| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| Other Sizes |
| Targets |
Thiorphan targets neprilysin (NEP), also known as membrane metalloendopeptidase or enkephalinase. NEP is a zinc-dependent metalloprotease that degrades various neuropeptides, including enkephalins, substance P, and neurokinins. Thiorphan is a competitive inhibitor with an IC50 of 6.9 nM.
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|---|---|
| ln Vitro |
In vitro, Thiorphan has been shown to inhibit NEP activity with an IC50 of 6.9 nM. The compound prevents the degradation of enkephalins, substance P, and neurokinin A. It potentiates morphine-induced analgesia and attenuates naloxone-precipitated withdrawal symptoms.
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| ln Vivo |
In vivo, Thiorphan has been shown to reduce increases in gastric acid output induced by pentagastrin by 64% in rats when administered intracerebroventricularly at a dose of 50 μg, but not when administered intravenously at doses of 1.7 and 17 mg/kg. Thiorphan shows antinociceptive activity in mice and potentiates morphine-induced analgesia.
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| Enzyme Assay |
Thiorphan's enzyme inhibition activity has been characterized using purified NEP enzyme preparations. The compound is a competitive inhibitor with an IC50 of 6.9 nM. Binding assays typically involve measuring the inhibition of NEP-mediated hydrolysis of synthetic substrates such as glutaryl-Ala-Ala-Phe-2-naphthylamide.
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| Cell Assay |
In vitro cell experiments with Thiorphan involve treating cells expressing NEP with the compound and measuring the degradation of neuropeptide substrates. The compound's effects on enkephalin degradation and neuropeptide signaling are assessed using biochemical assays.
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| Animal Protocol |
In vivo animal studies with Thiorphan have been conducted using rodent models. The compound is administered intracerebroventricularly (50 μg) to study its effects on gastric acid secretion. Antinociceptive activity is assessed in mice using standard pain models. Thiorphan potentiates morphine-induced analgesia in animal models.
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| ADME/Pharmacokinetics |
Thiorphan exhibits limited oral bioavailability due to its peptide-like structure. The compound is more effective when administered centrally (intracerebroventricularly) than systemically. It is rapidly metabolized and cleared from the circulation.
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| Toxicity/Toxicokinetics |
Thiorphan is considered safe for research use at typical concentrations. The compound has been studied in animal models with no significant adverse effects reported at the doses used. As a research compound, it is intended for laboratory use only and not for human consumption.
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| References | |
| Additional Infomation |
Thiorphan is an N-acyl amino acid. It is a potent inhibitor of membrane metalloendopeptidase (enkephalinase). Thiorphan can enhance the analgesic effect of morphine and alleviate naloxone-induced withdrawal symptoms.
Thiorphan is a potent NEP inhibitor with an IC50 of 6.9 nM. It has a molecular formula of C₁₂H₁₅NO₃S. The compound is a valuable tool for studying the role of NEP in neuropeptide degradation and pain modulation. It has been used to demonstrate the involvement of enkephalins in pain regulation and morphine analgesia. |
| Molecular Formula |
C12H15NO3S
|
|---|---|
| Molecular Weight |
253.31700
|
| Exact Mass |
253.077
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| CAS # |
76721-89-6
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| Related CAS # |
Thiorphan-d7;1276297-68-7;Thiorphan-d5;2183240-70-0
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| PubChem CID |
3132
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
524.0±50.0 °C at 760 mmHg
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| Melting Point |
138-140ºC
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| Flash Point |
270.7±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.577
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| LogP |
1.37
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
17
|
| Complexity |
265
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
LJJKNPQAGWVLDQ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H15NO3S/c14-11(15)7-13-12(16)10(8-17)6-9-4-2-1-3-5-9/h1-5,10,17H,6-8H2,(H,13,16)(H,14,15)
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| Chemical Name |
2-[(2-benzyl-3-sulfanylpropanoyl)amino]acetic acid
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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) |
DMSO : ~250 mg/mL (~986.89 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.08 mg/mL (8.21 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9476 mL | 19.7379 mL | 39.4758 mL | |
| 5 mM | 0.7895 mL | 3.9476 mL | 7.8952 mL | |
| 10 mM | 0.3948 mL | 1.9738 mL | 3.9476 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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