| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Linsidomine hydrochloride targets the nitric oxide (NO)-soluble guanylate cyclase (sGC)-cGMP pathway. Upon spontaneous decomposition, it releases NO and superoxide anion, with the simultaneous generation of peroxynitrite. The released NO activates sGC, leading to increased cGMP production, vasodilation, and platelet inhibition. It is a widely used tool in redox biology as a peroxynitrite donor.
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| ln Vitro |
In vitro, linsidomine hydrochloride is used to induce oxidative and nitrative stress in a controlled manner. It releases NO and superoxide, generating peroxynitrite (ONOO⁻), a potent biological oxidant. This property makes it a valuable tool for studying the role of oxidative and nitrative stress in disease pathophysiology. In the presence of electron acceptors, it acts as an NO donor.
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| ln Vivo |
In vivo, linsidomine hydrochloride is the active metabolite of molsidomine and is responsible for its anti-anginal effects. As a spontaneous NO donor, it causes vasodilation by relaxing vascular smooth muscle. Its concomitant release of superoxide and generation of peroxynitrite may contribute to its pharmacological and toxicological profile.
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| Enzyme Assay |
In vitro assays for linsidomine hydrochloride typically involve measuring NO release. The compound is incubated in a buffer solution at physiological pH, and NO production is quantified using the Griess reaction or a chemiluminescence NO analyzer. Peroxynitrite generation can be detected using fluorescent probes such as dihydrorhodamine 123 (DHR).
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| Cell Assay |
For in vitro cell assays, cells are cultured and treated with linsidomine hydrochloride. NO-mediated effects are evaluated by measuring cGMP accumulation. Oxidative stress is assessed by measuring ROS levels using DCFH-DA. Protein nitration, a marker of peroxynitrite activity, is detected by Western blot using anti-nitrotyrosine antibodies. Cell viability is assessed by MTT assay.
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| Animal Protocol |
For in vivo animal studies, linsidomine hydrochloride is administered to rodents via intravenous or intraperitoneal injection. Blood pressure is monitored to assess its vasodilatory effects. The compound's effects on platelet aggregation and thrombosis are evaluated in appropriate models. Pharmacokinetic studies measure its concentration in plasma.
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| ADME/Pharmacokinetics |
Linsidomine hydrochloride (MW 206.63) has the molecular formula C₆H₁₁ClN₄O₂. It is a white to off-white solid and is soluble in water and DMSO. The compound is stable under recommended storage conditions (desiccated at -20°C). Its spontaneous decomposition in aqueous solution requires careful handling in experiments.
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| Toxicity/Toxicokinetics |
Linsidomine hydrochloride is for research use only. As an NO and peroxynitrite donor, it can cause oxidative and nitrative stress, which may be cytotoxic. It should be handled with care, using appropriate personal protective equipment. Its toxicity profile is related to its potent vasodilatory and oxidative effects.
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| References |
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| Additional Infomation |
Linsidomine hydrochloride (CAS# 16142-27-1) is the active metabolite of the anti-anginal drug molsidomine. It has not been approved as a standalone therapeutic agent. The compound is widely used as a pharmacological tool for studying NO signaling, oxidative stress, and peroxynitrite biology. It is also known as SIN-1 chloride.
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| Molecular Formula |
C6H11CLN4O2
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|---|---|
| Molecular Weight |
206.63
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| Exact Mass |
206.057
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| CAS # |
16142-27-1
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| Related CAS # |
3-Morpholinosydnonimine;33876-97-0
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| PubChem CID |
197942
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| Appearance |
White to off-white solid powder
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| Melting Point |
186 °C
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
13
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| Complexity |
151
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1COCCN1[N+]2=NOC(=C2)N.[Cl-]
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| InChi Key |
ZRFWHHCXSSACAW-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C6H11N4O2.ClH/c7-6-5-10(8-12-6)9-1-3-11-4-2-9;/h5H,1-4,7H2;1H/q+1;/p-1
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| Chemical Name |
3-morpholin-4-yloxadiazol-3-ium-5-amine;chloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O: 50 mg/mL (241.98 mM)
DMSO: 25 mg/mL (120.99 mM) |
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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 | 4.8396 mL | 24.1978 mL | 48.3957 mL | |
| 5 mM | 0.9679 mL | 4.8396 mL | 9.6791 mL | |
| 10 mM | 0.4840 mL | 2.4198 mL | 4.8396 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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