2. GPCR/G Protein
  3. Prokineticin Receptor
  4. PKRA83 hydrochloride

PKRA83 hydrochloride  (Synonyms: PKRA7 hydrochloride)

目录号: HY-147056B
产品使用指南 技术支持

PKRA83 (PKRA7 ) hydrochloride 是一种可透过血脑屏障的有效的促动力 (PK2) 拮抗剂，可竞争 PK2 与其受体 PKR1 和 PKR2 的结合。PKRA83 hydrochloride 有效抑制 PK2 受体，对 PKR1 和 PKR2 的 IC50 值分别为 5.0 nM 和 8.2 nM。PKRA83 hydrochloride 具有抗癌，抗关节炎和抗血管生成活性。

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PKRA83 hydrochloride

PKRA83 hydrochloride Chemical Structure

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PKRA83 hydrochloride 的其他形式现货产品:

Customer Review

Other Forms of PKRA83 hydrochloride:

PKRA83 hydrochloride 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PKRA83 (PKRA7) hydrochloride is a potent, blood-brain-penetrating PK2 antagonist that competes for PK2 binding to its receptors, PKR1 and PKR2. PKRA83 hydrochloride potently inhibits PK2 receptors with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 hydrochloride exhibits anticancer, antiarthritis, and antiangiogenic activities[1].

IC50 & Target

IC50: 5.0 nM (PKR1) and 8.2 nM (PKR2)[1]
体外研究
(In Vitro)

PKRA83 (1 µg/mL) hydrochloride 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) hydrochloride 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]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PKRA83 hydrochloride 相关抗体:
体内研究
(In Vivo)

PKRA83 (20 mg/kg；腹腔注射) hydrochloride 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 可抑制患有胶原诱导性关节炎的小鼠的关节炎[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: glioblastoma (D456MG glioma cell) nu/nu mouse xenograft tumor model[1]
Dosage: 20 mg/kg
Administration: i.p, daily
Result: Decreased tumor growth rate and tumor weight.
Decreased relative blood vessel density and Increased areas of necrotic regions in tumors.
Animal Model: Collagen-induced arthritis in mice[2]
Dosage: 15 mg/kg
Administration: i.p, daily for 2 weeks
Result: Showed less extensive inflammatory cell infiltration and synovial thickening in the joints (Histological evaluation).
Lowered IL-1β and 1 L-6 gene expression levels in the joints.
分子量

541.48

Formula

C27H35Cl2FN2O4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PKRA83 hydrochloride 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PKRA83PKRA7PKRA 83PKRA-83PKRA 7PKRA-7Prokineticin ReceptorprokineticinPKR1PKR2anticanceranti-angiogenic activitiesblood-brain barrierarthritisInhibitorinhibitorinhibit

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