Names
| Name | Disodium 1-amino-4-[(4-anilino-3-sulfonatophenyl)amino]-9,10-diox o-9,10-dihydro-2-anthracenesulfonate |
|---|
PSB 0739 Biological Activity
| Description | PSB-0739 is a high-affinity potent, competitive, nonselective platelet P2Y12 receptor antagonist with a Ki values of 24.9 nM. The P2Y12 receptor plays a crucial role in platelet aggregation. Antithrombotic effect[1]. |
|---|
| Related Catalog | Research Areas >> Cardiovascular Disease Signaling Pathways >> GPCR/G Protein >> P2Y Receptor |
|---|
| In Vitro | PSB-0739 is a potent competitive non-nucleotide antagonist at the human P2Y12 receptor with a pA2 value of 9.8[2]. PSB-0739 inhibits ADP-evoked Ca2+ responses with an EC50 of 5.4±1.8 μM and causes a rightward parallel shift in the ADP concentration–response curve in THP-1 cells[3]. Cell Viability Assay[3] Cell Line: THP-1 monocytic cell line Concentration: 10 nM, 100 nM, 1 μM, 10 μM Incubation Time: Result: Attenuated ADP-evoked responses (IC50=5.4±1.8 μM). |
|---|
| In Vivo | PSB-0739 (0.01-0.3 mg/kg, intrathecally) has dose-dependent and significant antihyperalgesic effect in low doses. The minimal effective dose (mED) is 0.1 mg/kg[4]. Animal Model: Male Wistar rats, 150-250 g, 6-8/group[4] Dosage: 0.01, 0.03, 0.1, 0.3 mg/kg Administration: Intrathecal injection ( i.t.) Result: Displayed a dose-dependent inhibitory effect on mechanical hyperalgesia in the range of 0.01–0.1 mg/kg. |
|---|
| References | [1]. Younis Baqi, et al. High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y12 receptors. J Med Chem. 2009 Jun 25;52(12):3784-93. [2]. Kristina Hoffmann, et al. Interaction of new, very potent non-nucleotide antagonists with Arg256 of the human platelet P2Y12 receptor. J Pharmacol Exp Ther. 2009 Nov;331(2):648-55. [3]. J J Micklewright,et al. P2Y 12 receptor modulation of ADP-evoked intracellular Ca2+ signalling in THP-1 human monocytic cells. Br J Pharmacol.2018 Jun;175(12):2483-2491. [4]. Gergely Horváth, et al. Central P2Y12 receptor blockade alleviates inflammatory and neuropathic pain and cytokine production in rodents. Neurobiol Dis. 2014 Oct;70(100):162-78. |
|---|
Chemical & Physical Properties
| Molecular Formula | C26H17N3Na2O8S2 |
|---|
| Molecular Weight | 609.54 |
|---|
| Exact Mass | 609.02500 |
|---|
| PSA | 215.38000 |
|---|
| LogP | 6.22840 |
|---|
Company Profile
Our company is a high-tech enterprise specializing in chemical raw materials such as electronic materials, optoelectronic materials, semiconductor materials, UV monomers, silane catalysts, cosmetic raw materials, etc. The company integrates research and development, production, customized synthesis, and sales, and is committed to providing customers with high-quality chemical product solutions.
Our Company
Our Advantage
Rich experience
Our products have been exported to many countries, including Germany, Spain, the United Kingdom, the United States, Australia, the Middle East, Asia, and more. We have received highly positive feedback from our clients and have established long-term friendly cooperative relationships with them.
Excellent quality, purity, and competitive price
Excellent quality is one of the cornerstones of our success. We welcome ordering samples for quality testing.
Safe and fast delivery
We will arrange shipment of spot products as soon as we receive payment.
Customized products are determined based on the synthesis time of different products.
Excellent pre-sales and after-sales service
Pre sales:
We are committed to providing the most favorable quotes and detailed information about our products and company.
after-sale service:
We assist buyers in customs clearance by providing necessary documents and information.
If there is any dispute over product quality, we are committed to providing the best solution.
• Packaging:
1kg/bag, 25kg/drum, 50kg/drum, 180kg/drum, 200kg/drum, 1T/bag/drum, standard export packaging or packaging required by customers
• Shipping
• Delivery:
Within 7 days after receiving your payment
Contact information
For more details, pls contact us freely.
Contact name: Tina
Email address: Tina@fdachem.com
Mob: 86 13213167925
WhatsApp/Skype/Wechat/LINE: 86 15225627621
China
