货号:A1492963
同义名:
PPTN (hydrochloride); PPTN hydrochloride
PPTN HCl是一种高效、选择性的 P2Y14 受体拮抗剂,KB 为 434 pM。该化合物对 P2Y1、P2Y2、P2Y4、P2Y6、P2Y11、P2Y12 和 P2Y13 受体无显著作用,具有抗炎和抗免疫活性,适用于免疫系统疾病的研究。


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| Concentration | Treated Time | Description | References | |
| HEK cells | 1 µM | PPTN inhibited UDP-glucose-mediated signalling | Br J Pharmacol. 2014 Feb;171(3):701-13. | |
| Human C6 glioma cells | 434 pM | PPTN showed selectivity for P2Y14 receptors | Br J Pharmacol. 2014 Feb;171(3):701-13. | |
| Porcine coronary artery smooth muscle cells | 1 µM | 10 min | PPTN blocked UDP-glucose and MRS2690-induced contractile responses | Vascul Pharmacol. 2018 Apr;103-105:36-46. |
| HL-60 human promyelocytic leukemia cells | 1 nM to 100 nM | 2 hours | PPTN inhibits UDP-glucose-promoted chemotaxis of HL-60 cells | Mol Pharmacol. 2013 Jul;84(1):41-9. |
| RAW264.7 macrophages | 10–100 μg/mL | 4 hours | To evaluate the antioxidative and anti-inflammatory activities of PPTN. Results showed that PPTN significantly inhibited PMA-induced ROS generation and pro-inflammatory cytokine (e.g., IL-1β and IL-6) production in macrophages. | Adv Sci (Weinh). 2025 Feb;12(8):e2405483. |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | Chronic neuropathic pain model (CCI model) | Oral | 10 μmol/kg | Single dose | 15 and its prodrugs reversed chronic neuropathic pain | J Med Chem. 2023 Jul 13;66(13):9076-9094 |
| Mice | Chronic constriction injury (CCI) model | Intraperitoneal injection | 10 μmol/kg | Single administration, observed for 1-5 h | Evaluate the antihyperallodynic effect of compound 15 in a neuropathic pain model | J Med Chem. 2022 Feb 24;65(4):3434-3459 |
| Mice | ΒENaC transgenic mice | Intranasal instillation | 100 µM | Once daily for 12 days | PPTN reduces neutrophil lung inflammation in βENaC-Tg mice | Purinergic Signal. 2016 Dec;12(4):627-635 |
| Sprague-Dawley rats | Nerve injury-induced neuropathic pain model | Intravenous injection | 5 and 10 mg/kg | Single injection or three injections on days 1, 3, and 7 | To evaluate the therapeutic effects of PPTN in neuropathic pain rats. Results showed that PPTN significantly alleviated mechanical and thermal hypersensitivity, reduced microglia and astrocyte activation in the spinal dorsal horn, and promoted nerve regeneration. | Adv Sci (Weinh). 2025 Feb;12(8):e2405483. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.95mL 0.39mL 0.20mL |
9.77mL 1.95mL 0.98mL |
19.53mL 3.91mL 1.95mL |
|
| CAS号 | 1992047-65-0 |
| 分子式 | C29H25ClF3NO2 |
| 分子量 | 511.96 |
| SMILES Code | O=C(C1=CC(C2=CC=C(C3CCNCC3)C=C2)=C4C=CC(C5=CC=C(C(F)(F)F)C=C5)=CC4=C1)O.[H]Cl |
| MDL No. | MFCD30290153 |
| 别名 | PPTN (hydrochloride); PPTN hydrochloride |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C |
| 溶解方案 |
DMSO: 250 mg/mL(488.32 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
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