An analog of suramin that selectively inhibits P2X1 receptors (pIC50 = 6.3); selectively antagonizes the Gsα-subunit G protein

NF449 (sodium salt) – 1 mg

Brand:
Cayman
CAS:
627034-85-9
Storage:
-20
UN-No:
Non-Hazardous - /

NF449 is an analog of suramin that selectively inhibits P2X1 purinergic receptors (pIC50 = 6.3) with a potency 19-fold greater than at P2X3, P2Y1, P2Y2, or P2Y11.{23042,23041} Through selective inhibition of the P2X1 receptor, 10 mg/kg NF449 has been used to decrease intravascular platelet aggregation in a mouse model of systemic thromboembolism.{23040} NF449 has also demonstrated selective antagonism of the Gsα-subunit G protein, which suppresses the association rate of GTPγS binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks G protein coupling to certain GPCRs.{23039}  

 

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Description

An analog of suramin that selectively inhibits P2X1 receptors (pIC50 = 6.3); selectively antagonizes the Gsα-subunit G protein, which suppresses the association rate of GTPγS binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks G protein coupling to certain GPCRs

Formal name: 4,4′,4”,4”’-[carbonylbis[imino-5,1,3-benzenetriylbis(carbonylimino)]]tetrakis-1,3-benzenedisulfonic acid, octasodium salt

Synonyms: 

Molecular weight: 1,505.10

CAS: 627034-85-9

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Cardiovascular System|Blood|Thrombosis

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