| Bioactivity | PKRA83 (PKRA7) hydrochloride hydrate is a potent prokineticin (PK2) antagonist, which can compete for the binding of PK2 to its receptors PKR1 and PKR2. PKRA83 hydrochloride hydrate potently inhibits PK2 receptors, with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 hydrochloride hydrate has anticancer, anti-arthritis and anti-angiogenic activities. PKRA83 hydrochloride hydrate can penetrate the blood-brain barrier[1][2][3]. |
| Invitro | PKRA83 (1 µg/mL) 可有效减少 PK2 诱导的体外微血管内皮细胞分支[1]。PKRA83 (2 μM，24 小时) 阻断 rPK2 在多巴胺能 N27 细胞中的神经保护作用 (rPK2 保护 N27 细胞免受 MPP+ 诱导的多巴胺能神经元细胞死亡)[3]。 |
| In Vivo | PKRA83 (20 mg/kg；腹腔注射) hydrochloride hydrate 在胶质母细胞瘤异种移植肿瘤模型中显示出抗肿瘤活性[1].PKRA83 (15 mg/kg；腹膜内注射，每天一次，持续 2 周) hydrochloride hydrate 可抑制患有胶原诱导性关节炎的小鼠的关节炎[2]. Animal Model: |
| Name | PKRA83 hydrochloride hydrate |
| Formula | C27H34ClFN2O4.HCl.1.5H2O |
| Molar Mass | 532.05 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Valerie F Curtis, et al. A PK2/Bv8/PROK2 antagonist suppresses tumorigenic processes by inhibiting angiogenesis in glioma and blocking myeloid cell infiltration in pancreatic cancer. PLoS One. 2013;8(1):e54916. [2]. Ito H, et al. Prokineticin 2 antagonist, PKRA7 suppresses arthritis in mice with collagen-induced arthritis. BMC Musculoskelet Disord. 2016 Sep 8;17(1):387. [3]. Gordon R, et al. Prokineticin-2 upregulation during neuronal injury mediates a compensatory protective response against dopaminergic neuronal degeneration. Nat Commun. 2016 Oct 5;7:12932. |
PKRA83 hydrochloride hydrate
CAS: F: C27H34ClFN2O4.HCl.1.5H2O W: 532.05
PKRA83 (PKRA7) hydrochloride hydrate is a potent prokineticin (PK2) antagonist, which can compete for the binding of PK2
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.