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PKRA83

Catalog No.GC70984

PKRA83 (PKRA7) is a potent prokineticin (PK2) antagonist, which can compete for the binding of PK2 to its receptors PKR1 and PKR2.

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PKRA83 Chemical Structure

Cas No.: 1233926-87-8

Size Price Stock Qty
5 mg
$162.00
In stock
10 mg
$284.00
In stock
25 mg
$599.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Description of PKRA83

PKRA83 (PKRA7) is a potent prokineticin (PK2) antagonist, which can compete for the binding of PK2 to its receptors PKR1 and PKR2. PKRA83 potently inhibits PK2 receptors, with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 has anticancer, anti-arthritis and anti-angiogenic activities. PKRA83 can penetrate the blood-brain barrier.

PKRA83 (1 µg/mL) effectively reduces PK2-induced microvascular endothelial cell branching in vitro[1].
PKRA83 (2 μM, 24 h) blocks the neuroprotective action of rPK2 in dopaminergic N27 cells (rPK2 protects N27 cell against MPP+-induced dopaminergic neuronal cell death)[3].

PKRA83 (20 mg/kg; i.p) shows anti-tumor activity in the context of glioblastoma xenograft tumor models[1].
PKRA83 (15 mg/kg; i.p, daily for 2 weeks) inhibits arthritis in mice with collagen-induced arthritis[2].

References:
[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.

Chemical Properties of PKRA83

Cas No. 1233926-87-8 SDF
Formula C27H34ClFN2O4 M.Wt 505.02
Solubility DMSO : 25 mg/mL (49.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Storage -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of PKRA83

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1 mg 5 mg 10 mg
1 mM 1.9801 mL 9.9006 mL 19.8012 mL
5 mM 0.396 mL 1.9801 mL 3.9602 mL
10 mM 0.198 mL 0.9901 mL 1.9801 mL
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In vivo Formulation Calculator (Clear solution) of PKRA83

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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