| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
The primary target of A-350619 hydrochloride is soluble guanylate cyclase (sGC), a key enzyme in the nitric oxide (NO) signaling pathway. sGC catalyzes the conversion of guanosine triphosphate (GTP) to cyclic guanosine monophosphate (cGMP), a second messenger that mediates vasodilation. By activating sGC, A-350619 hydrochloride increases the production of cGMP, leading to smooth muscle relaxation and improved blood flow. This mechanism is particularly relevant for the treatment of erectile dysfunction and other cardiovascular conditions.
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| ln Vitro |
In vitro, A-350619 hydrochloride functions as a soluble guanylate cyclase (sGC) activator. Its activity is characterized by its ability to stimulate cGMP production in cell-free enzymatic assays. The compound's potency as an sGC activator is determined by measuring the increase in cGMP levels. These in vitro studies confirm its mechanism of action and its potential for treating conditions associated with impaired NO-cGMP signaling, such as erectile dysfunction.
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| ln Vivo |
In vivo, A-350619 hydrochloride has been studied for its potential therapeutic applications in erectile dysfunction. By activating sGC, the compound enhances the NO-cGMP pathway, promoting vasodilation and improving penile blood flow. Its in vivo efficacy would be evaluated in animal models of erectile dysfunction, where its ability to restore erectile function would be assessed. The compound's oral bioavailability and pharmacokinetic profile are important factors for its in vivo activity.
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| Enzyme Assay |
In vitro enzyme assays for A-350619 hydrochloride measure its activation of soluble guanylate cyclase (sGC). The enzyme is incubated with the compound, and the production of cGMP from GTP is quantified using methods such as radioimmunoassay or ELISA. The compound's EC₅₀, which represents the concentration required for half-maximal activation, is determined from dose-response curves. These assays are standard for characterizing sGC activators.
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| Cell Assay |
In vitro cell-based assays for A-350619 hydrochloride evaluate its effects on cellular signaling. Cells expressing sGC, such as smooth muscle cells or platelets, are treated with the compound, and intracellular cGMP levels are measured. The compound's ability to potentiate the effects of NO donors can also be assessed. These assays help to confirm its mechanism of action and its potential for modulating vascular function.
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| Animal Protocol |
In vivo animal studies for A-350619 hydrochloride would typically involve models of erectile dysfunction. The compound is administered orally or intravenously, and its effects on erectile function are assessed by measuring intracavernosal pressure or by evaluating the relaxation of corpus cavernosum tissue. Pharmacokinetic studies are conducted to determine its absorption, distribution, metabolism, and excretion. All procedures must comply with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of A-350619 hydrochloride have been characterized in preclinical studies. The compound is soluble in DMSO and may be formulated for in vivo administration. Its molecular weight is 425.41 g/mol. For research use, it is stored as a powder at -20°C for up to 3 years or in solvent at -80°C for up to 6 months. Further details on its half-life, Cmax, and bioavailability would be available from published studies.
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| Toxicity/Toxicokinetics |
The toxicity profile of A-350619 hydrochloride has not been extensively detailed in the available literature. It is classified for research use only and not for human consumption. As an sGC activator, its potential side effects may include hypotension and headache, which are common to vasodilators. Standard safety precautions for handling bioactive compounds should be followed.
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| Additional Infomation |
Additional information: A-350619 hydrochloride has the CAS number 1217201-17-6. Its IUPAC name is (E)-3-[2-(4-chlorophenyl)sulfanylphenyl]-N-[4-(dimethylamino)butyl]prop-2-enamide;hydrochloride. The compound is a soluble guanylate cyclase (sGC) activator. It is intended for research purposes only and is not for human therapeutic use.
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| Molecular Formula |
C21H26CL2N2OS
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|---|---|
| Molecular Weight |
425.414942264557
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| Exact Mass |
424.114
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| CAS # |
1217201-17-6
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| PubChem CID |
56924282
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
27
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| Complexity |
436
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.CN(CCCCNC(/C=C/C1=CC=CC=C1SC1=CC=C(Cl)C=C1)=O)C
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| InChi Key |
PDVBHWZPRQFKJS-KYIGKLDSSA-N
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| InChi Code |
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+;
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| Chemical Name |
(E)-3-[2-(4-chlorophenyl)sulfanylphenyl]-N-[4-(dimethylamino)butyl]prop-2-enamide;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3507 mL | 11.7534 mL | 23.5067 mL | |
| 5 mM | 0.4701 mL | 2.3507 mL | 4.7013 mL | |
| 10 mM | 0.2351 mL | 1.1753 mL | 2.3507 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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