Siguazodan - CAS 115344-47-3
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C14H16N6O
Molecular Weight:
284.32
COA:
Inquire
Targets:
Phosphodiesterase (PDE)
Description:
Siguazodan is a selective phosphodiesterase 3 (PDE3) inhibitor (IC50 = 117 nM). Siguazodan acts as a potent vasodilator.
Brife Description:
PDE3 inhibitor
Purity:
≥99% by HPLC
Synonyms:
N-Cyano-N'-methyl-N''-[4-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl]guanidine; SKF 94836; SKF-94836; SKF94836
MSDS:
Inquire
Application:
vasodilator
InChIKey:
NUHPODZZKHQQET-UHFFFAOYSA-N
InChI:
InChI=1S/C14H16N6O/c1-9-7-12(21)19-20-13(9)10-3-5-11(6-4-10)18-14(16-2)17-8-15/h3-6,9H,7H2,1-2H3,(H,19,21)(H2,16,17,18)
Canonical SMILES:
CC1CC(=O)NN=C1C2=CC=C(C=C2)NC(=NC)NC#N
1.Rolipram, but not siguazodan or zaprinast, inhibits the excitatory noncholinergic neurotransmission in guinea-pig bronchi.
Qian Y;Girard V;Martin CA;Molimard M;Advenier C Eur Respir J. 1994 Feb;7(2):306-10.
Theophylline has been reported to inhibit excitatory noncholinergic but not cholinergic-neurotransmission in guinea-pig bronchi. As theophylline might exert this effect through an inhibition of phosphodiesterases (PDE), and since many types of PDE have now been described, the aim of this study was to investigate the effects of three specific inhibitors of PDE on the electrical field stimulation (EFS) of the guinea-pig isolated main bronchus in vitro. The drugs used were siguazodan, rolipram and zaprinast, which specifically inhibit PDE types, III, IV and V, respectively. Guinea-pig bronchi were stimulated transmurally with biphasic pulses (16 Hz, 1 ms, 320 mA for 10 s) in the presence of indomethacin 10(-6) M and propranolol 10(-6) M. Two successive contractile responses were observed: a rapid cholinergic contraction, followed by a long-lasting contraction due to a local release of neuropeptides from C-fibre endings. Rolipram (10(-9) to 10(-6) M) but not siguazodan or zaprinast, inhibited the peptidergic contraction in a concentration-dependent manner. Conversely, the cholinergic response was unaffected. Contractile responses induced by exogenous acetylcholine (10(-8) to 10(-3) M) or [Nle10]NKA(4-10) (10(-10) to 10(-6) M) were also unaffected by rolipram, siguazodan and zaprinast (10(-7) M).
2.Modulation of oxazolone-induced hypersensitivity in mice by selective PDE inhibitors.
Moodley I;Sotsios Y;Bertin B Mediators Inflamm. 1995;4(2):112-6.
The effects of PDE inhibitors on oxazolone-induced contact hypersensitivity (CS) were studied in mice. Rolipram, Ro 20-1724 and theophylline dose dependently inhibited CS but none caused >53% inhibition. ED(30) values at 24 h before challenge for rolipram, Ro 20-1724 and theophylline were 2.1, 5.4 and 30.4 mg/kg, p.o., respectively. Milrinone and SKF 94836 at 30 mg/kg caused a small, but significant inhibition of 13% and 18%, respectively, although the inhibition (8%) caused by zaprinast was not significant. Betamethasone (10 mg/kg, p.o.) caused a marked inhibition (80%) as did indomethacin (65% at 5 mg/kg, p.o.). Rolipram and Ro 20-1724 inhibited proliferation of mouse lymphoblasts with IC(50) values of 0.08 muM and 0.83 muM, respectively. In contrast, zaprinast caused only a weak inhibition (IC(50) = 119 muM) of lymphocyte proliferation, whereas SKF 94836 and theophylline failed to cause any significant inhibition at 100 muM (26% and 2%, respectively). These findings suggest that PDE IV isozymes play a principal role in mediating CS by inhibiting lymphocyte activation.
3.Preliminary identification and role of phosphodiesterase isozymes in human basophils.
Peachell PT;Undem BJ;Schleimer RP;MacGlashan DW Jr;Lichtenstein LM;Cieslinski LB;Torphy TJ J Immunol. 1992 Apr 15;148(8):2503-10.
We attempted to identify and establish the role of cyclic nucleotide phosphodiesterase (PDE) isozymes in human basophils by using standard biochemical techniques as well as describing the effects of isozyme-selective and nonselective inhibitors of PDE. The nonselective PDE inhibitors, theophylline and 3-isobutyl-1-methylxanthine, inhibited anti-IgE-induced release of histamine and leukotriene C4 (LTC4) from basophils. This inhibition was accompanied by elevations in cAMP levels. Rolipram, an inhibitor of the low Km cAMP-specific PDE (PDE IV), inhibited the release of both histamine and LTC4 from activated basophils and increased cAMP levels in these cells. In contrast, mediator release from basophils was not inhibited by either siguazodan or SK&F 95654, inhibitors of the cGMP-inhibited PDE (PDE III) or zaprinast, an inhibitor of the cGMP-specific PDE (PDE V). SK&F 95654 failed to elevate basophil cAMP in these experiments whereas zaprinast induced significant increases in cAMP content. The inhibitory effect of rolipram on mediator release was potentiated by siguazodan or SK&F 95654, but not by zaprinast. SK&F 95654 also enhanced the ability of rolipram to increase cAMP content. Forskolin, a direct activator of adenylate cyclase, inhibited IgE-dependent release of mediators from basophils and increased cAMP levels in these cells.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Phosphodiesterase (PDE) Products


CAS 947620-48-6 RVT-501

RVT-501
(CAS: 947620-48-6)

RVT-501, also referred to E6005, is a selective phosphodiesterase 4 (PDE4) inhibitor (IC50= 2.8 nM) with potential effect to treat atopic dermatitis.

CAS 1236858-52-8 PF 04449613

PF 04449613
(CAS: 1236858-52-8)

PF 04449613 is a potent PDE9 inhibitor (IC50 = 22 nM), and also shows a high affinity for cGMP (Km ~170 nM). Some studies suggest that elevating the level of cG...

CAS 78351-75-4 MY-5445

MY-5445
(CAS: 78351-75-4)

MY-5445 is a specific inhibitor of cyclic GMP phosphodiesterase, selective for PDE5, with a Ki value of 1.3 µM. It inhibits calcium- and cAMP-selective PDEs wit...

CI-1018
(CAS: 245329-99-1)

CI-1018 is a selective type 4 phosphodiesterase inhibitor associated with vasculitis. CI-1018 has been in development to suppress inflammation.

CK 3197
(CAS: 132523-92-3)

CK 3197 is a Phosphoric diester hydrolase inhibitor originated by Bayer HealthCare Pharmaceuticals. CK 3197 has hemodynamic and myocardial energetic effects. In...

CAS 1229652-21-4 HA-130

HA-130
(CAS: 1229652-21-4)

HA-130, an effective autotaxin (ATX) inhibitor, has been found to restrain the cell migration related to ATX in in an A2058 melanoma cells. IC50: 28 nM.

CAS 50847-11-5 Ibudilast

Ibudilast
(CAS: 50847-11-5)

Ibudilast is a nonselective inhibitor of cyclic nucleotide phosphodiesterase (PDE) which has been marketed for treating asthma. It crosses the blood-brain barri...

CAS 189362-06-9 K134

K134
(CAS: 189362-06-9)

K134 is a selective phosphodiesterase 3 (PDE3) inhibitor, and has been shown to exhibit more potent anti-platelet activity than cilostazol. In vivo studies have...

Chemical Structure

CAS 115344-47-3 Siguazodan

Quick Inquiry

Verification code

Featured Items