| Size | Price | Stock | Qty |
|---|---|---|---|
| 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) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (12.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Suspended solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (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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