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Rp-8-CPT-cAMPS

Names

[ CAS No. ]:
129735-01-9

[ Name ]:
Rp-8-CPT-cAMPS

[Synonym ]:
Rp-8-CPT-cAMPS
sodium,(4aR,6R,7R,7aS)-6-[6-amino-8-(4-chlorophenyl)sulfanylpurin-9-yl]-2-oxido-2-sulfanylidene-4a,6,7,7a-tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinin-7-ol

Biological Activity

[Description]:

Rp-8-CPT-cAMPS, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI[1][2].

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PKA
Signaling Pathways >> Stem Cell/Wnt >> PKA
Research Areas >> Inflammation/Immunology
Research Areas >> Neurological Disease

[Target]

PKA[1]


[In Vitro]

Rp-8-CPT-cAMPS (100 μM; 15 min) blocks phosphorylation of VASP by 6-Bnz-cAMP and largely reduces VASP phosphorylation by forskolin and fenoterol[2]. Rp-8-CPT-cAMPS (100 μM; 30 min) reduces GTP-loading of Rap1 by both 8-pCPT-2'-O-Me-cAMP and 6-Bnz-cAMP[2]. Rp-8-CPT-cAMPS (100 μM; 30 min) largely diminishes the augmentation of bradykinin-induced IL-8 release by the PKA activator 6-Bnz-cAMP and the Epac activator 8-pCPT-2'-O-Me-cAMP[2]. Rp-8-CPT-cAMPS (10 μM) inhibits the endothelium-dependent and -independent relaxation which induced by Venom in pre-contracted rat mesenteric artery rings[3].

[References]

[1]. Dostmann WR , et, al. Probing the cyclic nucleotide binding sites of cAMP-dependent protein kinases I and II with analogs of adenosine 3',5'-cyclic phosphorothioates. J Biol Chem. 1990 Jun 25;265(18):10484-91.

[2]. Roscioni SS, et, al. PKA and Epac cooperate to augment bradykinin-induced interleukin-8 release from human airway smooth muscle cells. Respir Res. 2009 Sep 29;10(1):88.

[3]. Chaisakul J, et, al. In vivo and in vitro cardiovascular effects of Papuan taipan (Oxyuranus scutellatus) venom: Exploring "sudden collapse". Toxicol Lett. 2012 Sep 3;213(2):243-8.

Chemical & Physical Properties

[ Molecular Formula ]:
C16H14ClN5NaO5PS2

[ Molecular Weight ]:
509.85900

[ Exact Mass ]:
508.97600

[ PSA ]:
207.80000

[ LogP ]:
3.77360

MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

Articles

Mediation of hippocampal mossy fiber long-term potentiation by cyclic AMP.

Science 265 , 1878, (1994)

Repetitive activation of hippocampal mossy fibers evokes a long-term potentiation (LTP) of synaptic responses in pyramidal cells in the CA3 region that is independent of N-methyl-D-aspartate receptor ...


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Related Compounds

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