the ADAM8 gene to inhibit the progression of clear cell renal cell carcinoma[3].
In vivo, YL-365 treatment via intraperitoneal injection at a dose of 20mg/kg (twice a day) for 3 days substantially reduced mechanical allodynia in the mouse model of neuropathic pain with the L4 spinal nerve being cut off [2].
References:
[1] Chakraborty A, Kamat S S. Lysophosphatidylserine: A signaling lipid with implications in human diseases[J]. Chemical reviews, 2024, 124(9): 5470-5504.
[2] Xia A, Yong X, Zhang C, et al. Cryo-EM structures of human GPR34 enable the identification of selective antagonists[J]. Proceedings of the National Academy of Sciences, 2023, 120(39): e2308435120.
[3] Wu Y, Zhang Y, Sun K, et al. Prognostic significance of key immune cell functional alterations in clear cell renal cell carcinoma[J]. Translational Cancer Research, 2025, 14(10): 6364-6387.
YL-365是一种强效的GPR34拮抗剂，IC50值为17nM[1]。YL-365 竞争性结合至GPR34正构结合口袋区域，并诱导受体构象变化以发挥抑制作用[2]。YL-365被广泛用于靶向ADAM8基因，以抑制透明细胞肾细胞癌的进展[3]。
在体内，通过腹腔注射YL-365，剂量为20mg/kg（每日两次），连续3天，显著减轻了L4脊神经切断的神经病理性疼痛小鼠模型中的机械性痛觉超敏[2]。
| Animal experiment [1]: | |
Animal models | C57BL/6J mice |
Preparation Method | Male C57BL/6J (6 weeks old) were maintained on a 12:12 light–dark cycle at a room temperature of 22±1℃.To produce the spinal nerve injury (SNI) in mice, the mice were anesthetized with isoflurane and the L4 spinal nerves were cut off. For sham operations, the L4 spinal nerve was exposed but not cut off. Mice were intraperitoneal injected with vehicle or YL-365 (20mg/kg; i.p.; twice a day) 5h after operation. The mechanical allodynia was assessed by the plantar aesthesiometer following 3-day administration of vehicle or YL-365. |
Dosage form | 20mg/kg; twice a day for 3 days; i.p. |
Applications | YL-365 treatment substantially reduced mechanical allodynia in mice. |
References: | |
| Cas No. | SDF | ||
| 分子式 | C34H31ClN2O5 | 分子量 | 583.07 |
| 溶解度 | 储存条件 | 4°C, protect from light | |
| 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7151 mL | 8.5753 mL | 17.1506 mL |
| 5 mM | 343 μL | 1.7151 mL | 3.4301 mL |
| 10 mM | 171.5 μL | 857.5 μL | 1.7151 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。
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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