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A 350619 hydrochloride

Activator of soluble guanylyl cyclase (sGC) CAS# 1217201-17-6

A 350619 hydrochloride

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Quality Control of A 350619 hydrochloride

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Chemical structure

A 350619 hydrochloride

3D structure

Chemical Properties of A 350619 hydrochloride

Cas No. 1217201-17-6 SDF Download SDF
PubChem ID 56924282 Appearance Powder
Formula C21H26Cl2N2OS M.Wt 425.41
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water
Chemical Name (E)-3-[2-(4-chlorophenyl)sulfanylphenyl]-N-[4-(dimethylamino)butyl]prop-2-enamide;hydrochloride
SMILES CN(C)CCCCNC(=O)C=CC1=CC=CC=C1SC2=CC=C(C=C2)Cl.Cl
Standard InChIKey PDVBHWZPRQFKJS-KYIGKLDSSA-N
Standard InChI InChI=1S/C21H25ClN2OS.ClH/c1-24(2)16-6-5-15-23-21(25)14-9-17-7-3-4-8-20(17)26-19-12-10-18(22)11-13-19;/h3-4,7-14H,5-6,15-16H2,1-2H3,(H,23,25);1H/b14-9+;
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of A 350619 hydrochloride

DescriptionActivator of soluble guanylyl cyclase (sGC). Activates basal sGC and synergistically activates sGC in the presence of NO. Relaxes cavernosum smooth muscle in vitro and induces penile erections in rats. Induces a sustained increase in skin blood flow in vivo.

A 350619 hydrochloride Dilution Calculator

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A 350619 hydrochloride Molarity Calculator

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Preparing Stock Solutions of A 350619 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3507 mL 11.7534 mL 23.5067 mL 47.0135 mL 58.7668 mL
5 mM 0.4701 mL 2.3507 mL 4.7013 mL 9.4027 mL 11.7534 mL
10 mM 0.2351 mL 1.1753 mL 2.3507 mL 4.7013 mL 5.8767 mL
50 mM 0.047 mL 0.2351 mL 0.4701 mL 0.9403 mL 1.1753 mL
100 mM 0.0235 mL 0.1175 mL 0.2351 mL 0.4701 mL 0.5877 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on A 350619 hydrochloride

Km: 50 μM

Nitric oxide (NO) is a key mediator in many physiological processes and one of the key receptors through which NO exerts its effects is soluble guanylyl cyclase (GC). Guanylyl cyclase converts GTP to cyclic GMP that results in physiological processes such as smooth muscle relaxation, neurotransmission, platelet aggregation inhibition and immune response. A 350619 is a novel soluble guanylyl cyclase activator.

In vitro: A 350619 increased Vmax from 0.1 to 14.5 μmol/min/mg, and lowered Km from 300 to 50 μM. When A 350619 and YC-1 (another GC activator) were combined, a 156 fold increase in Vmax and a 5 fold decrease in Km were observed, indicating the modulation of the enzyme brought about by YC-1 and A 350619 are not additive, indicating a common binding site. Activation of soluble guanylyl cyclase by A 350619 was partially inhibited by ODQ, a specific inhibitor of soluble guanylyl cyclase by oxidation of the enzyme heme [1].

In vivo: Consistent with its biochemical activity, in a conscious rat model, A 350619 (1 μmol/kg) alone induced penile erection. Activation of soluble guanylyl cyclase in cavernosum tissue as an alternate method of enhancing the effect of NO may provide a novel treatment of sexual dysfunction [2].

Clinical trial: Up to now, A 350619 is still in the preclinical development stage.

Reference:
[1] Miller LN, Nakane M, Hsieh GC, Chang R, Kolasa T, Moreland RB, Brioni JD.  A 350619: a novel activator of soluble guanylyl cyclase. Life Sci. 2003 Jan 17;72(9):1015-25.

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References on A 350619 hydrochloride

Anodal iontophoresis of a soluble guanylate cyclase stimulator induces a sustained increase in skin blood flow in rats.[Pubmed:23838678]

J Pharmacol Exp Ther. 2013 Sep;346(3):424-31.

The treatment of systemic sclerosis-related digital ulcers is challenging. Although the only effective drugs are prostacyclin analogs, their use is limited by vasodilation-related adverse reactions. In this study, we assessed the local iontophoresis administration of three soluble guanylate cyclase (A-350619 [3-[2-[(4-chlorophenyl)thiophenyl]-N-[4-(dimethylamino)butyl]-2-propenamide hydrochloride], SIN-1 [amino-3-morpholinyl-1,2,3-oxadiazolium chloride], and CFM 1571 [3-[3-(dimethylamino)propoxy]-N-(4-methoxyphenyl)-1-(phenylmethyl)-1H-pyrazole-5- carboxamide hydrochloride]) and two nonprostanoid prostaglandin I2 (prostacyclin) receptor agonists (MRE-269 [[4-[(5,6-diphenylpyrazinyl)(1-methylethyl)amino]butoxy]-acetic acid] and BMY 45778 [[3-(4,5-diphenyl[2,4'-bioxazol]-5'-yl)phenoxy]acetic acid]) to induce vasodilation onto the hindquarters of anesthetized rats. Skin blood flow was quantified using laser Doppler imaging during the whole experience, and safety was assessed by continuous recording of blood pressure and histopathological examination. Anodal iontophoresis of A-350619 (7.54 mM) induced a sustained increase in cutaneous blood flow (P = 0.008 vs. control). All other drugs exhibited poor or no effect on skin blood flow. Vasodilation with A-350619 iontophoresis was concentration-dependent (7.5, 0.75, and 0.075 mM; P < 0.001, Jonckheere-Terpstra trend test), and repeated administrations do not suggest any risk of tolerance. This study also compared continuous versus intermittent iontophoresis protocols. Continuous anodal iontophoresis of A-350619 at 7.5 mM increases cutaneous blood flow with good local tolerance. Iontophoresis of soluble guanylate cyclase stimulators should be investigated as potential local therapy for digital ulceration in patients with scleroderma.

NO-independent stimulators and activators of soluble guanylate cyclase: discovery and therapeutic potential.[Pubmed:16955067]

Nat Rev Drug Discov. 2006 Sep;5(9):755-68.

Soluble guanylate cyclase (sGC) is a key signal-transduction enzyme activated by nitric oxide (NO). Impaired bioavailability and/or responsiveness to endogenous NO has been implicated in the pathogenesis of cardiovascular and other diseases. Current therapies that involve the use of organic nitrates and other NO donors have limitations, including non-specific interactions of NO with various biomolecules, lack of response and the development of tolerance following prolonged administration. Compounds that activate sGC in an NO-independent manner might therefore provide considerable therapeutic advantages. Here we review the discovery, biochemistry, pharmacology and clinical potential of haem-dependent sGC stimulators (including YC-1, BAY 41-2272, BAY 41-8543, CFM-1571 and A-350619) and haem-independent sGC activators (including BAY 58-2667 and HMR-1766).

A-350619: a novel activator of soluble guanylyl cyclase.[Pubmed:12495780]

Life Sci. 2003 Jan 17;72(9):1015-25.

Nitric oxide (NO) is a key mediator in many physiological processes and one of the major receptors through which NO exerts its effects is soluble guanylyl cyclase. Guanylyl cyclase converts GTP to cyclic GMP as part of the cascade that results in physiological processes such as smooth muscle relaxation, neurotransmission, inhibition of platelet aggregation and immune response. The properties of A-350619, a novel soluble guanylyl cyclase activator, were examined to determine the modulatory effect on the catalytic properties of soluble guanylyl cyclase. A-350619 increased V(max) from 0.1 to 14.5 micromol/min/mg (145 fold increase), and lowered K(m) from 300 to 50 microM (6 fold decrease). When YC-1 (another sGC activator) and A-350619 were combined, a 156 fold increase in V(max) and a 5 fold decrease in Km were observed, indicating that the modulation of the enzyme brought about by YC-1 and A-350619 are not additive, suggesting a common binding site. Activation of soluble guanylyl cyclase by A-350619 was partially inhibited by ODQ, a specific inhibitor of soluble guanylyl cyclase by oxidation of the enzyme heme. YC-1 and A-350619 after pre-treatment with N-omega-nitro-L-arginine, an NO-synthase inhibitor, relaxed cavernosum tissue strips in a dose-dependent manner with EC(50) of 50 microM and 80 microM, respectively. Addition of SNP potentiated the relaxation effect of YC-1 and A-350619, shifting the dose-response curve to the left to 3 microM and 10 microM, respectively. Consistent with its biochemical activity, A-350619 (1 micromol/kg) alone induced penile erection in a conscious rat model. Activation of soluble guanylyl cyclase in cavernosum tissue as an alternate method of enhancing the effect of NO may provide a novel treatment of sexual dysfunction.

Description

Soluble guanylyl cyclase (sGC) activator

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